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LY2603618 (IC-83)

Catalog No. A11036
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Chk 抑制剂

LY2603618 (IC-83)是一种chk2抑制剂，可与chk2结合并抑制其活性，这可能会阻止DNA损伤剂引起的DNA修复。了解更多

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- Hayakawa K, .et al. Planar compression of extracellular substrates induces S phase arrest via ATM-independent CHK2 activation, Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
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VX-765 (Belnacasan)

Catalog No. A10984
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Caspase-1/4 抑制剂

VX-765 (Belnacasan)是一种新型的Caspase-1抑制剂，是一种控制两种细胞因子IL-1b和IL-18生成的酶。了解更多

Product Citations (7)

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- Arjun Thapa, .et al. Danger-associated molecular pattern molecules take unexpectedly a central stage in Nlrp3 inflammasome-caspase-1-mediated trafficking of hematopoietic stem/progenitor cells, Leukemia, 2021, 23 February
- Prenitha Mercy Ignatius Arokia Doss, .et al. Male sex chromosomal complement exacerbates the pathogenicity of Th17 cells in a chronic model of central nervous system autoimmunity, Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. Pre-symptomatic Caspase-1 inhibitor delays cognitive decline in a mouse model of Alzheimer disease and aging, Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. Caspase-1 inhibition alleviates cognitive impairment and neuropathology in an Alzheimer's disease mouse model, Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. Canonical Stimulation of the NLRP3 Inflammasome by Fungal Antigens Links Innate and Adaptive B-Lymphocyte Responses by Modulating IL-1β and IgM Production, Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. Targeting inflammasome by the inhibition of caspase-1 activity using capped mesoporous silica nanoparticles, J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. Inflammasome activation leads to Caspase-1-dependent mitochondrial damage and block of mitophagy, Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
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Vorinostat (SAHA)

Catalog No. A10979
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HDAC 抑制剂

Vorinostat (SAHA)是HDAC的抑制剂，抑制脱乙酰和导致双方超乙酰化组蛋白和转录因子的积累。了解更多

Product Citations (5)

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- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- David Diaz-Carballo, .et al. Enhanced antitumoral activity of TLR7 agonists via activation of human endogenous retroviruses by HDAC inhibitors, Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Arshdeep Singh, .et al. CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition, Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Shariful Islam, .et al. Resistance to histone deacetylase inhibitors confers hypersensitivity to oncolytic reovirus therapy, Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. Virtual and In Vitro Antiviral Screening Revive Therapeutic Drugs for COVID-19, ACS Pharmacol Transl Sci, 2020, Oct 14
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Droxinostat

Catalog No. A10337
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HDAC 抑制剂

Droxinostat是HDAC3，HDAC6和HDAC8的选择性抑制剂，显示出可比较的HDAC6和HDAC8抑制作用，IC50分别为2.47和1.46μmol/ L。了解更多

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MK-1775

Catalog No. A10599
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WEE1 抑制剂

MK-1775是一种有效的体外和体内Wee1激酶抑制剂。了解更多

Product Citations (3)

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- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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Moxifloxacin HCl

Catalog No. A10609
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Topoisomerase 抑制剂

Moxifloxacin HCl是一种喹诺酮/氟喹诺酮类抗菌剂。了解更多

Product Citations (2)

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- Hiroshi Arakawa, .et al. Possible interaction of quinolone antibiotics with peptide transporter 1 in oral absorption of peptide-mimetic drugs, Biopharm Drug Dispos, 2016, Jan;37(1):39-45 PMID: 26590007
- Arisa Higa, .et al. Differing responses of human stem cell-derived cardiomyocytes to arrhythmogenic drugs, determined using impedance measurements, Fundam. Toxicol. Sci, 2016, 3(2): 47-53
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Tandutinib (MLN518)

Catalog No. A10887
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FLT3 抑制剂

Tandutinib (MLN518)是一种有效的FLT3抑制剂，c-KIT和PDGF受体酪氨酸激酶的自磷酸化，从而抑制细胞增殖并诱导细胞凋亡。了解更多

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SB 203580

Catalog No. A10824
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p38 MAPK 抑制剂

SB 203580是p38α和p38β的特异性抑制剂，可抑制MAPKAP激酶2和热激蛋白27的下游激活。了解更多

Product Citations (9)

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- Lei Zhang, .et al. Ripk3 signaling regulates HSCs during stress and represses radiation-induced leukemia in mice, Stem Cell Reports, 2022, Jun 14;17(6):1428-1441 PMID: 35561683
- Tomoyuki Hashimoto, .et al. Development of radioiodinated pyrimidinopyridone derivatives as targeted imaging probes of activated p38α for single photon emission computed tomography, Ann Nucl Med, 2021, Aug 19 PMID: 34410619
- Y Zou, .et al. Autophagy inhibition enhances Matrine derivative MASM induced apoptosis in cancer cells via a mechanism involving reactive oxygen species-mediated PI3K/Akt/mTOR and Erk/p38 signaling, BMC Cancer, 2019, Oct 15;19(1):949 PMID: 31615459
- Wei P, .et al. Transforming growth factor (TGF)-β1-induced miR-133a inhibits myofibroblast differentiation and pulmonary fibrosis, Cell Death Dis, 2019, Sep 11;10(9):670 PMID: 31511493
- Uwada J, .et al. Store-operated calcium entry (SOCE) contributes to phosphorylation of p38 MAPK and suppression of TNF-α signalling in the intestinal epithelial cells, Cell Signal, 2019, Nov;63:109358 PMID: 31295519
- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Uwada J, .et al. Activation of muscarinic receptors prevents TNF-α-mediated intestinal epithelial barrier disruption through p38 MAPK, Cell Signal, 2017, Jul;35:188-196 PMID: 28412413
- ZHIQIANG ZHANG, .et al. Tumor necrosis factor-like weak inducer of apoptosis regulates particle-induced inflammatory osteolysis via the p38 mitogen-activated protein kinase signaling pathway., Mol Med Rep. , 2015, Jul;12(1):1499-505. PMID: 25815691
- Choe YJ, .et al. Nutlin-3 induces HO-1 expression by activating JNK in a transcription-independent manner of p53., Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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SB 431542

Catalog No. A10826
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TGF-beta/Smad 抑制剂

SB 431542是转化生长因子-β超家族I型激活素受体样激酶（ALK）受体ALK4，ALK5和ALK7的有效抑制剂。了解更多

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- Huong Pham, .et al. BMP11 Negatively Regulates Lipid Metabolism in C2C12 Muscle Cells, Biotechnol Bioprocess Eng, 2020, ID: 222137835
- Tamara Chamberlin, .et al. Obesity Reduces Mammary Epithelial Cell TGFβ1 Activity Through Macrophage-Mediated Extracellular Matrix Remodeling, FASEB J, 2020, Jun;34(6):8611-8624 PMID: 32359100
- Satoshi Endo, .et al. Flavonol glycosides of Rosa multiflora regulates intestinal barrier function through inhibiting claudin expression in differentiated Caco-2 cells, Nutr Res, 2019, 4 November
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WYE-125132 (WYE-132)

Catalog No. A11038
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mTOR 抑制剂

WYE-125132 (WYE-132)是一种高度有效的，ATP竞争性的mTOR抑制剂，IC50为0.19 nM；作用于mTOR比作用于PI3Ks或PI3K相关激酶hSMG1和ATR选择性高。了解更多

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MLN8054

Catalog No. A10601
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Aurora A 抑制剂

MLN8054是一种有效的，选择性Aurora A抑制剂，在Sf9昆虫细胞中IC50为4 nM，作用于Aurora A比作用于Aurora B选择性高40倍，可在体内和体外诱导人肿瘤细胞衰老。了解更多

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ICG-001

Catalog No. A11039
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Wnt/beta-catenin 抑制剂

ICG-001是Wnt/β-catenin信号传导途径的特异性抑制剂，可抑制β-catenin/环状AMP响应元件结合（CREB）蛋白的转录（IC50 = 3 uM）。了解更多

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- Seonmin Choi, .et al. Indocyanine Green-Loaded PLGA Nanoparticles Conjugated with Hyaluronic Acid Improve Target Specificity in Cervical Cancer Tumors, Yonsei Med J, 2021, Nov;62(11):1042-1051 PMID: 34672138
- Jasper C.Munro, .et al. Cardiac function and feed efficiency: increased right-heart workload in feed inefficient beef cattle, Livest Sci, 2019, 229 (2019) 159-169
- Kim JH, .et al. Small Heterodimer Partner Controls the Virus-Mediated Antiviral Immune Response by Targeting CREB-Binding Protein in the Nucleus, Cell Rep, 2019, May 14;27(7):2105-2118.e5 PMID: 31091449
- Yamaoka R, .et al. CD90 expression in human intrahepatic cholangiocarcinoma is associated with lymph node metastasis and poor prognosis, J Surg Oncol, 2018, Sep;118(4):664-674 PMID: 30196535
- Aida Y, .et al. Wnt3a promotes differentiation of human bone marrow-derived mesenchymal stem cells into cementoblast-like cells, In Vitro Cell Dev Biol Anim, 2018, Jun;54(6):468-476 PMID: 29785536
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Caffeic acid

Catalog No. A10171
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Caffeic Acid是一种羟基肉桂酸，是一种天然存在的有机化合物。了解更多

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BIX 02189

Catalog No. A10151
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MEK 抑制剂

BIX 02189是选择性双重MEK5和ERK5（或BMK1）激酶抑制剂，对于MEK5，ERK5，TGFbR1和其他紧密相关的激酶，IC50值分别为1.5、59、580和> 6200 nM。了解更多

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- Mitsunori Miyazaki, .et al. TSC2/Rheb signaling mediates ERK-dependent regulation of mTORC1 activity in C2C12 myoblasts, FEBS Open Bio, 2017, Mar; 7(3): 424-433 PMID: 28286738
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TAK-733

Catalog No. A11040
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MEK 抑制剂

TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1，AKT3，c-RAF，CamK1，CDK2及c-Met等活性。了解更多

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Baicalin

Catalog No. A10121
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HIV-1 production 抑制剂

Baicalin是已知的脯氨酰内肽酶抑制剂，并且影响GABA受体。了解更多

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- Shoichi Ozawa, .et al. Uremic serum residue decreases SN-38 sensitivity through suppression of organic anion transporter polypeptide 2B1 in LS-180 colon cancer cells, Sci Rep, 2019, 9: 15464
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CP-690550 (Tofacitinib citrate)

Catalog No. A10241
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JAK3 抑制剂

CP-690550 (Tofacitinib citrate)是口服的高选择性Janus激酶（JAK）酶抑制剂。了解更多

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- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Daptomycin

Catalog No. A10289
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DNA/RNA Synthesis 抑制剂

Daptomycin是一种脂肽抗生素，用于治疗由革兰氏阳性生物体引起的某些感染。了解更多

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- Viktoria Lazar, .et al. Antibiotic combinations reduce Staphylococcus aureus clearance, Nature, 2022, 610: 540-546 PMID: 36198788
- Shigeru Fujimura, .et al. Antimicrobial efficacy of combined clarithromycin plus daptomycin against biofilms-formed methicillin-resistant Staphylococcus aureus on titanium medical devices., J Infect Chemother., 2015, Oct;21(10):756-9 PMID: 26162777
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SNS-032 (BMS-387032)

Catalog No. A10850
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CDK 抑制剂

SNS-032（BMS-387032）是细胞周期蛋白依赖性激酶（Cdks）2、7和9的高度选择性和有效抑制剂，具有体外生长抑制作用，并具有诱导恶性B细胞凋亡的能力。了解更多

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Danoprevir (RG7227)

Catalog No. A10284
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HCV NS3/4A protease 抑制剂

Danoprevir (RG7227)是HCV NS3/4A丝氨酸蛋白酶的有效抑制剂。了解更多

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- Mahim Khan, .et al. Hesperidin identified from Citrus extracts potently inhibits HCV genotype 3a NS3 protease, BMC Complement Med Ther, 2022, Apr 2;22(1):98 PMID: 35366855
- Inês GARCEZ PALHA, .et al. An in vivo translation-reporter system for the study of protein synthesis in zebrafish embryos, Biol Open, 2018, Nov 7 PMID: 30404898
- Hui Shen, .et al. Inhibitory Effects of Caffeic Acid Phenethyl Ester Derivatives on Replication of Hepatitis C Virus, PLoS One., 2013, 8(12): e82299 PMID: 24358168
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TAE684

Catalog No. A10662
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ALK 抑制剂

TAE684是ALK的抑制剂，也是LRRK2激酶活性的有效抑制剂（针对野生型LRRK2的IC（50）为7.8nM，针对G2019S突变体的为6.1nM）。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. Bruton's tyrosine kinase potentiates ALK signaling and serves as a potential therapeutic target of neuroblastoma, Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
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PCI-24781 (Abexinostat)

Catalog No. A10700
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HDAC 抑制剂

PCI-24781 (Abexinostat)是一种广谱苯基异羟肟酸HDAC抑制剂。了解更多

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Brivanib (BMS-540215)

Catalog No. A10254
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VEGFR-2 抑制剂

Brivanib (BMS-540215)是一种VEGFR-2抑制剂，IC50为25 nM，Ki为26 nM。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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Fulvestrant (Faslodex)

Catalog No. A10410
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Aromatase 抑制剂

Fulvestrant是一种雌激素受体拮抗剂，没有激动剂作用，它通过下调和降解雌激素受体发挥作用。了解更多

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- Samy A. F. Morad, .et al. Role of P-glycoprotein inhibitors in ceramide-based therapeutics for treatment of cancer, Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Kaneyasu Nishimura, .et al. Estradiol Facilitates Functional Integration of iPSC-Derived Dopaminergic Neurons into Striatal Neuronal Circuits via Activation of Integrin α5β1, Stem Cell Reports, 2016, Apr 12; 6(4): 511-524 PMID: 26997644
- Alejandro S. Cazzulino, .et al. Improved specificity of hippocampal memory trace labeling, Hippocampus, 2016, Jun; 26(6): 752-762 PMID: 26662713
- Rie Mukai, .et al. 8-Prenylnaringenin promotes recovery from immobilization-induced disuse muscle atrophy through activation of the Akt phosphorylation pathway in mice, Am J Physiol Regul Integr Comp Physiol, 2016, Dec 1;311(6):R1022-R1031 PMID: 27629889
- Sakanashi M, .et al. Long-term treatment with san'o-shashin-to, a kampo medicine, markedly ameliorates cardiac ischemia-reperfusion injury in ovariectomized rats via the redox-dependent mechanism., Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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Doramapimod (BIRB-796)

Catalog No. A10148
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p38 MAPK 抑制剂

Doramapimod（BIRB 796）是p38 MAPK的小分子抑制剂，在调节促炎细胞因子的产生中起关键作用。了解更多

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- Ken Kobayashi, .et al. Lactose on the basolateral side of mammary epithelial cells inhibits milk production concomitantly with signal transducer and activator of transcription 5 inactivation, Cell Tissue Res, 2022, Sep;389(3):501-515 PMID: 35748981
- Junsuke Uwada, .et al. PNU-120596, a positive allosteric modulator of α7 nicotinic acetylcholine receptor, directly inhibits p38 MAPK, Biochem Pharmacol, 2020, Oct 22;182:114297 PMID: 33132165
- Perera LMB, .et al. The regulation of skin fibrosis in systemic sclerosis by extracellular ATP via P2Y2 purinergic receptor, J Invest Dermatol, 2018, Nov 4. pii: S0022-202X(18)32791-X PMID: 30404019
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XL765

Catalog No. A10997
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PI3K 抑制剂

XL765是PI3K/mTOR双激酶抑制剂，与单独抑制PI3K激酶或mTOR激酶的药物相比，它的效力更高。了解更多

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Bleomycin sulfate

Catalog No. A10152
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DNA/RNA Synthesis 抑制剂

Bleomycin Sulfate硫酸博来霉素是一种糖肽类抗生素，也是一种鳞状细胞癌(SCC)抗癌剂。了解更多

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- Mai Kanemaru, .et al. Nanoparticle-mediated local delivery of pioglitazone attenuates bleomycin-induced skin fibrosis, J Dermatol Sci, 2018, Jan;93(1):41-49 PMID: 30655107
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Dienogest

Catalog No. A10308
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Dienogest是一种口服抗孕激素，具有抗雄激素活性，因此可以改善雄激素症状。了解更多

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Tubastatin A HCl

Catalog No. A11042
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HDAC6 抑制剂

Tubastatin A HCl是一种有效的选择性HDAC6抑制剂，在无细胞试验中IC50为15 nM。它对除HDAC8（57倍）以外的所有其他同工酶（1000倍）具有选择性。了解更多

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- Isin Cakir, .et al. Histone deacetylase 6 inhibition restores leptin sensitivity and reduces obesity, Nat Metab, 2022, Jan;4(1):44-59 PMID: 35039672
- Isin Cakir, .et al. Sulforaphane reduces obesity by reversing leptin resistance, Elife, 2022, Mar 24 PMID: 35323110
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Bosutinib (SKI-606)

Catalog No. A10161
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Src 抑制剂

Bosutinib (SKI-606)是一种酪氨酸激酶抑制剂。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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MG-132

Catalog No. A11043
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Proteasome 抑制剂

MG-132是蛋白酶体（IC50 = 100 nM）和钙蛋白酶（IC50 = 1.2μM）的有效的细胞渗透抑制剂。了解更多

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- Vo Thi Anh Nguyet, .et al. Acquired resistance to severe ethanol stress-induced inhibition of proteasomal proteolysis in Saccharomyces cerevisiae, Biochim Biophys Acta Gen Subj, 2022, Sep 6;1866(12):130241 PMID: 36075516
- Jalila Chagraoui, .et al. UM171 Preserves Epigenetic Marks that Are Reduced in Ex Vivo Culture of Human HSCs via Potentiation of the CLR3-KBTBD4 Complex, Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Eunsu Yoo, .et al. Anti-proliferative activity of A. Oxyphylla and its bioactive constituent nootkatone in colorectal cancer cells, BMC Cancer, 2020, Sep 14;20(1):881 PMID: 32928152
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Chi-Hung R Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Downregulates Survivin to Induce Apoptosis in Human Colorectal Carcinoma Cells Via Suppressing WNT/β-catenin Signaling, Int J Mol Sci, 2020, Mar 5;21(5):1773 PMID: 32150830
- Ghosh S, .et al. Interactions between Viperin, Vesicle-Associated Membrane Protein A, and Hepatitis C Virus Protein NS5A Modulate Viperin Activity and NS5A Degradation, Biochemistry, 2020, Feb 18;59(6):780-789 PMID: 31977203
- Kondo H, .et al. PITHD1 is a proteasome-interacting protein essential for male fertilization, J Biol Chem, 2020, Feb 7;295(6):1658-1672 PMID: 31915251
- Ohigashi I, .et al. Trans-omics Impact of Thymoproteasome in Cortical Thymic Epithelial Cells, Cell Rep, 2019, Nov 26;29(9):2901-2916 PMID: 31775054
- Paudel DB, .et al. Expression and antiviral function of ARGONAUTE 2 in Nicotiana benthamiana plants infected with two isolates of tomato ringspot virus with varying degrees of virulence, Virology, 2018, Nov;524:127-139 PMID: 30195250
- Ohkusu-Tsukada K, .et al. The Role of Proteasome Inhibitor MG132 in 2,4-Dinitrofluorobenzene-Induced Atopic Dermatitis in NC/Nga Mice, Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Chi-Hung R. Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells, Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
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Fluorouracil (Adrucil)

Catalog No. A10042
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DNA and RNA synthesis 抑制剂

Fluorouracil (Adrucil)是一种是DNA/RNA合成抑制剂，通过不可逆地抑制胸苷酸合酶起作用。了解更多

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- T Hoshiba ,etc. Decellularized matrices as in vitro models of extracellular matrix in tumor tissues at different malignant levels: Mechanism of 5-fluorouracil resistance in colorectal tumor cells. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 2016, 1863(11), 2749-2757.
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Gemcitabine HCl (Gemzar)

Catalog No. A10423
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DNA/RNA Synthesis 抑制剂

Gemcitabine HCl (Gemzar)是一种DNA synthesis抑制剂，作用于PANC1，MIAPaCa2，BxPC3和Capan2细胞，通过在癌细胞dna复制过程中取代核酸的一个组成部分，防止肿瘤生长。了解更多

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- G. R. Iglesias, .et al. Hyperthermia-Triggered Gemcitabine Release from Polymer-Coated Magnetite Nanoparticles, Polymers, 2018, 10(3), 269
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Maraviroc (UK-427857)

Catalog No. A10556
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CCR 拮抗剂

Maraviroc (UK-427857)是CCR5受体拮抗剂类别的抗逆转录病毒药物，用于治疗HIV感染。了解更多

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- Roman V Uzhachenko, .et al. Metabolic modulation by CDK4/6 inhibitor promotes chemokine-mediated recruitment of T cells into mammary tumors, Cell Rep, 2021, Apr 6;35(1):108944 PMID: 33826903
- Karampoor S, .et al. Maraviroc attenuates the pathogenesis of experimental autoimmune encephalitis, Int Immunopharmacol, 2020, Mar;80:106138 PMID: 32007705
- Taisuke Ito, .et al. CCR5 is a novel target for the treatment of experimental alopecia areata, JCIA, 2020, 22 January
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Vicriviroc Malate

Catalog No. A10971
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CCR5 拮抗剂

Vicriviroc Malate是CCR5拮抗剂，也是HIV-1进入靶细胞的有效抑制剂，对HIV分离株的平均IC50 = 0.46 nM，IC50 = 1?10 nM（n = 52）。了解更多

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- Tomohiro Nabekura, .et al. Effects of Antiviral Drugs on Organic Anion Transport in Human Placental BeWo Cells, Antimicrob Agents Chemother, 2015, Dec; 59(12): 7666-7670 PMID: 26416870
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PHA-793887

Catalog No. A10716
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CDK 抑制剂

PHA-793887是一种新型有效的CDK2，CDK5和CDK7抑制剂，IC50分别为8 nM，5 nM 和10 nM，作用于CDK2，5，和7比作用于CDK1，4，和9选择性高6倍以上。可在低浓度下靶向多种细胞周期蛋白依赖性激酶，并具有针对多种癌细胞的高活性。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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AT7519

Catalog No. A10093
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CDK 抑制剂

AT7519是多种细胞周期蛋白依赖性激酶（CDK）的抑制剂，可导致细胞周期停滞，诱导细胞凋亡和抑制肿瘤细胞增殖。作用于CDK1，2，4，6和9时，IC50为10-210 nM，对CDK3作用效果稍弱，对CDK7几乎没有抑制活性。了解更多

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BS-181

Catalog No. A10163
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CDK 抑制剂

BS-181 是作为CDK7抑制剂的潜在抗肿瘤剂。了解更多

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Flavopiridol HCl

Catalog No. A11045
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CDK 抑制剂

Flavopiridol HCl是细胞周期蛋白依赖性激酶的抑制剂。（-）-顺式形式诱导特定肿瘤细胞的凋亡。了解更多

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CHIR-124

Catalog No. A11046
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CHK 抑制剂

CHIR-124是一种新型有效的Chk1抑制剂（Chk1和Chk2的IC50：分别为0.32 nM和697 nM）。了解更多

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Chrysophanic acid (Chrysophanol)

Catalog No. A10210
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EGFR 抑制剂

Chrysophanic acid (Chrysophanol)是通过抑制EGFR/mTOR通路来阻止结肠癌细胞的增殖。了解更多

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Icariin

Catalog No. A10464
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PDE5 抑制剂

Icariin对抑制PDE5A1、PDE5A2和PDE5A3的所有三种PDE5A亚型均有抑制作用，IC50值分别为1.0、0.75和1.1 μM。了解更多

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LY2940680 (Taladegib)

Catalog No. A11048
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SMO 拮抗剂

LY2940680 (Taladegib)已显示可影响由Hedgehog（Hh）蛋白引发的癌细胞信号通路。了解更多

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OSU-03012

Catalog No. A10681
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PDK-1 抑制剂

OSU-03012 (AR-12)是一种有效的重组PDK-1(phosphoinositide-dependent kinase 1)抑制剂。了解更多

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URB597

Catalog No. A11049
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FAAH 抑制剂

URB597是脂肪酸酰胺水解酶（FAAH）的相对选择性抑制剂。了解更多

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- Lakhan S Khara, .et al. Inhibiting the endocannabinoid degrading enzymes FAAH and MAGL during zebrafish embryogenesis alters sensorimotor function, J Exp Biol, 2022, May 1;225(9):jeb244146 PMID: 35438163
- Md Shah Sufian, .et al. Early suppression of the endocannabinoid degrading enzymes FAAH and MAGL alters locomotor development in zebrafish, J Exp Biol, 2021, 21 JUNE
- Toshihiko Tsutsumi, .et al. Identification of human glycerophosphodiesterase 3 as an ecto phospholipase C that converts the G protein-coupled receptor 55 agonist lysophosphatidylinositol to bioactive monoacylglycerols in cultured mammalian cells, Biochim Biophys Acta Mol Cell Biol Lipids, 2020, Sep;1865(9):158761 PMID: 32629025
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Decitabine

Catalog No. A10292
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DNA Methyltransferase 抑制剂

Decitabine是一种次甲基化剂，它通过抑制DNA甲基转移酶来使DNA次甲基化。了解更多

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- Borbala Szabo, .et al. Aspirin mediates its antitumoral effect through inhibiting PTTG1 in pituitary adenoma, J Clin Endocrinol Metab, 2022, Sep 5;dgac496 PMID: 36059148
- Sangni Qian, .et al. Hypermethylation of tumor suppressor lncRNA MEF2C-AS1 frequently happened in patients at all stages of colorectal carcinogenesis, Clin Epigenetics, 2022, Sep 5;14(1):111 PMID: 36064442
- Borb??la Szab??, .et al. Demethylation status of somatic DNA extracted from pituitary neuroendocrine tumors indicates proliferative behavior, J Clin Endocrinol Metab, 2020, Jun 1;105(6):dgaa156 PMID: 32232382
- Bracha Shraibman, .et al. Human Leukocyte Antigen (HLA) Peptides Derived from Tumor Antigens Induced by Inhibition of DNA Methylation for Development of Drug-facilitated Immunotherapy, Mol Cell Proteomics, 2016, Sep; 15(9): 3058-3070 PMID: 27412690
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SB 202190

Catalog No. A10823
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p38 MAPK 抑制剂

SB202190是p38 MAP激酶的高度选择性，有效和细胞渗透性抑制剂。了解更多

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- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Tsai CC, .et al. Protease-activated receptor 2 induces migration and promotes Slug-mediated epithelial-mesenchymal transition in lung adenocarcinoma cells, Biochim Biophys Acta Mol Cell Res, 2018, Oct 13. pii: S0167-4889(18)30452-X PMID: 30321617
- Jia-Shiuan Tsai, .et al. Cadmium Activates Multiple Signaling Pathways That Coordinately Stimulate Akt Activity to Enhance c-Myc mRNA Stability, PLoS One, 2016, 11(1): e0147011 PMID: 26751215
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Raltegravir (MK-0518)

Catalog No. A10775
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HIV-1 integrase 抑制剂

Raltegravir (MK-0518)靶向整合酶，这是一种HIV酶，可将病毒遗传物质整合到人类染色体中，这是HIV发病机理中的关键步骤。了解更多

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- Michal S Barski, .et al. Structural basis for the inhibition of HTLV-1 integration inferred from cryo-EM deltaretroviral intasome structures, Nat Commun, 2021, Aug 17;12(1):4996 PMID: 34404793
- Lea El Khoury, .et al. Spectrometric and computational studies of the binding of HIV-1 integrase inhibitors to viral DNA extremities, PeerJ Preprints, 2019, 7:e27833v1
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Silibinin (Silybin)

Catalog No. A10842
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Silibinin (Silybin)是Silymarin化合物的主要活性成分。了解更多

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Geldanamycin

Catalog No. A11025
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Hsp90 抑制剂

Geldanamycin与Hsp90的ATP位点（Kd = 1.2μM）结合并抑制其分子伴侣活性。了解更多

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- Michael Heider, .et al. The IMiD target CRBN determines HSP90 activity toward transmembrane proteins essential in multiple myeloma, Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422

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