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OTSSP167

Catalog No. A12851
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MELK 抑制剂

OTSSP167是一种高效的MELK（母体亮氨酸拉链激酶）抑制剂，IC50为0.41 nM。了解更多

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- Yubao Wang ,etc. Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival. Proc Natl Acad Sci USA. 2016 Aug 30; 113(35): 9810–9815.
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Ro 61-8048

Catalog No. A12833
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Hydroxylase 抑制剂

Ro 61-8048是有效的竞争性犬尿氨酸3-羟化酶抑制剂（Ki = 4.8 nM，IC50 = 37 nM）。了解更多

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IKK-16

Catalog No. A12836
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IKK 抑制剂

IKK 16是针对IKK-2，IKK复合物和IKK-1的选择性IκB激酶（IKK）抑制剂，IC50分别为40 nM，70 nM和200 nM。了解更多

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- 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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IMD 0354

Catalog No. A12837
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IKK 抑制剂

IMD 0354是IκB激酶-β（IKKβ）抑制剂，可阻断NF-κB核易位。了解更多

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- Anton Lennikov, .et al. Selective IKK2 inhibitor IMD0354 disrupts NF-κB signaling to suppress corneal inflammation and angiogenesis, Angiogenesis, 2018, 21(2): 267-285 PMID: 29332242
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NQDI 1

Catalog No. A12838
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ASK1 抑制剂

NQDI 1是细胞凋亡信号调节激酶1（ASK1，MAP3K5）的选择性抑制剂（IC50 = 3 μM，Ki = 500 nM）。了解更多

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AZD-2461

Catalog No. A12393
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PARP 抑制剂

AZD2461是新型有效的PARP抑制剂，对P-糖蛋白的亲和力较低。了解更多

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XL019

Catalog No. A12394
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JAK2 抑制剂

XL019是janus相关激酶2 (JAK-2)的生物可利用抑制剂，具有潜在的抗肿瘤活性。了解更多

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XL388

Catalog No. A12395
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mTOR 抑制剂

XL388是哺乳动物雷帕霉素靶标(mTOR)的一类新型高效、选择性、ATP竞争性生物可利用抑制剂。了解更多

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AZD3514

Catalog No. A12396
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AR 抑制剂 downregulator

AZD3514是一种有效的雄激素受体下调剂，具有潜在的抗癌活性。了解更多

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Epirubicin

Catalog No. A12409
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Topoisomerase 抑制剂

Epirubicin是一种细胞可渗透的抗肿瘤抗生素。阿霉素的立体异构体，其心脏毒性降低。表柔比星的抗肿瘤作用是通过靶向和抑制Topo II（拓扑异构酶II）来介导的。了解更多

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- Xiu-wu Pan, .et al. Icaritin acts synergistically with epirubicin to suppress bladder cancer growth through inhibition of autophagy, Oncol Rep, 2016, Jan;35(1):334-42 PMID: 26496799
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Reparixin

Catalog No. A12383
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CXCL8/CXCR1/2 抑制剂

Reparixin是两种CXCL8受体CXCR1/2的有效抑制剂，它抑制CXCR2介导的细胞迁移（IC50 = 100 nM），而它强烈地阻断CXCR1介导的趋化性（IC50 = 1 nM）。了解更多

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- Naour AL, .et al. Tumor cells educate mesenchymal stromal cells to release chemoprotective and immunomodulatory factors, J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. N-acetyl cysteine improves the effects of corticosteroids in a mouse model of chlorine-induced acute lung injury, Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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MKT 077

Catalog No. A12388
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HSP70 抑制剂

MKT 077的p53结合位点，并使p53易位至细胞核。选择性细胞毒性；导致培养物中癌细胞生长停滞。也抑制端粒酶活性和交联f-肌动蛋白。了解更多

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(S)-(+)-Flurbiprofen

Catalog No. A12434
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COX 抑制剂

(S)-(+)-Flurbiprofen是一种非选择性的Cox-1和Cox-2抑制剂。了解更多

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- Xing Jin, .et al. Enantioselective analysis of ketoprofen in human saliva by liquid chromatography/tandem mass spectrometry with chiral derivatization, Microchemical Journal, 2018, 143: 280-285
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Gatifloxacin

Catalog No. A10419
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DNA gyrase/topoisomerase IV 抑制剂

Gatifloxacin是一种氟喹诺酮类抗生素，可抑制细菌dna回旋酶(IC50 = 0.109 ng/ml)和拓扑异构酶iv(IC50 = 13.8 ng/ml)。了解更多

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Omeprazole

Catalog No. A10672
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ATPase 抑制剂

Omeprazole是一种可透过细胞的选择性质子泵抑制剂。了解更多

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Ofloxacin (DL8280)

Catalog No. A10666
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Topoisomerase 抑制剂

Ofloxacin (DL8280)是一种合成的广谱抗菌剂。了解更多

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LY2835219 (abemaciclib)

Catalog No. A12989
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CDK4/6 抑制剂

LY2835219 (abemaciclib)是一种细胞周期蛋白依赖性激酶（CDK）抑制剂，靶向CDK4（cyclin D1）和CDK6（cyclin D3）细胞周期途径，具有潜在的抗肿瘤活性。了解更多

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- Yoshinori Tanaka, .et al. Abemaciclib and Vacuolin-1 induce vacuole-like autolysosome formation - A new tool to study autophagosome-lysosome fusion, Biochem Biophys Res Commun, 2022, Jul 23;614:191-97 PMID: 35598430
- Sumire Suzuki, .et al. Lysosome-targeted drug combination induces multiple organelle dysfunctions and non?canonical death in pancreatic cancer cells, Oncol Rep, 2022, Feb;47(2):40 PMID: 34958115
- Kana Nakatani, .et al. Inhibition of CDK4/6 and autophagy synergistically induces apoptosis in t(8;21) acute myeloid leukemia cells, Int J Hematol, 2020, Oct 17 PMID: 33068248
- Ryohei Ogata, .et al. Resistance to cyclin-dependent kinase (CDK) 4/6 inhibitors confers cross-resistance to other CDK inhibitors but not to chemotherapeutic agents in breast cancer cells, Breast Cancer, 2020, Aug 28 PMID: 32860163
- Elaheh Seyed Abutorabi, .et al. Abemaciclib (CDK4/6 Inhibitor) Blockade Induces Cytotoxicity in Human Anaplastic Thyroid Carcinoma Cells, Rep Biochem Mol Biol, 2020, Jan; 8(4): 438-445 PMID: 32582803
- Hidemasa Matsuo, .et al. Recurrent CCND3 mutations in MLL-rearranged acute myeloid leukemia, Blood Adv, 2018, Nov 13; 2(21): 2879-2889 PMID: 30381403
- Iriyama N, .et al. The cyclin-dependent kinase 4/6 inhibitor, abemaciclib, exerts dose-dependent cytostatic and cytocidal effects and induces autophagy in multiple myeloma cells, Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692
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IWP-2

Catalog No. A12707
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Wnt 抑制剂

IWP-2是Porcn功能的灭活剂和Wnt生成的抑制剂，无细胞试验中IC50为27 nM,并阻止β-catenin的积累。Wnt/b-catenin途径维持使干细胞保持多能性的转录程序。了解更多

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Dynasore

Catalog No. A12726
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Dynamin 抑制剂

dynasore是一种非竞争性的dynamin 1，dynamin 2和线粒体dynamin（Drp1）GTPase活性抑制剂。了解更多

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- KOLAC UK, .et al. Chemical Inhibition of Mitochondrial Fission Improves Mitochondrial Function and Subdues Hyperglycemia Induced Stress in Placental Trophoblast Cells, Research Square, 2022, 03 Jun
- Tsukamoto H, .et al. Lipopolysaccharide (LPS)-binding protein stimulates CD14-dependent Toll-like receptor 4 internalization and LPS-induced TBK1-IKKε-IRF3 axis activation, J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187
- Shigetoshi Yokoyama, .et al. A novel pathway of LPS uptake through syndecan-1 leading to pyroptotic cell death, eLife, 2018, 7: e37854 PMID: 30526845
- Naoko Fujii, .et al. Hypotonic Stress-induced Down-regulation of Claudin-1 and -2 Mediated by Dephosphorylation and Clathrin-dependent Endocytosis in Renal Tubular Epithelial Cells, J Biol Chem, 2016, Nov 18; 291(47): 24787-24799 PMID: 27733684
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XL-228

Catalog No. A13069
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IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂

XL228是靶向IGF1R，AURORA激酶，FGFR1-3，ABL和SRC家族激酶的蛋白激酶抑制剂。XL228是一种Aurora A抑制剂（IC50，f3 nmol/L），对ABL1（Ki，5 nmol/L）以及BCR-ABL1 T315I（Ki，1.4 nmol/L）激酶显示出有效的生化活性。了解更多

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NSC 405020

Catalog No. A13072
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MT1-MMP 抑制剂

NSC-405020是一种膜1型基质金属蛋白酶（MT1-MMP）抑制剂（IC50> 100μmol/ L）。了解更多

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- Kittaka M, .et al. Cherubism Mice Also Deficient in c-Fos Exhibit Inflammatory Bone Destruction Executed by Macrophages That Express MMP14 Despite the Absence of TRAP+ Osteoclasts, J Bone Miner Res, 2018, Jan;33(1):167-181 PMID: 28914985
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Tolrestat

Catalog No. A13083
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aldose reductase 抑制剂

Tolrestat是醛糖还原酶抑制剂[1],被批准用于控制某些糖尿病并发症。了解更多

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PR-619

Catalog No. A13190
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DUB 抑制剂

PR-619是一种细胞可渗透、可逆、广谱的去双基化酶抑制剂。了解更多

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- Anurag Rathore, .et al. CRISPR-based gene knockout screens reveal deubiquitinases involved in HIV-1 latency in two Jurkat cell models, Sci Rep, 2020, 10: 5350 PMID: 32210344
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CGK 733

Catalog No. A13191
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ATM/ATR 抑制剂

CGK733是ATR和ATM激酶的选择性抑制剂。在过早衰老的乳腺癌细胞中诱导细胞死亡。了解更多

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UNC0646

Catalog No. A13194
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G9a/GLP HMTase 抑制剂

UNC0646是一种有效且选择性的同源蛋白赖氨酸甲基转移酶G9a和GLP抑制剂（G9a和GLP的IC50值分别为6 nM和15 nM）。了解更多

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INCB024360 analog

Catalog No. A13004
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IDO1 抑制剂

INCB024360 analog是一种羟胺和吲哚胺2,3-二加氧酶（IDO1）抑制剂，具有潜在的免疫调节和抗肿瘤活性。了解更多

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AGI-5198 (IDH-C35)

Catalog No. A12902
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IDH1 抑制剂

AGI-5198 (IDH-C35)是一种非常有效的选择性IDH1突变抑制剂，具有潜在的抗癌活性。了解更多

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GSK343

Catalog No. A13114
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EZH2 抑制剂

GSK343是有效的组蛋白H3-赖氨酸27（H3K27）甲基转移酶EZH2抑制剂（IC = 4 nM）。对除EZH1以外的其他HMT的选择性是1000倍（选择性是60倍）。GSK343抑制HCC1806细胞中的H3K27甲基化，IC小于200nM（通过免疫荧光测量）。了解更多

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- Nie L, .et al. CDK2-mediated site-specific phosphorylation of EZH2 drives and maintains triple-negative breast cancer, Nat Commun, 2019, Nov 8;10(1):5114 PMID: 31704972
- 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
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Bromosporine

Catalog No. A13163
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bromodomain 抑制剂

Bromosporine是一种针对溴结构域的广谱抑制剂，对于BRD2，BRD4，BRD9和CECR2的IC50分别为0.41μM，0.29μM，0.122μM和0.017μM。了解更多

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UNC-1999

Catalog No. A13166
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EZH2/EZH1 抑制剂

UNC-1999是生物可利用抑制剂，对野生型和突变型ezh2以及ezh1具有高体外效力，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。了解更多

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- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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GLPG0634

Catalog No. A13162
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JAK1 抑制剂

GLPG0634是一种口服的JAK1(Janus激酶1)选择性抑制剂，对 JAK1/JAK2/JAK3的IC50值为50-200 nM。用于治疗类风湿性关节炎和潜在的其他炎性疾病。了解更多

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- Keisuke Nishimura, .et al. Tofacitinib facilitates the expansion of myeloid-derived suppressor cells and ameliorates arthritis in SKG mice., Arthritis Rheumatol., 2015, Apr;67(4):893-902 PMID: 25545152
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AVL-292

Catalog No. A13202
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Btk 抑制剂

AVL-292是一种高选择性共价Btk抑制剂。了解更多

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AZD1208

Catalog No. A13203
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pan-Pim kinase 抑制剂

AZD1208是PIM激酶的小分子抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Remy J, .et al. Inhibition of PIM1 blocks the autophagic flux to sensitize glioblastoma cells to ABT-737-induced apoptosis, Biochim Biophys Acta Mol Cell Res, 2019, Feb;1866(2):175-189 PMID: 30389373
- Andrea L. Casillas, .et al. Hypoxia-inducible PIM kinase expression promotes resistance to anti-angiogenic agents, Clin Cancer Res, 2018, Jan 1; 24(1): 169-180 PMID: 29084916
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
- Sathish K.R. Padi, .et al. Targeting the PIM protein kinases for the treatment of a T-cell acute lymphoblastic leukemia subset, Oncotarget, 2017, May 2; 8(18): 30199-30216 PMID: 28415816
- Lim R, .et al. Inhibition of PIM1 kinase attenuates inflammation-induced pro-labour mediators in human foetal membranes in vitro, Mol Hum Reprod, 2017, Jun 1;23(6):428-440 PMID: 28333279
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BMS-833923 (XL-139)

Catalog No. A13204
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Smoothened 抑制剂

BMS-833923 (XL-139)是一种生物可利用的小分子SMO(平滑)抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Valérian Pasche, .et al. Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni, Parasit Vectors, 2018, 11: 298 PMID: 29764454
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GENZ-644282

Catalog No. A13206
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topoisomerase 1 抑制剂

GENZ-644282是拓扑异构酶I的非喜树碱抑制剂，具有潜在的抗肿瘤活性。了解更多

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Nocodazole

Catalog No. A13219
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microtubule 抑制剂

Nocodazole是微管抑制剂；抑制有丝分裂。也抑制自噬体-溶酶体融合。了解更多

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KU 0060648

Catalog No. A13224
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DNA-PK 抑制剂

KU0060648是一种有效且选择性的DNA依赖性蛋白激酶（DNA-PK）抑制剂（IC50 = 8.6 nM）；对DNA-PK的选择性是其他PIKK的20-1000倍，并且有60种激酶。KU-0060648可提高HDR效率并衰减NHEJ频率。了解更多

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ABT-199 (Venetoclax)

Catalog No. A12500
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Bcl-2 抑制剂

ABT-199 (Venetoclax) 是一种所谓的BH3类似药物，旨在阻断Bcl 2蛋白的功能。了解更多

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- Ashlyn Parkhurst, .et al. Dual mTORC1/2 inhibition compromises cell defenses against exogenous stress potentiating Obatoclax-induced cytotoxicity in atypical teratoid/rhabdoid tumors, Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Anna L Koessinger, .et al. Increased apoptotic sensitivity of glioblastoma enables therapeutic targeting by BH3-mimetics, Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. Apoptotic stress-induced FGF signalling promotes non-cell autonomous resistance to cell death, Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Chauhan D, .et al. BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages, Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Martin Grundy, .et al. Predicting effective pro-apoptotic anti-leukaemic drug combinations using co-operative dynamic BH3 profiling, PLoS One, 2018, 13(1): e0190682 PMID: 29298347
- Joanne Dai, .et al. Intracellular BH3 profiling reveals shifts in anti-apoptotic dependency in B-cell maturation and activation, J Immunol, 2018, 200 (5) 1727-1736 PMID: 29358277
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SANT-1

Catalog No. A13095
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Sonic hedgehog 抑制剂

SANT-1是有效的细胞渗透性Sonic刺猬（Shh）信号传导抑制剂；平滑活性的高亲和力拮抗剂（KD = 1.2 nM）。以20 nM的IC50抑制平滑的激动剂作用（在Shh-LIGHT2细胞中）。了解更多

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Tipiracil

Catalog No. A13098
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Thymidine phosphorylase 抑制剂

Tipiracil，也称为TPI，是胸苷磷酸化酶抑制剂(TPI)。了解更多

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R1530

Catalog No. A13111
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Chk2, KDR, FGFR, Aurora A & Cdk2 抑制剂

R1530是吡唑并苯并二氮杂小分子，具有潜在的抗血管生成和抗肿瘤活性。R1530也是一种有丝分裂-血管生成抑制剂(MAI),可抑制多种参与血管生成的受体酪氨酸激酶，如血管内皮生长因子受体(VEGFR)-1，-2，-3，血小板衍生生长因子受体(PDGFR)βFMS样酪氨酸激酶(Flt)-3和成纤维细胞生长因子受体(FGFR) -1，-2。了解更多

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NS-398

Catalog No. A13116
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COX-2 抑制剂?

NS-398是具有镇痛和解热作用的非甾体类抗炎药，可选择性抑制前列腺素G / H合酶2 /环氧合酶2（COX-2）活性，IC50为3.8μM，对COX无影响了解更多

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PD173955

Catalog No. A13120
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Bcr-Abl 抑制剂

PD-173955是src酪氨酸激酶抑制剂。PD173955抑制Bcr-Abl依赖的细胞生长。PD173955显示G（1）中的细胞周期停滞。PD173955在Bcr-Abl的激酶抑制测定中的IC（50）为1-2 nM，在细胞生长测定中，其抑制Bcr-Abl依赖性底物酪氨酸磷酸化。 PD173955抑制试剂盒配体依赖性c-kit自磷酸化（IC（50）=约25 nM）和试剂盒配体依赖性M07e细胞增殖（IC（50）= 40 nM），但对白介素3依赖性（IC （50）= 250 nM）或粒细胞巨噬细胞集落刺激因子（IC（50）= 1 microM）依赖性细胞生长。了解更多

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1-NA-PP1

Catalog No. A13232
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Src Kinase 抑制剂

1-NA-PP1是v-Src和c-Fyn以及c-Abl的选择性抑制剂。了解更多

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CNX-774

Catalog No. A13233
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BTK 抑制剂

CNX-774是有效的Btk抑制剂（IC50 <1 nM）。了解更多

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GNF-5

Catalog No. A13237
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Bcr-Abl 抑制剂

GNF-5是BCR-ABL的选择性变构抑制剂。了解更多

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LDK-378

Catalog No. A13238
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ALK 抑制剂

LDK-378是ALK(间变性淋巴瘤激酶)的高度选择性、生物利用度和AT竞争性小分子抑制剂，ALK是一种受体酪氨酸激酶，被认为是肺癌的重要药物靶点。了解更多

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Beta-Lapachone

Catalog No. A13059
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DNA topoisomerase II 抑制剂

Beta-Lapachone是一种选择性的DNA拓扑异构酶I抑制剂，对DNA拓扑异构酶II或连接酶没有抑制活性。了解更多

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- Xiaoling Li, .et al. Nanozyme-Augmented Tumor Catalytic Therapy by Self-Supplied H2O2 Generation, ACS Appl. Bio Mater, 2020, 3, 3, 1769-1778
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Thiamet G

Catalog No. A12895
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O-GlcNAcase 抑制剂

Thiamet G是一种有效的，选择性的O-GlcNAcase抑制剂，Kiof为21 nM，相对于人类溶酶体-己糖胺酶具有37,000倍的选择性。了解更多

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- Zhu WZ, .et al. O-GlcNAc Transferase Promotes Compensated Cardiac Function and Protein Kinase A O-GlcNAcylation During Early and Established Pathological Hypertrophy From Pressure Overload, J Am Heart Assoc, 2019, Jun 4;8(11):e011260 PMID: 31131693
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AZD2858

Catalog No. A13060
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GSK-3β 抑制剂

AZD2858是一种选择性GSK-3抑制剂，IC50为68 nM，激活Wnt信号，增加大鼠的骨量。了解更多

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