“MK-2206 dihydrochloride”的搜索结果
-
Cell adhesion 抑制剂
K-7174 dihydrochloride是一种新型的细胞粘附抑制剂;抑制由IL-1beta或TNF-alpha诱导的血管细胞粘附分子1(VCAM-1)的表达。
了解更多
-
polyamine synthesis 抑制剂
Sardomozide dihydrochloride是第二代多胺合成抑制剂,可抑制多胺生物合成酶S-腺苷甲硫氨酸脱羧酶(SAMDC)的活性。
了解更多
-
PKs 抑制剂
HA-100 dihydrochloride是具有添加的哌嗪基磺酰基的异喹啉化合物,可充当蛋白激酶(PKs)的抑制剂,包括PKA,PKC和PKG(IC50分别为8、12和4 μM)。
了解更多
-
DAT and SLC6A2 抑制剂
GBR-12935 dihydrochloride是一种有效的选择性多巴胺再摄取抑制剂。
了解更多
-
Thymidylate synthase 抑制剂
Nolatrexed Dihydrochloride是一种抗叶酸胸苷酸合酶抑制剂。
了解更多
-
DPP-4 抑制剂
NVP DPP 728 dihydrochloride是一种有效的活性二肽基肽酶(DPP)-IV抑制剂,Ki和IC50值分别为11 nM和14 nM。
了解更多
-
Src 抑制剂
Tirbanibulin dihydrochloride是首个靶向Src肽底物位点的临床Src抑制剂(拟肽类),在癌细胞系中GI50为9-60 nM。
了解更多
-
dopamine re-uptake 抑制剂
Vanoxerine 2HCl (GBR-12909)是哌嗪衍生物,是一种有效的、选择性的多巴胺摄取(dopamine uptake)抑制剂。
了解更多
-
PKA 抑制剂
H 89 dihydrochloride是一种可渗透细胞的,选择性的,可逆的,具有ATP竞争性的有效蛋白激酶抑制剂。
了解更多
- Guo Q, .et al. Antineuropathic pain actions of Wu-tou decoction resulted from the increase of neurotrophic factor and decrease of CCR5 expression in primary rat glial cells, Biomed Pharmacother, 2020, Mar;123:109812 PMID: 31945696
- Y Kaibori, .et al. EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity, the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
-
dopamine uptake 抑制剂
GBR 12783 dihydrochloride是一种非常有效的选择性多巴胺摄取抑制剂(抑制大鼠纹状体突触体中[3H]-多巴胺摄取的IC50为1.8 nM)。
了解更多
-
Syk 抑制剂
BAY 61-3606 dihydrochloride是一种有效的Syk激酶抑制剂(Ki = 7.5 nM)。
了解更多
-
PTPMT1 抑制剂
Alexidine dihydrochloride是烷基双(双胍)防腐剂,已用于漱口水中以消除形成斑块的微生物。
了解更多
-
Urokinase 抑制剂
GGACK Dihydrochloride是尿激酶(uPA(ICkin <1 ?M),凝血因子VIIa,凝血因子IXa,凝血因子Xa和胰蛋白酶的有效且不可逆的抑制剂。
了解更多
-
p38 MAPK 抑制剂
DBM 1285 dihydrochloride是p38 MAPK抑制剂。在巨噬细胞和体内抑制p38磷酸化和LPS诱导的TNF-α产生。
了解更多
-
MAO-A inhibitor
Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.
了解更多
-
ROCK inhibitor
Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
了解更多
-
ROCK 抑制剂
SR 3677 dihydrochloride是一种有效的选择性Rho激酶抑制剂(ROCK-II和ROCK-I的IC50值分别为3和56 nM)。
了解更多
-
INOS 抑制剂
1400W Dihydrochloride是一种缓慢,紧密结合,有效和高度选择性的诱导型一氧化氮合酶抑制剂(Kd = 7 nM)。对nNOS和eNOS具有选择性(Ki值分别为2和50μM)。细胞可渗透并在体内具有活性。
了解更多
-
ROCK 抑制剂
HA-1077 dihydrochloride通过充当细胞内Ca2+拮抗剂来抑制血管平滑肌收缩。
了解更多
-
Akt 抑制剂
AT7867 dihydrochloride是一种有效的ATP竞争性Akt1/2/3和p70S6K/PKA抑制剂,IC50分别为32 nM/17 nM/47 nM和85 nM/20 nM,在AGC激酶家族之外几乎没有活性。
了解更多
-
p38 MAPK 抑制剂
SKF 86002 Dihydrochloride是p38 MAP激酶的抑制剂(IC50 = 0.1-1 uM)。有效抑制人单核细胞中LPS诱导的IL-1和TNF-α的产生(IC50 = 1 uM)。
了解更多
-
Raf 抑制剂
ML 786 dihydrochloride是一种有效的Raf激酶抑制剂(B-RafV600E,C-Raf和野生型B-Raf的IC50值分别为2.1、2.5和4.2 nM)。
了解更多
-
DPP-II 抑制剂
UAMC 00039 dihydrochloride是二肽基肽酶II(DPP-II)的有效抑制剂(IC50 = 0.48 nM)。展示了DPP-II对DPP-9,DPP-8和DPP-IV的选择性(IC50值分别为78.6、142和165μM)。
了解更多
-
tubulin polymerisation inhibitor
Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulin polymerisation inhibitor with IC50 of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo.
了解更多
-
DDR1 receptor tyrosine kinase inhibitor
DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM).
了解更多
-
Raf kinase inhibitor
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
了解更多
-
SHIP1 抑制剂
3AC是SHIP1多磷酸酶对PIP3的活性的细胞渗透性选择性抑制剂(IC50 = 10μM),但对SHIP2或PIP3的PTEN活性没有影响。
了解更多
-
ROCK 抑制剂
H-1152 dihydrochloride是一种异喹啉磺酰胺衍生物,是Rho激酶的一种更特异,更强且可透过膜的抑制剂,Ki值为1.6 nM,但对其他丝氨酸/苏氨酸激酶的抑制作用较弱。
了解更多
-
MET 抑制剂
LY2801653 dihydrochloride是一种有效的,口服可生物利用的c-MET激酶小分子抑制剂(Ki = 2 nM)。
了解更多
-
NOS inhibitor
L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor.
了解更多
-
S1P inhibitor
PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.
了解更多
-
ULK1/ULK2 inhibitor
MRT68921 dihydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
了解更多
-
ACAT-1 inhibitor
K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45??0.06 μM.
了解更多
-
LSD1 inhibitor
GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
了解更多
-
PARP inhibitor
Veliparib dihydrochloride is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
了解更多
-
ALK 抑制剂
LDK378 (Ceritinib) dihydrochloride是有效的抗ALK抑制剂,IC50为0.2 nM,对IGF-1R和InsR的选择性分别为40倍和35倍。
了解更多
-
CYP450 dependent inhibitor
Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).
了解更多
-
p38α MAPK inhibitor
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
了解更多
-
serotonin reuptake 抑制剂
Azaphen dihydrochloride monohydrate是5-羟色胺再摄取的有效抑制剂。
了解更多
-
EGFR inhibitor
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
了解更多
-
PDE-5 inhibitor
Mirodenafil dihydrochloride (SK3530 dihydrochloride) is a phosphodiesterase type 5 (PDE-5) inhibitor developed for the treatment of erectile dysfunction.
了解更多
-
JAK2 inhibitor
NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
了解更多
-
CDK4/CDK6 inhibitor
Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
了解更多
-
ACDase inhibitor
LCL521 dihydrochloride (1,3DMG-B13 dihydrochloride) is an acid ceramidase (ACDase) inhibitor.
了解更多
-
PRMT inhibitor
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)).
了解更多
-
CHK1 inhibitor
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
了解更多
-
pan-Akt inhibitor
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA.
了解更多
-
AKT 抑制剂
MK-2206 2HCl是Akt1/2/3的高选择性抑制剂,IC50分别为8 nM/12 nM/65 nM。
了解更多
- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Yusuke Murase, .et al. Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells, Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Ali Nasrollahzadeh, .et al. Anti-proliferative activity of disulfiram through regulation of the AKT-FOXO axis: A proteomic study of molecular targets, Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Rona Aviram, .et al. Ultradian rhythms of AKT phosphorylation and gene expression emerge in the absence of the circadian clock components Per1 and Per2, PLoS Biol, 2021, Dec 30;19(12):e3001492 PMID: 34968386
- Cristina Rosell??-Busquets, .et al. Nystatin Regulates Axonal Extension and Regeneration by Modifying the Levels of Nitric Oxide, Front Mol Neurosci, 2020, 13: 56 PMID: 32317932
- Dai-Chi Liu, .et al. Chronic Activation of Gp1 mGluRs Leads to Distinct Refinement of Neural Network Activity Through Non-Canonical p53 and Akt Signaling, eNeuro, 2020, Mar 27;7(2):ENEURO.0438-19.2020 PMID: 32161037
- Nishihama K, .et al. Anti-apoptotic activity of human matrix metalloproteinase-2 attenuates diabetes mellitus, Metabolism, 2018, May;82:88-99 PMID: 29366755
- J Wei, .et al. Profiling the surface proteome identifies actionable biology for TSC1 mutant cells beyond mTORC1 signaling, bioRxiv, 2018, 2018
- Joo Sang Lee, .et al. Harnessing synthetic lethality to predict the response to cancer treatment, Nat Commun, 2018, 9: 2546 PMID: 29959327
- Wan-Ting Hu, .et al. The O-glycosylating enzyme GALNT2 suppresses the malignancy of gastric adenocarcinoma by reducing EGFR activities, Am J Cancer Res, 2018, 8(9): 1739-1751 PMID: 30323967
- Angela M. Gocher, .et al. Akt activation by Ca2+/calmodulin-dependent protein kinase kinase 2 (CaMKK2) in ovarian cancer cells, J Biol Chem, 2017, Aug 25; 292(34): 14188-14204 PMID: 28634229
- Kusuyama J, .et al. Constitutive activation of p46JNK2 is indispensable for C/EBPδ induction in the initial stage of adipogenic differentiation, Biochem J, 2017, Oct 5;474(20):3421-3437 PMID: 28887384
- Pi-Lin Sung, .et al. Periostin in tumor microenvironment is associated with poor prognosis and platinum resistance in epithelial ovarian carcinoma, Oncotarget, 2016, Jan 26; 7(4): 4036-4047 PMID: 26716408
- Mikaël M. Martino, .et al. Inhibition of IL-1R1/MyD88 signalling promotes mesenchymal stem cell-driven tissue regeneration, Nat Commun, 2016, 7: 11051 PMID: 27001940
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
- Jewett KA, .et al. The tumor suppressor p53 guides GluA1 homeostasis through Nedd4-2 during chronic elevation of neuronal activity., J Neurochem., 2015, Oct;135(2):226-33 PMID: 26250624