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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEKK (MAP3K)-GS-444217
GS-444217

Chemical Structure : GS-444217

CAS No.: 1262041-49-5

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GS-444217 (GS444217)

货号: PC-35427Not For Human Use, Lab Use Only.

GS-444217 (GS444217) is a potent, selective, ATP-competitive, orally available inhibitor of ASK1 with Kd/IC50 of 4.1/2.87 nM.

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10 mg ￥1380 In stock
25 mg ￥2380 In stock
50 mg ￥3980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GS-444217 (GS444217) is a potent, selective, ATP-competitive, orally available inhibitor of ASK1 with Kd/IC50 of 4.1/2.87 nM。
GS-444217 displays >53-fold selectivity over DYRK1A and 104-fold over RSK4 in a panel of 442 kinases。
GS-444217 strongly suppresses the activation of ASK1, p38, and JNK in the kidney resulting in decreased death of parenchymal cells, inflammation, and fibrosis。
GS-444217 abrogates p38 MAPK activation in diabetic kidneys but has no effect upon hypertension in Nos3(-/-) mice。
GS-444217 dose dependently reduced pulmonary arterial pressure and reduced RV hypertrophy in pulmonary arterial hypertension (PAH) models。
GS-444217 also reduces the progressive inflammation and fibrosis in the kidney and halted decline of glomerular filtration rate in models of kidney disease, causes regression of fibrosis combined with RAS inhibitor enalapril.

物理化学性质&存储条件

分子量 411.469
分子式 C23H21N7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-(4-cyclopropyl-1H-imidazol-1-yl)-N-(3-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)phenyl)picolinamide

参考文献

1. Liles JT, et al. J Clin Invest. 2018 Jul 19. pii: 99768. doi: 10.1172/JCI99768.

2. Tesch GH, et al. Diabetes. 2015 Nov;64(11):3903-13.

3. Budas GR, et al. Am J Respir Crit Care Med. 2018 Feb 1;197(3):373-385.

4. Amos LA, et al. J Cell Mol Med. 2018 Jul 11. doi: 10.1111/jcmm.13705.

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