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GS-444217
CAS No. 1262041-49-5
GS-444217 ( GS444217 )
产品货号. M11087 CAS No. 1262041-49-5
GS-444217 (GS444217) 是一种有效、选择性、ATP 竞争性、口服 ASK1 抑制剂，Kd/IC50 为 4.1/2.87 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥2271 | 有现货 |
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| 10MG | ￥3316 | 有现货 |
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| 25MG | ￥5292 | 有现货 |
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| 50MG | ￥7403 | 有现货 |
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| 100MG | ￥9630 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥2499 | 有现货 |
|
生物学信息
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产品名称GS-444217
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述GS-444217 (GS444217) 是一种有效、选择性、ATP 竞争性、口服 ASK1 抑制剂，Kd/IC50 为 4.1/2.87 nM。
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产品描述GS-444217 (GS444217) is a potent, selective, ATP-competitive, orally available inhibitor of ASK1 with Kd/IC50 of 4.1/2.87 nM; displays >53-fold selectivity over DYRK1A and 104-fold over RSK4 in a panel of 442 kinases; strongly suppresses the activation of ASK1, p38, and JNK in the kidney resulting in decreased death of parenchymal cells, inflammation, and fibrosis;abrogates p38 MAPK activation in diabetic kidneys but has no effect upon hypertension in Nos3(-/-) mice; dose dependently reduced pulmonary arterial pressure and reduced RV hypertrophy in pulmonary arterial hypertension (PAH) models; 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.
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体外实验——
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体内实验——
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同义词GS444217
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通路MAPK/ERK Signaling
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靶点MEK
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受体ASK1
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研究领域Cancer
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适应症——
化学信息
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CAS Number1262041-49-5
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分子量411.469
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分子式C23H21N7O
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纯度>98% (HPLC)
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溶解度DMSO: 13 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )
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SMILESO=C(NC1=CC=CC(C2=NN=CN2C3CC3)=C1)C4=NC=CC(N5C=C(C6CC6)N=C5)=C4
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化学全称4-(4-cyclopropyl-1H-imidazol-1-yl)-N-(3-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)phenyl)picolinamide
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
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.
