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CHIR-98014

CAS No. : 252935-94-7

MCE 站：CHIR-98014

产品活性：CHIR-98014 是一种有效的，细胞通透的 GSK-3 抑制剂，可抑制 GSK-3α 和 GSK-3β 的活性，IC₅₀ 值分别为 0.65 和 0.58 nM；CHIR-98014 对 cdc2 和 erk2 的作用较弱。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt

作用靶点：GSK-3

In Vitro: CHIR 98014 inhibits human GSK-3β with K_i value of 0.87 nM. CHIR 98014 causes GS stimulation in CHO-IR cells and rat hepatocytes, with EC₅₀s of 106 nM and 107 nM, respectively. CHIR-98014 (1 μM) reduces the viability of ES-CCE cells by 52%, with IC₅₀ of 1.1 μM. Moreover, CHIR-98014 in combination with CHIR-99021 results in a significant activation of the Wnt/beta-catenin pathway in ES-D3 cells. In CHIR-98014 treated cells, the T gene expression is induced up to 2,500-fold. CHIR-98014 (1 μM) also yields around 50% Brachyury-positive cells, with EC₅₀ of 0.32 μM. CHIR98014 (10 μM) prevents loss of neurites caused by 20 μM PrP1-30 in cortical and hippocampal neurons, and substantially decreases the amount of dead cells.

In Vivo: CHIR 98014 (30 mg/kg, i.p.) exhibits a significant reduction in fasting hyperglycemia within 4 h of treatment and shows improved glucose disposal during an ipGTT in markedly diabetic and insulin-resistant db/db mice.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Aging Compound Library  |  Reprogramming Compound Library  |  Diabetes Related Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  CHIR-99021  |  SB 216763  |  AR-A014418  |  TDZD-8  |  Kenpaullone  |  GSK 3 Inhibitor IX  |  Cromolyn sodium  |  R547  |  SB 415286  |  IM-12  |  Indirubin-3'-monoxime  |  1-Azakenpaullone  |  AZD2858  |  BIO-acetoxime  |  CP21R7  |  Bikinin  |  GNF4877  |  GSK-3β inhibitor 1  |  hSMG-1 inhibitor 11j  |  TCS 21311  |  BIP-135  |  5-Iodo-indirubin-3'-monoxime  |  Alsterpaullone  |  GSK-3 inhibitor 1  |  GSK-3β inhibitor 2  |  Manzamine A hydrochloride  |  2B-(SP)

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