{{cart_num}}
My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > PI3K/Akt/mTOR > CHIR-99021 HydrochlorideCAS：1797989-42-4
Molecular Formula：C22H18Cl2N8·HCl
Molecular Weight：501.8
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
Qty：
Size：
| CAS | 1797989-42-4 |
| Name | CHIR-99021 Hydrochloride |
| Molecular Formula | C22H18Cl2N8·HCl |
| Molecular Weight | 501.8 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD30489757 |
| SMILES | N#CC1=CC=C(NCCNC2=NC=C(C3=NC=C(C)N3)C(C4=CC=C(Cl)C=C4Cl)=N2)N=C1.[H]Cl |
| Target Point | GSK-3α，GSK-3β |
| Passage | PI3K/Akt/mTOR;Stem Cells |
| Background | It is a GSK-3α/β inhibitor. |
| Biological Activity | CHIR-99021的盐酸盐, 是GSK-3α/β抑制剂，IC50为10 nM/6.7 nM。其对GSK-3的选择性比对Cdc2和ERK2高500倍以上。CHIR-99021 是一种有效的药理性的 Wnt/beta-catenin 信号通路的激活剂。CHIR-99021 可显著地拯救光诱导的 autophagy，并可增强 GR，RORα和自噬相关蛋白等表达。[1-3] |
| In Vitro | CHIR-99021作用于GSK-3比作用于其最接近的同系物CDC2和ERK2，及其他蛋白激酶选择性高500倍。此外，CHIR-99021只与一组22种药理相关的受体微弱结合，且对一组23种非激酶的酶几乎没有抑制活性。CHIR-99021作用于表达胰岛素受体的CHO-IR细胞，诱导糖原合成酶(GS)激活，EC50为0.763 μM。[1]CHIR-99021(3 μM)作用于3T3-L1前脂肪细胞，除了模拟胰岛素的作用，抑制GSK-3，使胞内游离β-catenin增加1.9倍，模仿经典Wnt信号通路。在分化的前3天，CHIR-99021处理，抑制脂肪细胞分化，IC50为0.3 μM，通过抑制CCAAT/增强子结合蛋白α(C/EBPα)和过氧化物酶体增殖物激活受体γ(PPARγ)的诱导作用。[2] 不像LiCl和AR-A014418，CHIR-99021处理，即使在高浓度，不会降低INS-1E细胞活力。相反，CHIR-99021增加INS-1E细胞增殖，这种作用具有剂量依赖性，且显著抑制高糖和高棕榈酸诱导的INS-E细胞死亡，这种作用具有浓度依赖性。CHIR-99021浓度低至1 μM，处理离体大鼠胰岛，促进β细胞复制，5 μM CHIR-99021处理，使细胞复制增长2-3倍。[3] |
| In Vivo | CHIR-99021按30 mg/kg 剂量口服处理患2型糖尿病的啮齿类动物模型，增强葡萄糖代谢，处理3-4小时后，最大血浆葡萄糖减少近150 mg/dl，而血浆胰岛素保持或低于对照水平。CHIR-99021按16 或 48 mg/kg剂量口服给药ZDF大鼠，1小时后，再口服葡萄糖，显著改善糖耐量，16 mg/kg 和 48 mg/kg处理组的血浆葡萄糖分别减少14％和33％，较高剂量CHIR-99021处理，再口服葡萄糖，还可以降低高血糖。[1]CHIR-99021处理移植小鼠或人造血干细胞(HSC)的受体小鼠，显著增强造血重建功能，说明GSK-3是一种特异性的HSC活性调节剂。[4] |
| Animal Experiment | Animal Models: 雌性db/db小鼠或雄性2型糖尿病ZDF大鼠; Dosages: ~48 mg/kg; Administration: 口服处理[1] |
| Data Literature Source | [1] Ring DB，et al. Diabetes，2003，52(3)，588-595. [2] Bennett CN，et al. J Biol Chem，2002，277(34)，30998-31004. [3] Mussmann R，et al. J Biol Chem，2007，282(16)，12030-12037 |
| Unit | Bottle |
| Specification | 5mg |
是一个GSK-3α/β的抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Sorry, there is no more information.
Sorry, there is no more information.
Manual Download
