货号:A133052 同义名: CT99021;Laduviglusib
Laduviglusib (CHIR-99021)是一种有效、选择性且具有口服活性的 GSK-3α/β 抑制剂,可用作细胞疗法中的辅助试剂。
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产品名称 | GSK-3 ↓ ↑ | GSK-3α ↓ ↑ | GSK-3β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
AZD2858 |
+
GSK-3, IC50: 68 nM |
99% | |||||||||||||||||
Bikinin | ✔ | 99%+ | |||||||||||||||||
GSK 3 Inhibitor IX |
++++
GSK-3, IC50: 5 nM |
99%+ | |||||||||||||||||
AZD1080 |
+++
GSK-3α, IC50: 6.9 nM |
++
GSK-3β, IC50: 31 nM |
99%+ | ||||||||||||||||
BIO-acetoxime |
+++
GSK-3α, IC50: 10 nM |
+++
GSK-3β, IC50: 10 nM |
95% | ||||||||||||||||
SB-216763 |
++
GSK-3α, IC50: 34.3 nM |
++
GSK-3β, IC50: ~34.3 nM |
98% | ||||||||||||||||
SB 415286 |
+
GSK-3α, IC50: 78 nM |
+
GSK-3β, IC50: ~78 nM |
99%+ | ||||||||||||||||
CHIR-98014 |
++++
GSK-3α, IC50: 0.65 nM |
++++
GSK-3β, IC50: 0.58 nM |
98% | ||||||||||||||||
LY2090314 |
++++
GSK-3α, IC50: 1.5 nM |
++++
GSK-3β, IC50: 0.9 nM |
99%+ | ||||||||||||||||
CHIR 99021 |
+++
GSK-3α, IC50: 10 nM |
++++
GSK-3β, IC50: 6.7 nM |
99%+ | ||||||||||||||||
TDZD-8 |
+
GSK-3β, IC50: 2 μM |
99%+ | |||||||||||||||||
Indirubin |
+
GSK-3β, IC50: 0.6 μM |
98% | |||||||||||||||||
IM-12 |
++
GSK-3β, IC50: 53 nM |
98% | |||||||||||||||||
TWS119 |
++
GSK-3β, IC50: 30 nM |
99% | |||||||||||||||||
1-Azakenpaullone |
+++
GSK-3β, IC50: 18 nM |
99%+ | |||||||||||||||||
AR-A014418 |
++
GSK-3β, Ki: 38 nM |
99%+ | |||||||||||||||||
Tideglusib |
+
GSK-3β, IC50: 60 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase, consisting of GSK-3α andβsubunit, which plays a key role in many different biological processes including tumorigenesis, cell survival, and developmental patterning. GSK-3 is constitutively active in non-stimulated cells and can negatively regulate canonical Wnt/β-catenin signaling. CHIR 99021 (CT99021)is highly selective aminopyrimidine-derivatived inhibitor of GSK-3 with IC50 of 10nM and 6.7nM for GSK-3α and GSK-3β(measured by kinase assays), respectively, and exhibits >500-fold selectivity for GSK-3 over closely related kinases, such as cdc2[8]Bennett CN, Ross SE, Longo KA, Bajnok L, Hemati N, Johnson KW, Harrison SD, MacDougald OA. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. doi: 10.1074/jbc.M204527200. Epub 2002 Jun 7. PMID: 12055200. https://pubmed.ncbi.nlm.nih.gov/12055200/. CHIR-99021 can mimic Wnt signaling in preadipocytes. Analysis of cytosolic and membranous fractions show that the free cytosolic -catenin was evaluated in 3T3-L1 preadipocytes treated with 3uM CHIR-99021 for 4 h [4]. Chir-99021 can activate glycogen synthase in cells. The concentrations of CHIR-99021 causing half-maximal glycogen synthase stimulation (EC50) were 76 nmol/l for CHO-IR cells. A single oral dose of CHIR 99021 (30mg/kg) rapidly lowered plasma glucose in ZDF rats[8]. In combination with different small molecules, CHIR-99021 can facilitate cardiomyocyte differentiation from human embryonic stem cells and iPS cells[10][9], reprogramming, like generation of functional astrocytes from mammalian fibroblasts[10] and maintaining undifferentiated mouse ES cells in the absence of LIF[11]. |
作用机制 | CHIR 99021 can inhibit GSK3 by competing for their ATP-binding sites. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
human 769-P cell | Growth inhibition assay | Inhibition of human 769-P cell growth in a cell viability assay, IC50=584.99 nM. | SANGER | ||
human A172 cell | Growth inhibition assay | Inhibition of human A172 cell growth in a cell viability assay, IC50=3.75498 μM. | SANGER | ||
human A498 cell | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50=1.3 μM. | SANGER | ||
human A704 cell | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay, IC50=3.0812 μM. | SANGER | ||
Dose | Rat[3] (p.o.): 16 mg/kg - 48 mg/kg | ||||||||
Administration | p.o. | ||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.15mL 0.43mL 0.21mL |
10.74mL 2.15mL 1.07mL |
21.49mL 4.30mL 2.15mL |
CAS号 | 252917-06-9 |
分子式 | C22H18Cl2N8 |
分子量 | 465.338 |
别名 | CT99021;Laduviglusib |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 16 mg/mL(34.38 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear PO 0.5% CMC-Na 55 mg/mL suspension |