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产品编号 T2310   CAS 252917-06-9
别名: Laduviglusib, CT99021, CHIR-99021

CHIR-99021 (CT99021) 是一种 Wnt/β-catenin 信号通路激活剂,也是一种 GSK-3α/β抑制剂 (IC50=10/6.7 nM),具有选择性和口服活性。CHIR-99021 可以诱导细胞自噬,可增强小鼠和人类胚胎干细胞的自我更新。

CHIR-99021 Chemical Structure
CHIR-99021, CAS 252917-06-9
规格 价格/CNY 货期 数量
1 mg ¥ 318 现货
2 mg ¥ 538 现货
5 mg ¥ 892 现货
10 mg ¥ 1,490 现货
25 mg ¥ 2,530 现货
50 mg ¥ 3,590 现货
100 mg ¥ 5,180 现货
200 mg ¥ 6,890 现货
500 mg ¥ 9,500 现货
1 mL * 10 mM (in DMSO) ¥ 933 现货
其他形式的 CHIR-99021:
千万补贴 助力科研
产品目录号及名称: CHIR-99021 (T2310)
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存储 & 溶解度
产品描述 CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.
靶点活性 GSK-3α:10 nM (cell free), GSK-3β:6.7 nM (cell free)
体外活性 方法:小鼠干细胞 ES-D3 用 CHIR-99021 (1-10 µM) 处理 72 h,使用 MTT 方法检测细胞生长抑制情况。
结果:CHIR-99021 剂量依赖性地抑制 ES-D3 细胞生长,IC50 为 4.9 µM。[1]
方法:小鼠胚胎干细胞 J1 mESCs 和小鼠胚胎瘤细胞 F9 mEC 用 CHIR-99021 (3 μM) 处理 24 h,使用 immunofluorescence 方法检测靶点蛋白表达水平。
结果:CHIR-99021 处理后,J1-mESCs 和 F9-mEC 细胞的细胞质和细胞核中的β-连环蛋白增加。[2]
方法:人 Tenon 成纤维细胞 HTFs 用 CHIR-99021 (5 μM) 处理 48 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:CHIR-99021 处理使活性形式的 GSK-3β (p-GSK-3β (Y216)) 的产生显著减少。[3]
体内活性 方法:为检测体内抗肿瘤活性,将 CHIR-99021 (37.5 mg/kg/第 0-3、6-10、13-17 和 20 天每天两次) 口服给药和 paclitaxel (10 mg/kg/第 0 天单次给药) 腹腔注射给携带人非小细胞肺癌肿瘤 H1975 的 Balb/c nude 小鼠。
结果:CHIR-99021 和 paclitaxel 在体内协同作用,抑制 NSCLC 肿瘤的生长。[4]
方法:为研究 GSK-3 的直接药理学抑制是否会改变酒精在小鼠体内的积极增强作用,将 CHIR-99021 (1-10 mg/kg) 单次腹腔注射给有酒精或蔗糖自给药史的 C57BL/6J 小鼠。
结果:CHIR-99021 剂量依赖性地增加了酒精强化反应,而对蔗糖自我给药或运动活性没有影响。CHIR-99021 显著降低了 pGSK-3β 在所有测试脑区的表达,仅在 NAcb 中降低了 PICK1 并增加了 GluA2 的总表达。[5]
激酶实验 Kinases were purified from SF9 cells through the use of their His or Glu tag. Glu-tagged proteins were purified as described, and His-tagged proteins were purified according to the manufacturer's instructions. Kinase assays were performed in 96-well plates with appropriate peptide substrates in a 300-μl reaction buffer (variations on 50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mMβ-glycerophosphate, 1 mM NaF, and 0.01% bovine serum albumin). Peptides had Km values from 1 to 100 μM. CHIR 99021 or CHIR GSKIA was added in 3.5 μl of Me2SO, followed by ATP to a final concentration of 1 μM. After incubation, triplicate 100-μl aliquots were transferred to Combiplate 8 plates containing 100 μl/well of 50 μM ATP and 20 mM EDTA. After 1 hour, the wells were rinsed five times with phosphate-buffered saline, filled with 200 μl of scintillation fluid, sealed, and counted in a scintillation counter 30 min later. All of the steps were at room temperature. The percentage of inhibition was calculated as 100 × (inhibitor ? no enzyme control)/(Me2SO control ? no enzyme control) [4].
细胞实验 The Wnt/beta-catenin reporter assay was performed with the M50 Super 8× TOPFlash and M51 Super 8× FOPFlash vector containing the firefly luciferase gene under the control of TCF/LEF binding sites or mutated bindings sites. 12,500 cells were seeded overnight on gelatine-coated 96-well plates in LIF-containing ES cell medium. On the next day, the cells were transfected using Lipofectamine with one of the aforementioned vectors plus pGL4.75 [hRluc/CMV] encoding the renilla luciferase reporter gene hRluc as a transfection control. Six hours after transfection the medium was changed to medium devoid of LIF, with reduced serum, and supplemented with 5 μM CHIR-99021. The Dual-Luciferase? reporter assay system was employed 48 and 72 h after the medium change to follow the luminescence reaction using a GloMax?-multi detection system [4].
动物实验 Blood was obtained by shallow tail snipping at lidocaine-anesthetized tips. Blood glucose was measured directly or heparinized plasma was collected for measurement of glucose or insulin. Animals were pre-bled and randomized to vehicle control or GSK-3 inhibitor treatment groups. For glucose tolerance tests (GTTs), animals fasted throughout the procedure with food removal early in the morning, 3 h before the first prebleed (db/db mice), or the previous night, 16 h before the bleed (ZDF rats). When the time course of plasma glucose and insulin changes in fasting ZDF rats was measured, food was removed ~16 h before test agent administration. The glucose challenges in the GTT were 1.35 g/kg i.p. (ipGTT) or 2 g/kg via oral gavage (oGTT). CHIR-99021 were formulated as solutions in 20 mmol/l citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose [1].
别名 Laduviglusib, CT99021, CHIR-99021
分子量 465.34
分子式 C22H18Cl2N8
CAS No. 252917-06-9


Powder: -20°C for 3 years | In solvent: -80°C for 1 year


DMSO: 50 mg/mL (107.45 mM)


可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.149 mL 10.7448 mL 21.4897 mL 53.7242 mL
5 mM 0.4298 mL 2.149 mL 4.2979 mL 10.7448 mL
10 mM 0.2149 mL 1.0745 mL 2.149 mL 5.3724 mL
20 mM 0.1074 mL 0.5372 mL 1.0745 mL 2.6862 mL
50 mM 0.043 mL 0.2149 mL 0.4298 mL 1.0745 mL
100 mM 0.0215 mL 0.1074 mL 0.2149 mL 0.5372 mL

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TargetMol Library Books参考文献

1. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors. BMC Res Notes. 2014 Apr 29;7:273. 2. Wu Y, et al. GSK3 inhibitors CHIR99021 and 6-bromoindirubin-3'-oxime inhibit microRNA maturation in mouse embryonic stem cells. Sci Rep. 2015 Mar 2;5:8666. 3. Lee SY, et al. The Effect of CHIR 99021, a Glycogen Synthase Kinase-3β Inhibitor, on Transforming Growth Factor β-Induced Tenon Fibrosis. Invest Ophthalmol Vis Sci. 2021 Dec 1;62(15):25. 4. O'Flaherty L, et al. Tumor growth suppression using a combination of taxol-based therapy and GSK3 inhibition in non-small cell lung cancer. PLoS One. 2019 Apr 10;14(4):e0214610. 5. Faccidomo S, et al. Pharmacological inhibition of glycogen synthase kinase 3 increases operant alcohol self-administration in a manner associated with altered pGSK-3β, protein interacting with C kinase and GluA2 protein expression in the reward pathway of male C57BL/6J mice. Behav Pharmacol. 2020 Feb;31(1):15-26. 6. Gong-Bo Fu, Wei-Jian Huang, Min Zeng, Xu Zhou, Hong-Ping Wu, Chang-Cheng Liu, Han Wu, Jun Weng, Hong-Dan Zhang, Yong-Chao Cai, Charles Ashton, Min Ding, Dan Tang, Bao-Hua Zhang, Yi Gao, Wei-Feng Yu, Bo Zhai, Zhi-Ying He, Hong-Yang Wang, and He-Xin Yan . Expansion and differentiation of human hepatocyte-derived liver progenitor-like cells and their use for the study of hepatotropic pathogens [J]. Cell Research. 2019 Jan;29(1):8-22.

TargetMol Library Books文献引用

1. Lin Y Y, Yao R, Zhuang J, et al.PACT inhibits the replication of SARS‐CoV‐2 through the blockage of GSK‐3β‐N‐nsp3 cascade.Journal of Medical Virology.2023, 95(6): e28832. 2. Yu Y, Li X, Jiao R, et al.H3K27me3-H3K4me1 transition at bivalent promoters instructs lineage specification in development.Cell & Bioscience.2023, 13(1): 1-20. 3. Wu M, Zhang X, Zhang W, et al.Paracrine secretion of IL8 by breast cancer stem cells promotes therapeutic resistance and metastasis of the bulk tumor cells.Cell Communication and Signaling.2023, 21(1): 1-17. 4. Han L, Song B, Zhang P, et al.PC3T: a signature-driven predictor of chemical compounds for cellular transition.Communications Biology.2023, 6(1): 989. 5. Yang Y, Xiao L, Xue Y, et al.ZBTB7A regulates primed‐to‐naïve transition of pluripotent stem cells via recognition of the PNT‐associated sequence by Zinc Fingers 1–2 and recognition of γ‐globin− 200 gene element by Zinc Fingers 1–4.The FEBS Journal.2023 6. Yang Z, Liu H, Song R, et al. Reduced MAGI3 level by HPV18E6 contributes to Wnt/β‐catenin signaling activation and cervical cancer progression. FEBS Open bio. 2021, 11(11): 3051. 7. He W, Zhu X, Xin A, et al. Long-term maintenance of human endometrial epithelial stem cells and their therapeutic effects on intrauterine adhesion. Cell & Bioscience. 2022, 12(1): 1-20. 8. Fu G B, Huang W J, Zeng M, et al. Expansion and differentiation of human hepatocyte-derived liver progenitor-like cells and their use for the study of hepatotropic pathogens. Cell Research. 2019, 29(1): 8-22 9. Ma X, Lu Y, Zhou Z, Human expandable pancreatic progenitor–derived β cells ameliorate diabetes. Science Advances. 2022, 8(8): eabk1826. 10. Wang W, Ren S, Lu Y, et al. Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production. The EMBO Journal. 2021 Jun 1;40(11):e106771. doi: 10.15252/embj.2020106771. Epub 2021 Apr 28.
KenPaullone Bakkenolide A AR-A014418 GSK3β inhibitor II GNF4877 Dehydroglyasperin D Moringin Indirubin-3′-oxime


神经退行性疾病化合物库 激酶抑制剂库 抑制剂库 高选择性抑制剂库 细胞骨架化合物库 抗结直肠癌化合物库 抗糖尿病库 PI3K/Akt/mTOR 化合物库 抗癌化合物库 抗胰腺癌化合物库

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CHIR-99021 252917-06-9 Autophagy Cytoskeletal Signaling PI3K/Akt/mTOR signaling Stem Cells GSK-3 Wnt/beta-catenin Glycogen synthase kinase 3 CHIR99021 β-catenin Laduviglusib inhibit CT99021 Beta catenin CT-99021 CHIR 99021 Wnt Inhibitor Glycogen synthase kinase-3 CT 99021 inhibitor


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