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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 (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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 302 | In stock | |
2 mg | ¥ 511 | In stock | |
5 mg | ¥ 847 | In stock | |
10 mg | ¥ 1,410 | In stock | |
25 mg | ¥ 2,400 | In stock | |
50 mg | ¥ 3,410 | In stock | |
100 mg | ¥ 4,920 | In stock | |
200 mg | ¥ 6,530 | In stock | |
1 mL x 10 mM (in DMSO) | ¥ 886 | In stock |
CHIR-99021 相关产品
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 | HepG2 cells:1.5 μM (EC50), CDC2:8800 nM, CHO cells:0.13 μM (EC50), 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。 |
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。 |
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 |
Smiles | Cc1c[nH]c(n1)-c1cnc(NCCNc2ccc(cn2)C#N)nc1-c1ccc(Cl)cc1Cl |
密度 | 1.48 g/cm3 |
颜色 | White |
物理性状 | Solid |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 105 mg/mL (225.64 mM), Sonication is recommended. ![]() | |||||||||||||||||||||||||||||||||||
体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 0.93 mg/mL (2 mM), Solution. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。![]() | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
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