1. PI3K/Akt/mTOR Stem Cell/Wnt
  2. GSK-3
  3. CHIR-98014

CHIR-98014 是一种有效的,细胞通透的 GSK-3 抑制剂,可抑制 GSK-3αGSK-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。

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CHIR-98014 Chemical Structure

CHIR-98014 Chemical Structure

CAS No. : 252935-94-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥910
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1 mg ¥365
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5 mg ¥850
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10 mg ¥1350
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25 mg ¥2800
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50 mg ¥4500
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100 mg ¥6412
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查看 GSK-3 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.

IC50 & Target[1]

GSK-3β

0.58 nM (IC50)

GSK-3α

0.65 nM (IC50)

cdc2

3700 nM (IC50)

体外研究
(In Vitro)

CHIR 98014 抑制人 GSK-3β,Ki 值为 0.87 nM。CHIR 98014 在 CHO-IR 细胞和大鼠肝细胞中引起 GS 刺激,EC50 分别为 106 nM 和 107 nM[1]。CHIR-98014 (1 μM) 将 ES-CCE 细胞的活力降低 52%,IC50 为 1.1 μM。此外,CHIR-98014 与 CHIR-99021 联合使用可显著激活 ES-D3 细胞中的 Wnt/β-连环蛋白通路。在 CHIR-98014 处理的细胞中,T 基因表达被诱导高达 2,500 倍。CHIR-98014 (1 μM) 还可产生约 50% 的 Brachyury 阳性细胞,EC50 为 0.32 μM[2]。CHIR98014 (10 μM) 可防止皮质和海马神经元中 20 μM PrP1-30 引起的神经突丢失,并显著减少死细胞的数量[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CHIR 98014 (30 mg/kg,腹腔注射) 在处理后 4 小时内显著降低空腹高血糖,并在 ipGTT 期间显著改善糖尿病和胰岛素抵抗的 db/db 小鼠的葡萄糖处理[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

486.31

Formula

C20H17Cl2N9O2

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 12.5 mg/mL (25.70 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0563 mL 10.2815 mL 20.5630 mL
5 mM 0.4113 mL 2.0563 mL 4.1126 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥98.0%

参考文献
Kinase Assay
[1]

Polypropylene 96-well plates are filled with 300 μL/well buffer (50 mM tris HCl, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mM β-glycerophosphate, 1 mM NaF, 0.01% BSA, pH 7.5) containing kinase, peptide substrate, and any activators. Information on the kinase concentration, peptide substrate, and activator for these assays is as follows: GSK-3α (27 nM, and 0.5 μM biotin-CREB peptide); GSK-3β (29 nM, and 0.5 μM biotin-CREB peptide); cdc2 (0.8 nM, and 0.5 μM biotin histone H1 peptide); erk2 (400 units/mL, and myelin basic protein-coated Flash Plate); PKC-α (1.6 nM, 0.5 μM biotin-histone H1 peptide, and 0.1 mg/mL phosphatidylserine + 0.01 mg/mL diglycerides); PKC-ζ (0.1 nM, 0.5 μM biotin-PKC-86 peptide, and 50 μg/mL phosphatidylserine + 5 μg/mL diacylglycerol); akt1 (5.55 nM, and 0.5 μM biotin phospho-AKT peptide); p70 S6 kinase (1.5 nM, and 0.5 μM biotin-GGGKRRRLASLRA); p90 RSK2 (0.049 units/mL, and 0.5 μM biotin-GGGKRRRLASLRA); c-src (4.1 units/mL, and 0.5 μM biotin-KVEKIGEGTYGVVYK); Tie2 (1 μg/mL, and 200 nM biotin-GGGGAPEDLYKDFLT); flt1 (1.8 nM, and 0.25 μM KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2); KDR (0.95 nM, and 0.25 μM KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2); bFGF receptor tyrosine kinase (RTK; 2 nM, and 0.25 μM KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2); IGF1 RTK (1.91 nM, and 1 μM biotin-GGGGKKKSPGEYVNIEFG-amide); insulin RTK (using DG44 IR cells); AMP kinase (470 units/mL, 50 μM SAMS peptide, and 300 μM AMP); pdk1 (0.25 nM, 2.9 nM unactivated Akt, and 20 μM each of DOPC and DOPS + 2 μM PIP3); CHK1 (1.4 nM, and 0.5 μM biotin-cdc25 peptide); CK1-ε (3 nM, and 0.2 μM biotin-peptide); DNA PK (see 31); and phosphatidylinositol (PI) 3-kinase (5 nM, and 2 μg/mL PI). Test compounds or controls are added in 3.5 μL of DMSO, followed by 50 μL of ATP stock to yield a final concentration of 1 μM ATP in all cell-free assays. After incubation, triplicate 100-μL aliquots are transferred to Combiplate eight plates containing 100 μL/well 50 μM ATP and 20 mM EDTA. After 1 h, the wells are rinsed five times with PBS, filled with 200 μL of scintillation fluid, sealed, left 30 min, and counted in a scintillation counter. All steps are performed at room temperature. Inhibition is calculated as 100% × (inhibited − no enzyme control)/(DMSO control − no enzyme control)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

The viability of the mouse ES cells is determined after exposure to different concentrations of GSK3 inhibitors for three days using the MTT assay. The decrease of MTT activity is a reliable metabolism-based test for quantifying cell viability; this decrease correlates with the loss of cell viability. 2,000 cells are seeded overnight on gelatine-coated 96-well plates in LIF-containing ES cell medium. On the next day the medium is changed to medium devoid of LIF and with reduced serum and supplemented with 0.1-1 μM BIO, or 1-10 μM SB-216763, CHIR-99021 or CHIR-98014. Basal medium without GSK3 inhibitors or DMSO is used as control. All tested conditions are analyzed in triplicates[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Blood is obtained by shallow tail snipping at lidocaine-anesthetized tips. Blood glucose is measured directly or heparinized plasma is collected for measurement of glucose or insulin. Animals are prebled and randomized to vehicle control or GSK-3 inhibitor treatment groups. For glucose tolerance tests (GTTs), animals are fasted throughout the procedure with food removal early in the morning, 3 h before 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 is measured, food is removed ∼16 h before test agent administration. The glucose challenges in the GTT are 1.35 g/kg i.p. (ipGTT) or 2 g/kg via oral gavage (oGTT). Test inhibitors are formulated as solutions in 20 mM citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

CHIR-98014 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0563 mL 10.2815 mL 20.5630 mL 51.4075 mL
5 mM 0.4113 mL 2.0563 mL 4.1126 mL 10.2815 mL
10 mM 0.2056 mL 1.0282 mL 2.0563 mL 5.1408 mL
15 mM 0.1371 mL 0.6854 mL 1.3709 mL 3.4272 mL
20 mM 0.1028 mL 0.5141 mL 1.0282 mL 2.5704 mL
25 mM 0.0823 mL 0.4113 mL 0.8225 mL 2.0563 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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