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JNK-IN-8

JNK-IN-8 (JNK Inhibitor XVI) 是一种有效的JNK 抑制剂，抑制JNK1、JNK2和JNK3，IC50分别为 4.7、18.7 和 1 nM。

CAS号

1410880-22-6

分子式

C29H29N7O2

主要靶点

c-Kit|JNK

仅限科研使用

Cat No : CM04926

Print datasheet

Synonyms

JNK Inhibitor XVI

验证数据展示

  • CAS No.: 1410880-22-6

    JNK-IN-8
    CAS#: 1410880-22-6

产品信息

JNK-IN-8 is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line.

CAS号 1410880-22-6
分子式 C29H29N7O2
主要靶点 c-Kit|JNK
主要通路 MAPK信号通路|蛋白酪氨酸激酶
分子量 507.59
纯度 98.25%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 JNK Inhibitor XVI

靶点活性

JNK2:18.7 nM|JNK1:4.7 nM|JNK:1 nM

体内活性

JNK-IN-8（10 mM）对IL-1R细胞中IL-1β刺激的c-Jun磷酸化有抑制作用。与伊马替尼相比,JNK-IN-8有明显的1,4-双苯胺和1,3-氨基苯甲酸结构区域选择性,且以N,N-二甲基丁烯乙酰胺共价结合Cys154靶点。JNK-IN-8抑制HeLa（EC50：486 nM）和A375（EC50：338 nM）细胞中c-Jun的磷酸化。JNK-IN-8与PIK3C3,IRAK1,PIP5K3和PIP4K2C结合可使选择性和消除率显著提高。JNK-IN-8经Cys116抑制JNK2。

溶解度

Ethanol:<1 mg/mL,H2O:<1 mg/mL,DMSO:93 mg/mL (183.2 mM)

细胞实验

JNK-IN-8 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. HEK-293 cells stably expressing Interleukin Receptor 1 (HEK293-IL1R) are cultured in Dulbecco's Modified Eagle's medium (DMEM) supplemented with 10% FBS, 2 mM glutamine and 1×antimycotic/antibiotic solution. Cells are serum starved for 18 h before incubation with DMSO or JNK-IN-8, stimulated with 2 μM Anisomycin for 1h and lysates are clarified by centrifugation for 10 min at 16000 g and 4°C[1].

参考文献

1.Zhang T, et al. Chem Biol, 2012, 19(1), 140-154.
2.Goh ET, et al. Biochem J, 2012, 441(1), 339-346.
3.Liu Q, et al. Chem Biol, 2013, 20(2), 146-159.

The molarity calculator equation

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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