JNK

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抑制剂选择性比较

特异性亚型抑制剂

JNK产品

所有产品 JNK抑制剂(8) JNK激活剂(2) 新JNK产品

产品目录	产品描述	文献引用	实验数据
S1460	SP600125 SP600125是一种广谱JNK抑制剂，作用于JNK1，JNK2和JNK3，无细胞试验中IC50分别为40 nM，40 nM和90 nM，比作用于MKK4选择性高10倍，比作用于MKK3， MKK6， PKB，和PKCα选择性高25倍，比作用于ERK2， p38， Chk1， EGFR等选择性高100倍。	Cancer Cell, 2019, 35(5):798-815 Cancer Cell, 2019, 36(1):68-83 Mol Cell, 2019, 76(1):148-162	Loss of DUSP4 function upregulates IL-6 and IL-8 and enhances mammosphere growth. Immunoblot analysis of MDA-231 cells after treatment of 24 hours with 1 umol/L selumetinib (MEKi) or 10 umol/L SP600125 (JNKi). I, MDA-231 mammosphere formation quantitated by GelCount software 7 days after siRNA transfection. Where indicated, selumetinib (MEKi) or SP600125 (JNK1) or the combination was added to the mammosphere cultures.
S4901	JNK-IN-8 JNK-IN-8是第一个不可逆的JNK抑制剂，作用于JNK1，JNK2和JNK3，在A375细胞系中IC50分别为4.7 nM，18.7 nM和1 nM，比作用于MNK2，Fms选择性高10倍以上，对c-Kit， Met， PDGFRβ没有抑制作用。	Nat Genet, 2019, 51(6):999-1010 Cancer Cell, 2019, 36(1):68-83 Clin Cancer Res, 2019, 25(13):4117-4127	SCC-9 cells were pre-treated with JNK inhibitor SP 600125 (1 umol/L) or JNK-IN-8 (1 umol/L) for 1 h, cells were also stimulated with indicated AZD8055 and cultured for 72 h, cell survival was analyzed. Scramble RNAi or JNK1/2 RNAi (JNK RNAi-1 or JNK RNAi-2, see methods) transfected HEK-293 cells were stimulated with AZD8055, cells were further cultured for 72 h before cell survival was tested.
S8867^New	Bentamapimod (AS602801) Bentamapimod (AS602801)是新型的、具有口服活性的JNK抑制剂，对JNK1、JNK2、JNK3的IC50值分别为80 nM、90 nM和230 nM。
S7508	JNK Inhibitor IX JNK inhibitor IX 是一种高度选择性JNK抑制剂，其作用于JNK2和JNK3的pIC50分别为6.5和6.7。	Tumour Biol, 2016, 37(3):3135-44	ICT induces JNK activation, mediating mPTP opening and CRC cell necrosis. JNK expression (p- and regular) in HT-29 or the primary CRC cells stimulated with applied ICT was tested by Western blots (a). HT-29 cells were pre-treated with JNK inhibitors SP600125 (SP), JNK inhibitor IX (JNK-IX), and JNK-IN-8 (JNKi-8) (5 μM each) for 1 h, followed by ICT (25 μM) stimulation, MMP decrease was tested by JC-10 dye assay (b, after 12 h), and cell necrosis was tested by LDH release assay (c, after 72 h).
S6711^New	IQ-1S IQ-1S是JNK3抑制剂，对JNK3、JNK2、JNK1的Kd值分别为87 nM、360 nM和390 nM。
S6730^New	CC-401 Hydrochloride CC-401是有效的JNK抑制剂，其对JNK的选择性是对其他相关性激酶的选择性的至少40倍。
S8490	Tanzisertib(CC-930) CC-930对依赖于JNK的蛋白质底物c-Jun和JNK所有亚型的磷酸化具有ATP竞争性抑制作用(Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM)，选择性抑制ERK1和p38a的IC50分别为0.48 μM和3.4 μM。
S8201	BI-78D3 BI-78D3是一种竞争性的JNK抑制剂，IC50为280 nM，其选择性比对p38α高100倍，对mTOR和PI-3K没有活性。
S7409	Anisomycin Anisomycin 是一种抗生素，抑制蛋白质合成，也是一种 JNK 激活剂。	J Physiol Sci, 2019, 69(3):489-502 Cell Cycle, 2019, 18(4):379-394 Int J Mol Med, 2019, 44(1):89-102	Effect of TMZ (100 μmol/l for U87 cells, 50 μmol/l for U251 cells), anisomycin (4 μmol/l), SB203580 (10 μmol/l), TMZ+SB203580 (10 μmol/l) treatment on thephosphorylation of p38 and AQP4 for 24 h in U87 cells and U251 cells, detected by Western blotting. (A) Protein expression of p-p38, p38 and AQP4 in U87 cells with differenttreatments. (B) The ration of p-p38/p38 in U87 cells. (C) The proportion of AQP4 in GAPDH in U87 cells. (D) Protein expression of p-p38, p38 and AQP4 in U251 cells withdifferent treatments. (E) The ration of p-p38/p38 in U251 cells. (F) The proportion of AQP4 in GAPDH in U251 cells. *P< 0.05 versus the control group
S7637	DTP3 DTP3是一种选择性GADD45β/MKK7抑制剂，能够抑制癌症选择性NF-κB存活途径。

产品目录	产品描述	文献引用	实验数据
S1460	SP600125 SP600125是一种广谱JNK抑制剂，作用于JNK1，JNK2和JNK3，无细胞试验中IC50分别为40 nM，40 nM和90 nM，比作用于MKK4选择性高10倍，比作用于MKK3， MKK6， PKB，和PKCα选择性高25倍，比作用于ERK2， p38， Chk1， EGFR等选择性高100倍。	Cancer Cell,2019, 35(5):798-815 Cancer Cell,2019, 36(1):68-83 Mol Cell,2019, 76(1):148-162	Loss of DUSP4 function upregulates IL-6 and IL-8 and enhances mammosphere growth. Immunoblot analysis of MDA-231 cells after treatment of 24 hours with 1 umol/L selumetinib (MEKi) or 10 umol/L SP600125 (JNKi). I, MDA-231 mammosphere formation quantitated by GelCount software 7 days after siRNA transfection. Where indicated, selumetinib (MEKi) or SP600125 (JNK1) or the combination was added to the mammosphere cultures.
S4901	JNK-IN-8 JNK-IN-8是第一个不可逆的JNK抑制剂，作用于JNK1，JNK2和JNK3，在A375细胞系中IC50分别为4.7 nM，18.7 nM和1 nM，比作用于MNK2，Fms选择性高10倍以上，对c-Kit， Met， PDGFRβ没有抑制作用。	Nat Genet,2019, 51(6):999-1010 Cancer Cell,2019, 36(1):68-83 Clin Cancer Res,2019, 25(13):4117-4127	SCC-9 cells were pre-treated with JNK inhibitor SP 600125 (1 umol/L) or JNK-IN-8 (1 umol/L) for 1 h, cells were also stimulated with indicated AZD8055 and cultured for 72 h, cell survival was analyzed. Scramble RNAi or JNK1/2 RNAi (JNK RNAi-1 or JNK RNAi-2, see methods) transfected HEK-293 cells were stimulated with AZD8055, cells were further cultured for 72 h before cell survival was tested.
S8867^New	Bentamapimod (AS602801) Bentamapimod (AS602801)是新型的、具有口服活性的JNK抑制剂，对JNK1、JNK2、JNK3的IC50值分别为80 nM、90 nM和230 nM。
S7508	JNK Inhibitor IX JNK inhibitor IX 是一种高度选择性JNK抑制剂，其作用于JNK2和JNK3的pIC50分别为6.5和6.7。	Tumour Biol,2016, 37(3):3135-44	ICT induces JNK activation, mediating mPTP opening and CRC cell necrosis. JNK expression (p- and regular) in HT-29 or the primary CRC cells stimulated with applied ICT was tested by Western blots (a). HT-29 cells were pre-treated with JNK inhibitors SP600125 (SP), JNK inhibitor IX (JNK-IX), and JNK-IN-8 (JNKi-8) (5 μM each) for 1 h, followed by ICT (25 μM) stimulation, MMP decrease was tested by JC-10 dye assay (b, after 12 h), and cell necrosis was tested by LDH release assay (c, after 72 h).
S6711^New	IQ-1S IQ-1S是JNK3抑制剂，对JNK3、JNK2、JNK1的Kd值分别为87 nM、360 nM和390 nM。
S6730^New	CC-401 Hydrochloride CC-401是有效的JNK抑制剂，其对JNK的选择性是对其他相关性激酶的选择性的至少40倍。
S8490	Tanzisertib(CC-930) CC-930对依赖于JNK的蛋白质底物c-Jun和JNK所有亚型的磷酸化具有ATP竞争性抑制作用(Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM)，选择性抑制ERK1和p38a的IC50分别为0.48 μM和3.4 μM。
S8201	BI-78D3 BI-78D3是一种竞争性的JNK抑制剂，IC50为280 nM，其选择性比对p38α高100倍，对mTOR和PI-3K没有活性。

产品目录

产品描述

文献引用

实验数据

S7409

Anisomycin

Anisomycin 是一种抗生素，抑制蛋白质合成，也是一种 JNK 激活剂。

J Physiol Sci, 2019, 69(3):489-502

Cell Cycle, 2019, 18(4):379-394

Int J Mol Med, 2019, 44(1):89-102

S7637

DTP3

DTP3是一种选择性GADD45β/MKK7抑制剂，能够抑制癌症选择性NF-κB存活途径。