JNK

信号通路图

研究领域

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(14) JNK激活剂(5)

目录号	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。SP600125也是一种广谱的serine/threonine kinases抑制剂，包括Aurora kinase A、FLT3和TRKA，对应的IC50值为60 nM、90 nM和70 nM。SP600125可抑制自噬而激活细胞凋亡。	Nat Commun, 2020, 8;11(1):2286 Cancer Res, 2020, 9 pii: canres J Control Release, 2020, 320:201-213	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.
S1574	Doramapimod (BIRB 796) Doramapimod (BIRB 796)是一种泛p38 MAPK抑制剂，在无细胞试验中作用于p38α/β/γ/δ的IC50分别为38 nM，65 nM，200 nM 和520 nM，并且能够与p38α结合，在THP-1细胞中K_d为0.1 nM，比作用于JNK2选择性高330倍，对c-RAF，Fyn 和Lck具有较弱的抑制作用，对ERK-1，SYK，IKK2也有微弱抑制作用。	Nature, 2020, 3 Nature, 2020, 3 Genome Biol, 2020, 21(1):33	Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.
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。	Genome Biol, 2020, 21(1):33 Cell Chem Biol, 2020, 20;27(2):197-205.e6 J Cell Physiol, 2020, 235(3):2792-2799	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.
S6740^New	DB07268 DB07268是有效的选择性JNK1抑制剂，IC50为9 nM，对JNK1的效力是对CHK1、CK2和PLK的70-90倍。
S7794^New	JNK Inhibitor VIII JNK Inhibitor VIII (TCS JNK 6o) 是一种 c-Jun N-terminal kinases 的抑制剂，对JNK-1和JNK-2的IC50值分别为45 nM和160 nM。JNK Inhibitor VIII (TCS JNK 6o) 可抑制JNK-1、JNK-2和JNK-3，对应的Ki值分别为2 nM、4 nM和52 nM。
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。
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。	Nat Biomed Eng, 2018, 2(8):578-588
S3901	Astragaloside IV Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems.
S4884	Trans-Zeatin Trans-Zeatina是植物生长激素的成员之一，属于细胞分裂素，可调节细胞分裂、发育和营养加工。
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。	Nat Commun, 2020, 11(1):258 Cell Discov, 2019, 5:2 Elife, 2018, 7	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).
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。	Int J Cancer, 2020, 146(9):2563-2575 Cell Discov, 2019, 5:2
S3811	Ginsenoside Re Ginsenoside Re (Ginsenoside B2) 是三七的提取物、人参中的主要人参皂苷，属于20(S)-原人参三醇组 (protopanaxatriol group)。它具有多种体外和体内作用，包括血管舒张作用，抗氧化剂，抗高血脂和血管生成作用。Ginsenoside Re 会降低 β-amyloid protein (Aβ) 并通过抑制 JNK 和 NF-κB 起到抗炎的作用。
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。	Cell Discov, 2019, 5:2
S1950	Metformin HCl Metformin HCl 降低肝细胞中高血糖症，主要通过抑制肝糖原的产生（肝脏糖异生作用)发挥作用。Metformin可促进单核细胞中的线粒体自噬。Metformin可通过激活JNK/p38 MAPK 信号通路和GAD153来诱导肺癌细胞系的凋亡。	Cell Death Dis, 2020, 8;11(6):427 Int J Oncol, 2020, 56(5):1140-1151 J Biomed Sci, 2020, 27(1):5	Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.
S3940	3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT)是苦马豆和紫檀木心中的活性成分之一，可能对治疗不同类型的恶性血液肿瘤有效。3'-Hydroxypterostilbene 可通过诱导凋亡和自噬，从而有效地抑制人结肠癌细胞的生长，对COLO 205，HCT-116和HT-29 cells的IC50值分别为9.0 µM、40.2 µM和70.9 µM。3'-Hydroxypterostilbene 会抑制 PI3K/Akt/mTOR 信号通路中的p70S6K 和 p38MAPK信号通路，而激活ERK1/2, JNK1/2 信号通路。
S7409	Anisomycin Anisomycin 是一种抗生素，抑制蛋白质合成，也是一种 JNK 激活剂。	Stem Cell Res Ther, 2020, 4;11(1):49 Sci Rep, 2020, 10(1):931 Int J Biol Sci, 2020, 16(8):1303-1323	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。
S9114	Polyphyllin I Polyphyllin I 是从巴黎茶树素中提取的小分子单体，用于治疗传染病和癌症。 Polyphyllin I 抑制U251细胞增殖并诱导其凋亡。 Polyphyllin I 是 JNK 信号传导途径的激活剂，具有潜在的抗神经胶质瘤作用。

目录号	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。SP600125也是一种广谱的serine/threonine kinases抑制剂，包括Aurora kinase A、FLT3和TRKA，对应的IC50值为60 nM、90 nM和70 nM。SP600125可抑制自噬而激活细胞凋亡。	Nat Commun,2020, 8;11(1):2286 Cancer Res,2020, 9 pii: canres J Control Release,2020, 320:201-213	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.
S1574	Doramapimod (BIRB 796) Doramapimod (BIRB 796)是一种泛p38 MAPK抑制剂，在无细胞试验中作用于p38α/β/γ/δ的IC50分别为38 nM，65 nM，200 nM 和520 nM，并且能够与p38α结合，在THP-1细胞中K_d为0.1 nM，比作用于JNK2选择性高330倍，对c-RAF，Fyn 和Lck具有较弱的抑制作用，对ERK-1，SYK，IKK2也有微弱抑制作用。	Nature,2020, 3 Nature,2020, 3 Genome Biol,2020, 21(1):33	Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.
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。	Genome Biol,2020, 21(1):33 Cell Chem Biol,2020, 20;27(2):197-205.e6 J Cell Physiol,2020, 235(3):2792-2799	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.
S6740^New	DB07268 DB07268是有效的选择性JNK1抑制剂，IC50为9 nM，对JNK1的效力是对CHK1、CK2和PLK的70-90倍。
S7794^New	JNK Inhibitor VIII JNK Inhibitor VIII (TCS JNK 6o) 是一种 c-Jun N-terminal kinases 的抑制剂，对JNK-1和JNK-2的IC50值分别为45 nM和160 nM。JNK Inhibitor VIII (TCS JNK 6o) 可抑制JNK-1、JNK-2和JNK-3，对应的Ki值分别为2 nM、4 nM和52 nM。
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。
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。	Nat Biomed Eng,2018, 2(8):578-588
S3901	Astragaloside IV Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems.
S4884	Trans-Zeatin Trans-Zeatina是植物生长激素的成员之一，属于细胞分裂素，可调节细胞分裂、发育和营养加工。
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。	Nat Commun,2020, 11(1):258 Cell Discov,2019, 5:2 Elife,2018, 7	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).
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。	Int J Cancer,2020, 146(9):2563-2575 Cell Discov,2019, 5:2
S3811	Ginsenoside Re Ginsenoside Re (Ginsenoside B2) 是三七的提取物、人参中的主要人参皂苷，属于20(S)-原人参三醇组 (protopanaxatriol group)。它具有多种体外和体内作用，包括血管舒张作用，抗氧化剂，抗高血脂和血管生成作用。Ginsenoside Re 会降低 β-amyloid protein (Aβ) 并通过抑制 JNK 和 NF-κB 起到抗炎的作用。
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。	Cell Discov,2019, 5:2

目录号	产品描述	文献引用	实验数据
S1950	Metformin HCl Metformin HCl 降低肝细胞中高血糖症，主要通过抑制肝糖原的产生（肝脏糖异生作用)发挥作用。Metformin可促进单核细胞中的线粒体自噬。Metformin可通过激活JNK/p38 MAPK 信号通路和GAD153来诱导肺癌细胞系的凋亡。	Cell Death Dis, 2020, 8;11(6):427 Int J Oncol, 2020, 56(5):1140-1151 J Biomed Sci, 2020, 27(1):5	Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.
S3940	3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT)是苦马豆和紫檀木心中的活性成分之一，可能对治疗不同类型的恶性血液肿瘤有效。3'-Hydroxypterostilbene 可通过诱导凋亡和自噬，从而有效地抑制人结肠癌细胞的生长，对COLO 205，HCT-116和HT-29 cells的IC50值分别为9.0 µM、40.2 µM和70.9 µM。3'-Hydroxypterostilbene 会抑制 PI3K/Akt/mTOR 信号通路中的p70S6K 和 p38MAPK信号通路，而激活ERK1/2, JNK1/2 信号通路。
S7409	Anisomycin Anisomycin 是一种抗生素，抑制蛋白质合成，也是一种 JNK 激活剂。	Stem Cell Res Ther, 2020, 4;11(1):49 Sci Rep, 2020, 10(1):931 Int J Biol Sci, 2020, 16(8):1303-1323	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。
S9114	Polyphyllin I Polyphyllin I 是从巴黎茶树素中提取的小分子单体，用于治疗传染病和癌症。 Polyphyllin I 抑制U251细胞增殖并诱导其凋亡。 Polyphyllin I 是 JNK 信号传导途径的激活剂，具有潜在的抗神经胶质瘤作用。