JNK
Signaling Pathway Map
Research Area
Inhibitory Selectivity
JNK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1460 |
SP600125SP600125 is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A，FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
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.
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| S1574 |
Doramapimod (BIRB 796)Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2. |
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.
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| S4901 |
JNK-IN-8JNK-IN-8 is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line. |
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. |
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| S6740New |
DB07268DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK. |
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| S7794New |
JNK Inhibitor VIIIJNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively. |
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| S6711New |
IQ-1SIQ-1S is a JNK3 inhibitor with Kd values of 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively. |
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| S6730New |
CC-401 HydrochlorideCC-401 is a potent inhibitor of JNK with at least 40-fold selectivity against other related kinases. |
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| S8867New |
Bentamapimod (AS602801)Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively. |
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| S3901 |
Astragaloside IVAstragaloside 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. Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. |
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| S4884 |
Trans-ZeatinTrans-Zeatina is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently. |
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| S7508 |
JNK Inhibitor IXJNK inhibitor IX is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively. |
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).
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| S8490 |
Tanzisertib(CC-930)CC-930 is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively. |
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| S3811 |
Ginsenoside ReGinsenoside Re (Ginsenoside B2), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. |
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| S8201 |
BI-78D3BI-78D3 is a competitive JNK inhibitor with IC50 of 280 nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K. |
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| S1950 |
Metformin HClMetformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
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.
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| S3940 |
3'-Hydroxypterostilbene3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies. 3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways. |
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| S7409 |
AnisomycinAnisomycin is an antibiotic, which inhibits protein synthesis, and also act as a JNK activator. |
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 |
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| S7637 |
DTP3DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits cancer-selective NF-κB survival pathway. |
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| S9114 |
Polyphyllin IPolyphyllin I, a small molecular monomer extracted from Rhizoma of Paris polyphyllin, is used in the treatment of infectious disease and cancer. Polyphyllin I inhibits proliferation and induces apoptotic cell death in U251 cells. Polyphyllin I is an activator of the JNK signaling pathway with a potential anti-glioma effect. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1460 |
SP600125SP600125 is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A，FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
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) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2. |
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-8JNK-IN-8 is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line. |
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. |
|
| S6740New |
DB07268DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK. |
||
| S7794New |
JNK Inhibitor VIIIJNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively. |
||
| S6711New |
IQ-1SIQ-1S is a JNK3 inhibitor with Kd values of 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively. |
||
| S6730New |
CC-401 HydrochlorideCC-401 is a potent inhibitor of JNK with at least 40-fold selectivity against other related kinases. |
||
| S8867New |
Bentamapimod (AS602801)Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively. |
||
| S3901 |
Astragaloside IVAstragaloside 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. Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. |
||
| S4884 |
Trans-ZeatinTrans-Zeatina is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently. |
||
| S7508 |
JNK Inhibitor IXJNK inhibitor IX is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively. |
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 is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively. |
||
| S3811 |
Ginsenoside ReGinsenoside Re (Ginsenoside B2), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. |
||
| S8201 |
BI-78D3BI-78D3 is a competitive JNK inhibitor with IC50 of 280 nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1950 |
Metformin HClMetformin HCl decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
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'-Hydroxypterostilbene3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies. 3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways. |
||
| S7409 |
AnisomycinAnisomycin is an antibiotic, which inhibits protein synthesis, and also act as a JNK activator. |
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 |
DTP3DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits cancer-selective NF-κB survival pathway. |
||
| S9114 |
Polyphyllin IPolyphyllin I, a small molecular monomer extracted from Rhizoma of Paris polyphyllin, is used in the treatment of infectious disease and cancer. Polyphyllin I inhibits proliferation and induces apoptotic cell death in U251 cells. Polyphyllin I is an activator of the JNK signaling pathway with a potential anti-glioma effect. |
