JNK inhibitor 8
JNK-IN-8
CAS: 1410880-22-6
Molecular Formula: C29H29N7O2
JNK inhibitor 8 - Names and Identifiers
JNK inhibitor 8 - Physico-chemical Properties
| Molecular Formula | C29H29N7O2 |
| Molar Mass | 507.59 |
| Density | 1.283±0.06 g/cm3(Predicted) |
| Appearance | powder |
| Color | white to beige |
| pKa | 13.34±0.70(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | JNK-IN-8 inhibited c-Jun phosphorylation in HeLa and A375 cells with EC50 of 486 nM and 338 nM, respectively. JNK-IN-8 combined with IRAK1,PIK3C3,PIP4K2C and PIP5K3 significantly improved the selectivity and elimination rate. JNK-IN-8 inhibition of JNK2 requires the involvement of cys116. JNK-IN-8 (10 mM) inhibited IL-1R of IL-1β stimulated phosphorylation in c-Jun of cells, an established JNKs mechanism. JNK-IN-8 covalently binds to the JNK subtype, causing a slight delay in electrophoretic migration of the JNK subtype. JNK-IN-8 was found to be able to inhibit JNK kinase through the extensive kinase selection properties in the acrylamide kinase inhibitor expression library, using the kinomscan method to function based on the structure of imatinib. JNK-IN-8 has a clear regioselectivity for 1, 4-bisaniline and 1, 3-aminobenzoic acid structures relative to imatinib, and uses N,N-dimethylbutenylacetamide to bind to the covalent target cys154. In JNK-IN-8, L-shaped type I binding conformation was adopted, and Cys 154 located at the edge of ATP binding site was accessed. JNK-IN-8 inhibited c-Jun phosphorylation in HeLa and A375 cells with EC50 of 486 nM and 338 nM, respectively. JNK-IN-8 combined with IRAK1,PIK3C3,PIP4K2C and PIP5K3 significantly improved the selectivity and elimination rate. JNK-IN-8 inhibition of JNK2 requires the involvement of cys116. JNK-IN-8 (10 mM) inhibited IL-1R of IL-1β stimulated phosphorylation in c-Jun of cells, an established JNKs mechanism. JNK-IN-8 covalently binds to the JNK subtype, causing a slight delay in electrophoretic migration of the JNK subtype. JNK-IN-8 was found to be able to inhibit JNK kinase through the extensive kinase selection properties in the acrylamide kinase inhibitor expression library, using the kinomscan method to function based on the structure of imatinib. JNK-IN-8 has a clear regioselectivity for 1, 4-bisaniline and 1, 3-aminobenzoic acid structures relative to imatinib, and uses N,N-dimethylbutenylacetamide to bind to the covalent target cys154. In JNK-IN-8, L-shaped type I binding conformation was adopted, and Cys 154 located at the edge of ATP binding site was accessed. |
JNK inhibitor 8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.97 ml | 9.85 ml | 19.701 ml |
| 5 mM | 0.394 ml | 1.97 ml | 3.94 ml |
| 10 mM | 0.197 ml | 0.985 ml | 1.97 ml |
| 5 mM | 0.039 ml | 0.197 ml | 0.394 ml |
Last Update：2024-01-02 23:10:35
JNK inhibitor 8 - Reference Information
| biological activity | JNK-IN-8 is the first irreversible JNK inhibitor to act on JNK1, JNK2 and JNK4,IC50 is 4.7 nM, 18.7 nM and 1 nM respectively, which is more than 10 times higher than that on MNK2 and Fms, and has no inhibitory effect on c-Kit, Met and PDGFR. JNK-IN-8 (JNK Inhibitor XVI) is the first irreversible JNK inhibitor, which acts on JNK1,JNK2 and JNK3. in A375 cell line, IC50 is 4.7 nM,18.7 nM and 1 nM respectively, which is more than 10 times higher than that on MNK2 and Fms, and has no inhibitory effect on c-Kit, Met and PDGFRβ. |
| in vitro study | JNK-IN-8 inhibit phosphorylation of c-Jun in HeLa and A375 cells with EC50 of 486 nM and 338 nM respectively. JNK-IN-8 combined with IRAK1,PIK3C3,PIP4K2C and PIP5K3 significantly improved selectivity and elimination rate. JNK-IN-8 inhibition of JNK2 requires the participation of Cys116. JNK-IN-8 (10 mM) inhibits IL-1β-stimulated c-Jun phosphorylation in IL-1R cells and is an established JNKs mechanism. JNK-IN-8 covalently binds to JNK subtypes, causing a slight delay in electrophoretic migration of JNK subtypes. JNK-IN-8 have been found to be able to inhibit JNK kinase through a wide range of kinase selection properties in the expression library of acrylamide kinase inhibitors, using KinomeScan methods based on the structure of the imatinib. Relative to imatinib,JNK-IN-8 has a significant regioselectivity of 1,4-bisaniline and 1,3-aminobenzoic acid structure, and N,N-dimethylbutene acetamide is used to bind the covalent target Cys154. The JNK-IN-8 adopts L-shaped type I binding conformation and accesses Cys 154 located at the edge of ATP binding site. JNK-IN-8 inhibited phosphorylation of c-Jun in HeLa and A375 cells with EC50 of 486 nM and 338 nM respectively. JNK-IN-8 combined with IRAK1,PIK3C3,PIP4K2C and PIP5K3 significantly improved selectivity and elimination rate. JNK-IN-8 inhibition of JNK2 requires the participation of Cys116. JNK-IN-8 (10 mM) inhibits IL-1β-stimulated c-Jun phosphorylation in IL-1R cells and is an established JNKs mechanism. JNK-IN-8 covalently binds to JNK subtypes, causing a slight delay in electrophoretic migration of JNK subtypes. JNK-IN-8 have been found to be able to inhibit JNK kinase through a wide range of kinase selection properties in the expression library of acrylamide kinase inhibitors, using KinomeScan methods based on the structure of the imatinib. Relative to imatinib, the JNK-IN-8 has significant 1,4-bisaniline and 1,3-aminobenzoic acid structure regioselectivity, and N,N-dimethylbuteneacetamide is used to bind the covalent target Cys154. The JNK-IN-8 adopts L-shaped type I binding conformation and accesses Cys 154 located at the edge of ATP binding site. |
| Features | JNK-IN-8 and JNK-IN-7 are very similar in structure, but the former is a specific covalent inhibitor of JNKs. |
| target | TargetValue jnk3 (A375 cells) 1 nmjnk1 (A375 cells) 4.7 nmjnk2 (A375 cells) 18.7 nmkit (V559D,T670I) (A375 cells) 56 nmkit (V559D) (A375 cells) 92 nm |
| Target | Value |
| JNK3 (A375 cells) | 1 nM |
| JNK1 (A375 cells) | 4.7 nM |
| JNK2 (A375 cells) | 18.7 nM |
| Kit (V559D,T670I) (A375 cells) | 56 nM |
| Kit (V559D) (A375 cells) | 92 nM |
Last Update：2024-04-09 21:54:55
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Product Name: JNK-IN-8 Visit Supplier Webpage Request for quotationCAS: 1410880-22-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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