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Formula | C14H8N2O |
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Molecular Weight | 220.23 | CAS No. | 129-56-6 | |
Solubility (25°C)* | In vitro | DMSO | 44 mg/mL (199.79 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | SP600125 (Nsc75890) 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. | |||||||||||
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In vitro | SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50 of 5 μM to 12 μM. [1] However, later studies reveal that SP600125 also suppresses aryl hydrocarbon receptor (AhR) [2], Mps1 [3], and a panel of other serine/threonine kinases, including Aurora kinase A, FLT3, MELK, and TRKA [4]. In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation. [5] In HCT116 cells, SP600125 (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1. [6] |
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In vivo | In mice, SP600125 (15 mg/kg or 30 mg/kg) significantly inhibits lipopolysaccharide (LPS)-induced TNF-α expression and anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. [1] |
Kinase Assay: |
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Cell Assay: |
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Animal Study: |
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Data from [Cancer Res, 2013, 73(20):6346-58]
Data from [Biochim Biophys Acta, 2012, 1823(5), 987-96]
, , Lee lay hoon from National University of Singapore
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Pharmacogenomic profiling of intra-tumor heterogeneity using a large organoid biobank of liver cancer [ Cancer Cell, 2024, 42(4):535-551.e8] | PubMed: 38593780 |
Cancer cell genetics shaping of the tumor microenvironment reveals myeloid cell-centric exploitable vulnerabilities in hepatocellular carcinoma [ Nat Commun, 2024, 15(1):2581] | PubMed: 38519484 |
Phosphorylation of human glioma-associated oncogene 1 on Ser937 regulates Sonic Hedgehog signaling in medulloblastoma [ Nat Commun, 2024, 15(1):987] | PubMed: 38307877 |
Phosphorylation by JNK switches BRD4 functions [ Mol Cell, 2024, S1097-2765(24)00821-9] | PubMed: 39454579 |
Hyperglycemia activates FGFR1 via TLR4/c-Src pathway to induce inflammatory cardiomyopathy in diabetes [ Acta Pharm Sin B, 2024, 14(4):1693-1710] | PubMed: 38572108 |
TRPM2-mediated feed-forward loop promotes chondrocyte damage in osteoarthritis via calcium-cGAS-STING-NF-κB pathway [ J Adv Res, 2024, S2090-1232(24)00499-5] | PubMed: 39505144 |
Cell mechanics regulate the migration and invasion of hepatocellular carcinoma cells via JNK signaling [ Acta Biomater, 2024, S1742-7061(24)00036-9] | PubMed: 38272199 |
Palmitate induces integrated stress response and lipoapoptosis in trophoblasts [ Cell Death Dis, 2024, 15(1):31] | PubMed: 38212315 |
CRLF1 bridges AKT and mTORC2 through SIN1 to inhibit pyroptosis and enhance chemo-resistance in ovarian cancer [ Cell Death Dis, 2024, 15(9):662] | PubMed: 39256356 |
Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728] | PubMed: 39264808 |
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