Network Version
Tanzisertib Data Sheet
| Product Name: | Tanzisertib |
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|---|---|---|
| CAS No.: | 899805-25-5 | |
| Cat. No.: | HY-15495 | |
| MWt: | 448.44 | |
| Formula: | C21H23F3N6O2 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 33 mg/mL;1M HCl : 100 mg/mL (ultrasonic;adjust pH to 1 with HCl) | |
| Mechanisms: | Target: Inflammation/Immunology | |
| Biological Activity: | ||
| Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC50s of 61/7/6 nM, respectively. IC50 & Target:IC50: 61 nM (JNK1), 7 nM (JNK2), 6 nM (JNK3)[1] In Vitro: Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM)[1]. Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes[2]. Tanzisertib (CC-930) blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis[3]. In Vivo: Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model[1]. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models, but can also induce the regression of pre-existing fibrosis[3]. | ||
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