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CC-930
- Tanzisertib
Axon 2634
CAS:
899805-25-5
- Optical Purity: Optically pure
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C21H23F3N6O2
- MW: 448.44
Description
CC-930 (Tanzisertib) is a potent, selective, and orally active anti-fibrotic JNK inhibitor with IC50 values of 61 nM, 7 nM, and 60 nM against JNK1, JNK2, and JNK3, respectively. It demonstrates a high degree of selectivity for JNKs over a massive panel of 240 non-MAP kinases. It blocks c-Jun phosphorylation, reducing scarring and collagen deposition in lung and skin fibrosis models. Tanzisertib showed therapeutic potential to treat idiopathic pulmonary fibrosis (IPF).
JNK pharmacology is relevant to fibrosis, idiopathic pulmonary fibrosis, IPF; CC-930 supports mechanistic studies of JNK, MAPK, c-Jun N-terminal kinase in biochemical, cellular and disease-model assays.
Key Features
- Potent JNK inhibitor, targeting JNK3 (6 nM), JNK2 (7 nM), and JNK1 (61 nM)
- Highly selective over 240 non-MAP kinases
- Modulates JNK-dependent signaling or biological activity
- Blocks critical scarring pathways to combat tissue degeneration in lung disease models
Applications
- JNK pharmacology and target-validation studies
- JNK pathway and signaling assays
- Disease-model research related to fibrosis, idiopathic pulmonary fibrosis
- Kinase signaling, phosphorylation and pathway-inhibition assays
More Information
| Parent CAS No. | 899805-25-5 |
|---|---|
| Chemical Name | trans-4-(9-((S)-tetrahydrofuran-3-yl)-8-(2,4,6-trifluorophenylamino)-9H-purin-2-ylamino)cyclohexanol |
| SMILES | [C@@H]1(O)CC[C@@H](NC2=NC=C3C(=N2)N([C@H]2CCOC2)C(NC2=C(F)C=C(F)C=C2F)=N3)CC1 |&1:0,4,13,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H23F3N6O2/c22-11-7-15(23)18(16(24)8-11)28-21-27-17-9-25-20(26-12-1-3-14(31)4-2-12)29-19(17)30(21)13-5-6-32-10-13/h7-9,12-14,31H,1-6,10H2,(H,27,28)(H,25,26,29)/t12?,13-,14?/m0/s1 |
| InChiKey | IBGLGMOPHJQDJB-MOKVOYLWSA-N |
| CID | 11597537 |
| Short Description | JNK inhibitor |
CC-930 (Tanzisertib)
selective JNK1/2/3 inhibitor
CC-930
Tanzisertib
CC930
p38α
JNK1/2/3
MAPK
JNK
JNK1
JNK2
JNK3
c-Jun N-terminal kinase
Inhibitor
MAPK/ERK signaling
JNK pharmacology
JNK signaling assays
fibrosis and idiopathic pulmonary fibrosis
kinase signaling and phosphorylation
fibrosis
kinase signaling
receptor selectivity
signal transduction
drug discovery
CAS 899805-25-5
Axon Medchem
Axon 2634
Supplier
Vendor
References
- VP Krenitsky et al. Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8.
- SA Antoniu. Discontinued drugs for pulmonary, allergy, gastrointestinal, arthritis (2012). Expert Opin Investig Drugs. 2013 Nov;22(11):1453-64.
- N Reich et al. Jun N-terminal kinase as a potential molecular target for prevention and treatment of dermal fibrosis. Ann Rheum Dis. 2012 May;71(5):737-45.
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