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SB 590885
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C27H27N5O2
- MW: 453.54
Description
SB 590885 is a potent and selective inhibitor of B-Raf kinase. It suppresses RAF/MEK/ERK pathway signaling and has also been used in stem-cell culture protocols where MAPK pathway modulation supports pluripotency. SB590885 maintains OCT4-ΔPE-GFP reporter activity and pluripotency gene expression in human ESCs after removal of exogenous KLF2 and NANOG expression, preserving the best colony morphology and proliferation.
BRAF is a key MAPK pathway kinase that drives proliferation and survival downstream of RAS signaling and oncogenic BRAF mutations. SB 590885 is useful for BRAF selectivity studies, MAPK pathway inhibition and pluripotent stem-cell signaling research.
Key Features
- Potent BRAF kinase inhibitor
- Reported Kd: 0.3 nM for BRAF
- Selective over several kinases including p38α, GSK3β and Lck in reported assays
- Inhibits RAF/MEK/ERK signaling
Applications
- BRAF and MAPK pathway pharmacology
- Oncogenic kinase signaling studies
- Stem-cell pluripotency culture research
- Kinase selectivity and pathway inhibition assays
SB 590885 is frequently used in a combination of five compounds, including inhibitors of MEK, GSK-3β, BRAF, ROCK, and SRC, which support the expansion of viable OCT4-ΔPE-GFP+ human pluripotent cells after exogenous transcription factor expression has been removed:
| Axon 2504 | SB 590885 | BRAF inhibitor |
| Axon 2511 | IM 12 | GSK-3β inhibitor |
| Axon 1408 | PD 0325901 | MEK inhibitor |
| Axon 1683 | Y 27632 | ROCK inhibitor |
| Axon 2381 | WH4-023 | Lck/Src inhibitor |
(alternatively, CHIR99021 (Axon 1386) could be used as GSK-3β inhibitor)
Naive Stem Cell 5i inhibitor Set is commercially available (Axon 5011)
More Information
| Parent CAS No. | 405554-55-4 |
|---|---|
| Chemical Name | 5-(2-(4-(2-(dimethylamino)ethoxy)phenyl)-5-(pyridin-4-yl)-1H-imidazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime |
| SMILES | C1(=N/O)C2=C(C=C(C3=C(C4C=CN=CC=4)NC(C4=CC=C(OCCN(C)C)C=C4)=N3)C=C2)CC1 |
| MFCD | MFCD16038645 |
| InChi | InChI=1S/C27H27N5O2/c1-32(2)15-16-34-22-7-3-19(4-8-22)27-29-25(18-11-13-28-14-12-18)26(30-27)21-5-9-23-20(17-21)6-10-24(23)31-33/h3-5,7-9,11-14,17,33H,6,10,15-16H2,1-2H3,(H,29,30)/b31-24+ |
| InChiKey | MLSAQOINCGAULQ-QFMPWRQOSA-N |
| CID | 135421339 |
| Short Description | BRAF inhibitor |
References
- T.W. Theunissen et al. Systematic identification of culture conditions for induction and maintenance of naive human pluripotency. Cell Stem Cell. 2014 Oct 2;15(4):471-87.
- A.K. Takle et al. The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81.
- A.J. King et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer Res. 2006 Dec 1;66(23):11100-5.
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