Bulk Inquiry
CGP 77675
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C26H29N5O2
- MW: 443.54
Description
CGP 77675 is a potent and selective Src family kinase (SFK) inhibitor that inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src with IC50 values of 5–20 nM and 40 nM, respectively. CGP 77675 effectively suppresses Src-dependent signaling pathways involved in cell proliferation, differentiation, migration, and survival.
In recent stem cell research, dual inhibition of Src and GSK-3 signaling using CGP 77675 and CHIR99021 (Axon 1386) (Alternative 2i; Axon 2130) has been shown to maintain mouse embryonic stem cell (mESC) self-renewal and pluripotency marker expression as efficiently as the conventional 2i (Axon 2128) system consisting of PD0325901 (Axon 1408) and CHIR99021 (Axon 1386). This alternative 2i approach supports serum-free maintenance of mESCs and facilitates derivation of embryonic stem cells from mouse embryos.
Key Features
- Potent and selective, orally active Src family kinase inhibitor
- IC50: 5–20 nM for Src substrate phosphorylation
- IC50: 40 nM for Src autophosphorylation
- Suppresses Src-dependent signaling pathways
- Used in stem cell research to maintain pluripotency
Applications
- Src family kinase signaling research
- Stem cell self-renewal and pluripotency studies
- Alternative 2i stem cell culture systems
- Embryonic stem cell derivation and maintenance
- Cell signaling and developmental biology research
*Promotion: CGP 77675 is also part of Inhibitor Set(s):
| Stem Cell Alternative 2i inhibitor Set (Axon 2130) |
More Information
| Parent CAS No. | 234772-64-6 |
|---|---|
| Chemical Name | 1-(amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol |
| SMILES | N1(CCC2=CC=C(N3C4C(C(C5=CC=CC(OC)=C5)=C3)=C(N)N=CN=4)C=C2)CCC(O)CC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C26H29N5O2/c1-33-22-4-2-3-19(15-22)23-16-31(26-24(23)25(27)28-17-29-26)20-7-5-18(6-8-20)9-12-30-13-10-21(32)11-14-30/h2-8,15-17,21,32H,9-14H2,1H3,(H2,27,28,29) |
| InChiKey | WUPXZZWTHIZICK-UHFFFAOYSA-N |
| CID | 5311381 |
| Short Description | Src inhibitor |
References
- M Missbach et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellular substrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999, 24(5), 437-449.
- T Shimizu et al. Dual inhibition of Src and GSK3 maintains mouse embryonic stem cells, whose differentiation is mechanically regulated by Src signaling. Stem Cells 2012, 30(7), 1394-1404.
- List of publications using CGP 77675 (Axon 2097) purchased from Axon Medchem
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