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CXL146
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C24H20N2O5
- MW: 416.43
Description
CXL146 is a selective inhibitor of HL60/MX2 cell proliferation by targeting GRP78 overexpression. CXL146 treatment activated the unfolded protein response (UPR). CXL146-induced UPR activation led to a series of downstream events, including extracellular signal-regulated kinase 1/2 and c-Jun N-terminal kinase activation, which contributed to CXL146-induced apoptosis.
More Information
| Parent CAS No. | 2244586-41-0 |
|---|---|
| Chemical Name | Prop-2-ynyl 2-amino-6-(2-methylpyridin-4-yl)-4-(2-oxo-2-(prop-2-ynyloxy)ethyl)-4H-chromene-3-carboxylate |
| SMILES | N1C=CC(C2C=C3C(CC(=O)OCC#C)C(C(OCC#C)=O)=C(N)OC3=CC=2)=CC=1C |
| MFCD | N.A. |
| InChi | InChI=1S/C24H20N2O5/c1-4-10-29-21(27)14-19-18-13-16(17-8-9-26-15(3)12-17)6-7-20(18)31-23(25)22(19)24(28)30-11-5-2/h1-2,6-9,12-13,19H,10-11,14,25H2,3H3 |
| InChiKey | HLNKVUKTJMCVKX-UHFFFAOYSA-N |
| CID | 145954090 |
| Short Description | GRP78 inhibitor |
References
- T Bian et al. Exploring the Structure-Activity Relationship and Mechanism of a Chromene Scaffold (CXL Series) for Its Selective Antiproliferative Activity toward Multidrug-Resistant Cancer Cells. J Med Chem. 2018 Aug 9;61(15):6892-6903.
- T Bian at al. CXL146, a Novel 4 H-Chromene Derivative, Targets GRP78 to Selectively Eliminate Multidrug-Resistant Cancer Cells. Mol Pharmacol. 2020 Jun;97(6):402-408.
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