182135-66-6
Chemical Structure
BMS-195614
Synonym(s): BMS 614
- CAS No.: 182135-66-6
- Formula:C29H24N2O3
- Molecular Weight:448.51
IUPAC Name: 4-(5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-carboxamido)benzoic acid
InChIKey: WGLMBRZXZDAQHP-UHFFFAOYSA-N
SMILES: O=C(O)C1=CC=C(NC(C2=CC=C3C(C)(C)CC=C(C4=CC5=CC=CC=C5N=C4)C3=C2)=O)C=C1
Biological Activity: BMS-195614 (BMS 614) is an orally active neutral RARα-selective antagonist with a Ki of 2.5 nM. BMS-195614 restores the expression of Bcl2. BMS-195614 inhibits the transactivation of NF-κB, AP-1 and PPAR. BMS-195614 downregulates the expression of IL-6 and VEGF. BMS-195614 reduces blue light-induced phototoxicity and inhibits cell migration. BMS-195614 modulates inflammation and angiogenesis[1][2][3][4][5].
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BMS-195614 | 99.5% | BMS-195614 (BMS 614) is an orally active neutral RARα-selective antagonist with a Ki of 2.5 nM. BMS-195614 restores the expression of Bcl2. BMS-195614 inhibits the transactivation of NF-κB, AP-1 and PPAR. BMS-195614 downregulates the expression of IL-6 and VEGF. BMS-195614 reduces blue light-induced phototoxicity and inhibits cell migration. BMS-195614 modulates inflammation and angiogenesis. | ||||||||||||||||||||
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- [1]. Géhin M, et al. Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists. Chem Biol. 1999;6(8):519-529. [Content Brief]
- [2]. Fontaine V, et al. RAR Inhibitors Display Photo-Protective and Anti-Inflammatory Effects in A2E Stimulated RPE Cells In Vitro through Non-Specific Modulation of PPAR or RXR Transactivation. Int J Mol Sci. 2024 Mar 6;25(5):3037. [Content Brief]
- [3]. Kurtys E, et al. The combination of vitamins and omega-3 fatty acids has an enhanced anti-inflammatory effect on microglia. Neurochem Int. 2016 Oct;99:206-214. [Content Brief]
- [4]. Inubushi M, et al. Retinoic acid promotes migration of MC3T3‐E1 osteoblast‐like cells via RARα signaling‐mediated upregulation of profilin‐1 expression. Journal of Osaka Dental University, 2019, 53(2): 149-156.
- [5]. Chung SS, et al. Pharmacological activity of retinoic acid receptor alpha-selective antagonists in vitro and in vivo. ACS Med Chem Lett. 2013 May 9;4(5):446-450. [Content Brief]
Keywords
