| Identification | Back Directory | [Name]
BMS 195614 | [CAS]
182135-66-6 | [Synonyms]
BMS614
BMS-614
BMS 614
BMS-195614 >=97% (HPLC)
WGLMBRZXZDAQHP-UHFFFAOYSA-N
Benzoic acid, 4-[[[5,6-dihydro-5,5-dimethyl-8-(3-quinolinyl)-2-naphthalenyl]carbonyl]amino]- | [Molecular Formula]
C29H24N2O3 | [MDL Number]
MFCD00952209 | [MOL File]
182135-66-6.mol | [Molecular Weight]
448.51 |
| Chemical Properties | Back Directory | [Boiling point ]
607.3±55.0 °C(Predicted) | [density ]
1.285±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | [form ]
A crystalline solid | [pka]
4.27±0.10(Predicted) | [color ]
White to off-white | [InChIKey]
WGLMBRZXZDAQHP-UHFFFAOYSA-N | [SMILES]
CC1(C)CC=C(C2=CN=C(C=CC=C3)C3=C2)C4=C1C=CC(C(NC5=CC=C(C(O)=O)C=C5)=O)=C4 |
| Hazard Information | Back Directory | [Description]
BMS614 is a neutral retinoic acid receptor (RAR) α-selective antagonist (Ki = 2.5 nM). BMS614 antagonizes agonist-induced coactivator (CoA) recruitment. | [Uses]
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]. | [Definition]
ChEBI: BMS 195614 is a carboxamide resulting from the formal condensation of the carboxy group of 5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-carboxylic acid with the amino group of p-aminobenzoic acid. It is a neutral retinoic acid receptor (RAR) alpha-selective antagonist (Ki = 2.5 nM). It displays no significant effect on nuclear receptor corepressor (NCoR) binding; moderately decreases SMRT binding to RAR. It antagonizes agonist-induced coactivator (CoA) recruitment. It has a role as a retinoic acid receptor alpha antagonist. It is a member of quinolines, a member of benzoic acids and a secondary carboxamide. | [in vivo]
BMS-195614 (2-10 mg/kg, p.o., 7 days) results in minimal or no inhibition of overall spermatogenesis in mice[5].
| [IC 50]
BCL2; IL-6 | [storage]
Store at -20°C | [References]
[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. DOI:10.1016/S1074-5521(99)80084-2
[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. DOI:10.3390/ijms25053037
[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. DOI:10.1016/j.neuint.2016.07.008
[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. DOI:10.1021/ml300365k |
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