BMS 195614

Product NameBMS 195614
CAS182135-66-6
MFC29H24N2O3
MW448.51
EINECS
MOL File182135-66-6.mol

Chemical Properties

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

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

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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