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Merck
모든 사진(1)

문서

SML1149

Sigma-Aldrich

BMS-189453

≥98% (HPLC)

동의어(들):

(E)-4-[2-(5,6-Dihydro-5,5-dimethyl-8-phenyl-2-naphthalenyl)ethenyl]-benzoic acid, BMS-453, BMS453

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About This Item

실험식(Hill 표기법):
C27H24O2
CAS Number:
Molecular Weight:
380.48
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 10 mg/mL, clear

저장 온도

−20°C

SMILES string

OC(C(C=C1)=CC=C1/C=C/C(C=C2)=CC3=C2C(C)(C)CC=C3C4=CC=CC=C4)=O

InChI

1S/C27H24O2/c1-27(2)17-16-23(21-6-4-3-5-7-21)24-18-20(12-15-25(24)27)9-8-19-10-13-22(14-11-19)26(28)29/h3-16,18H,17H2,1-2H3,(H,28,29)/b9-8+

InChI key

VUODRPPTYLBGFM-CMDGGOBGSA-N

생화학적/생리학적 작용

BMS-189453 is a potent RARβ agonist that acts as an antagonist against RARα and RARγ. BMS-189453 induces RARβ reporter gene expression at sub nanomolar levels, and is 30 fold more potent than all-trans retinoic acid for inducing TGFβ activity in normal breast cells. The compound BMS-189453 does not transactivate RARα or γ transcriptional activity, but binding to those family members induces a strong transrepression of phorbol ester-induced AP-1 activity (IC50 = 0.1 nM in HeLa and MCSF-7). BMS-189453 significantly increases the efficiency of cardiac differentiation of hESCs.
BMS-189453 specifically has sufficient bioavailability in rats and monkeys. BMS-189453 only binds to α, β, and γ retinoid receptors but its activation is unknown. BMS-189453 is found to inhibit the action of collagenase-3 (MMP-13) which catalyses cartilage matrix degradation. Thus, it serves to treat rheumatoid arthritis.

특징 및 장점

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

이미 열람한 고객

BMS-189453, a novel retinoid receptor antagonist, is a potent testicular toxin.
Schulze G E, et al.
Toxicological Sciences, 59(2), 297-308 (2001)
Inhibition of disease progression by a novel retinoid antagonist in animal models of arthritis.
Beehler B C, et al.
The Journal of Rheumatology, 30(2), 355-363 (2003)
Siyu Wu et al.
Journal of cellular physiology, 236(5), 3929-3945 (2020-11-10)
Traumatic injuries of the central nervous system (CNS) are followed by the accumulation of cellular debris including proteins and lipids from myelinated fiber tracts. Insufficient phagocytic clearance of myelin debris influences the pathological process because it induces inflammation and blocks

문서

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

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