BMS 493

Names

[ Name ]:
BMS 493

[Synonym ]:
4-[(E)-(5 6-Dihydro-5,5-dimethyl-8-phenylethynyl-2-naphthalenyl)ethenyl]benzoic acid
(E)-4-[2-[2-[[(p-methoxyphenyl)sulfonyl]amino]phenyl]ethenyl]pyridine
(E)-4-(2-(2-(N-(4-METHOXYBENZENESULFONYL)AMINO)PHENYL)VINYL)PYRIDINE
(E)-4-[2-[5,6-dihydro-5,5-dimethyl-8-(2-phenylethynyl)naphthalen-2-yl]ethen-1-yl]benzoic acid
Benzenesulfonamide,4-methoxy-N-[2-[2-(4-pyridinyl)ethenyl]phenyl]-,(E)
(E)-4-[2-[5,6-dihydro-5,5-dimethyl-8-(2-phenylethynyl)naphthalene-2-yl]ethen-1-yl]benzoic acid
Benzenesulfonamide,4-methoxy-N-[2-[(1E)-2-(4-pyridinyl)ethenyl]phenyl]
(E)-4-[2-{2-[N-(4-methoxybenzenesulfonyl)amino]phenyl}ethenyl ]pyridine
(E)-4-[2-[2-[N-[(p-Methoxyphenyl)sulfonyl]amino]phenyl]ethenyl]pyridine
(E)-4-[2-[2-(p-methoxy-benzene-sulfonamide)phenyl]ethenyl]pyridine
BMS-204493

Biological Activity

[Description]:

BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation[1][2].

[Related Catalog]:

Research Areas >> Metabolic Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> RAR/RXR

[Target]

RAR

[In Vitro]

BMS493 (100 nM; 6 days; ALDHhi UCB cells) treatment shows a twofold increase in the number of ALDHhi cells available for transplantation compared with untreated controls. Newly expanded ALDHhi cells shows increased numbers of CD34 and CD133-positive cells, as well as a reduction in CD38 expression, a marker of hematopoietic cell differentiation[1]. Cell Viability Assay[1] Cell Line: ALDHhi UCB cells Concentration: 100 nM Incubation Time: 6 days Result: Showed a twofold increase in the number of ALDHhi cells available for transplantation compared with untreated controls.

[In Vivo]

Intrapancreatic transplantation of cell progeny after expansion of ALDHhi cells with or without BMS493 shows no reduction of hyperglycemia in Streptozotocin-treated NOD/SCID mice. Thus, Umbilical cord blood (UCB)-derived ALDHhi cells effectively lost islet regenerative capacity during ex vivo expansion[1].

[References]

[1]. Elgamal RM, et al. BMS 493 Modulates Retinoic Acid-Induced Differentiation During Expansion of Human Hematopoietic Progenitor Cells for Islet Regeneration. Stem Cells Dev. 2018 Aug 1;27(15):1062-1075.

[2]. Yu Z, et al. Apoptosis induced by atRA in MEPM cells is mediated through activation of caspase and RAR. Toxicol Sci. 2006 Feb;89(2):504-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₂₄O₂

[ Molecular Weight ]:
404.50000

[ Exact Mass ]:
404.17800

[ PSA ]:
37.30000

[ LogP ]:
6.67160

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Statements ]:
H413

[ RIDADR ]:
NONH for all modes of transport

Articles

Trichostatin A reduces GnRH mRNA expression with a concomitant increase in retinaldehyde dehydrogenase in GnRH-producing neurons.

Mol. Cell. Endocrinol. 413 , 113-9, (2015)

Trichostatin A (TSA) is a selective inhibitor of mammalian histone deacetylase and is widely used to modify the ability of DNA transcription factors to bind DNA within chromatin by interfering with hi...

Retinoic acid signalling regulates the development of tonotopically patterned hair cells in the chicken cochlea.

Nat. Commun. 5 , 3840, (2014)

Precise frequency discrimination is a hallmark of auditory function in birds and mammals and is required for distinguishing similar sounding words, like 'bat,' 'cat' and 'hat.' In the cochlea, tuning ...

Retinoic acid receptor alpha is associated with tamoxifen resistance in breast cancer.

Nat. Commun. 4 , 2175, (2013)

About one-third of oestrogen receptor alpha-positive breast cancer patients treated with tamoxifen relapse. Here we identify the nuclear receptor retinoic acid receptor alpha as a marker of tamoxifen ...