AGN 194310_229961-45-9_DataSheet_MedChemExpress

P d D Sh

Product Name:

AGN 194310CAS No.:

229961-45-9Cat. No.:

HY-16681

Product Data Sheet MWt:

424.55Formula:

C28H24O2S Purity :>98%

Solubility:

DMSO

Mechanisms:

Biological Activity:

AGN 194310(VTP-194310) is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM Pathways:Others; Target:RAR/RXR

for RAR α/β/γ respectively.

IC50 value: 3/2/5 nM (Kd for RAR α/β/γ) [1][2]

Target: RARs agonist in vitro: A high affinity pan-RAR antagonist (AGN194310, K(d) for binding to RARs = 2-5 nM)inhibited colony formation (by 50%) by all three lines at 16-34 nM, and led to a transient

accumulation of flask-cultured cells in G1 followed by apoptosis. AGN194310 is 12-22 fold more potent than all-trans retinoic acid (ATRA) against cell lines and also more potent in inhibiting the

growth of primary prostate carcinoma cells [2].in vivo:The administration of all trans retinoic acid to VAD mice resulted in a transient reduction in References:

[1]. Johnson AT, et al. Synthesis and biological activity of high-affinity retinoic acid receptor

antagonists. Bioorg Med Chem. 1999 Jul;7(7):1321-38.[2]Hammond LA et al Antagonists of retinoic acid receptors (RARs)are potent growth inhibitors in vivo: The administration of all-trans retinoic acid to VAD mice resulted in a transient reduction in NF-kappaB activity and, conversely, a single dose of the RAR-pan-antagonist, AGN 194310,administered to control mice, led to a marked, transient induction of wh...

[2]. Hammond LA, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors

of prostate carcinoma cells. Br J Cancer. 2001 Aug 3;85(3):453-62.[3]. Austenaa LM, et al. Vitamin A status significantly alters nuclear factor-kappaB activity assessed

by in vivo imaging. FASEB J. 2004 Aug;18(11):1255-7.[4]. Walkley CR, et al. Retinoic acid receptor antagonism in vivo expands the numbers of precursor

cells during granulopoiesis. Leukemia. 2002 Sep;16(9):1763-72.Caution: Not fully tested. For research purposes only

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