RAR/RXR Antagonist

RAR/RXR Antagonists (27):

Cat. No.	Product Name	Effect	Purity

HY-U00449

AGN 193109	Antagonist	98.50%
AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with K_ds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively. AGN 193109 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AGN 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.

HY-101106

AR7	Antagonist	99.38%
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.

HY-108521

HX531	Antagonist	99.87%
HX531 is an effective RXR antagonist with oral activity, with an IC₅₀ of 18 nM, with activity against black melanoma. HC531 can eliminate the anti-apoptotic effects of all-trans-retinoic acid (t-RA) and exerts anti-obesity and anti-diabetic effects through leptin-dependent pathways and the p53-p21Cip1 pathway, resulting in G0/G1 cell cycle arrest.

HY-16681

AGN 194310	Antagonist	98.07%
AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with K_d values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively. AGN 194310 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-107765

LY2955303	Antagonist	98.60%
LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a K_i of 1.09 nM.

HY-107436

LE135	Antagonist	99.03%
LE135 is a potent RAR antagonist that binds selectively to RARα (K_i of 1.4 μM) and RARβ (K_i of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC₅₀s of 2.5?μM and 20?μM, respectively.

HY-108522

PA452	Antagonist	≥99.0%
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.

HY-116248

Ro 41-5253	Antagonist	98.44%
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity.

HY-101953

β-Apo-13-carotenone	Antagonist
β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.

HY-108530

MM11253	Antagonist	98.64%
MM11253 is a potent and selective RARγ antagonist with an IC₅₀ of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists.

HY-101259

BMS-195614	Antagonist	99.5%
BMS-195614 (BMS 614) is a neutral RARα-selective antagonist with a K_i of 2.5 nM.

HY-107437

CD2665	Antagonist	99.91%
CD2665 is an orally active and selective RAR-β,γ antagonist, with K_d values of 306 nM, 110 nM for RAR-β and RAR-γ, repectively.

HY-16682

AGN 196996	Antagonist	99.37%
AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).

HY-108531A

ER 50891 quarterhydrate	Antagonist	99.86%
ER 50891 quarterhydrate is a potent antagonist of retinoic acid receptor α(RARα). ER 50891 quarterhydrate significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis.

HY-105689

AGN 192870	Antagonist	98.10%
AGN 192870 is a RAR neutral antagonist with K_ds of 147, 33, and 42 nM for RARα, RARβ, and RARγ, respectively. AGN 192870 shows IC₅₀s of 87 and 32 nM for RARαand RARγ, respectively. AGN 192870 shows RARβ partial agonism. AGN 192870 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-163436

F44-A13	Antagonist
F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC₅₀ value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.

HY-108531

ER 50891	Antagonist	99.86%
ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). ER-50891 significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis.

HY-16683

AGN 205728	Antagonist
AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.

HY-149085

XS-060	Antagonist	98.67%
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome.

HY-U00449G

AGN 193109 (GMP)	Antagonist
AGN 193109 (GMP) is AGN 193109 (HY-U00449) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AGN 193109 is a specific and highly effective retinoic acid receptor (RAR) antagonist. AGN 193109 (GMP) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AGN 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.

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