RAR/RXR Antagonist

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.

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.

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

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).

AGN 205728 is a potent and selective RARγ antagonist with K_i/IC₉₅ values of 3 nM/0.6 nM; no inhibiton on RARα and RARβ. AGN 205728 can inhibit abnormal proliferation of leukemia cells.

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

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.

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.

RARα antagonist 1 (compound 21) is an orally active and selective retinoic acid receptor α(RARα) antagonist, with the IC₅₀ of 4.6nM.

ER 50891 quarterhydrate is a RARα antagonist. ER 50891 can significantly antagonize the inhibitory effect of all-trans retinoic acid (ATRA) on the total cell metabolic activity and proliferation of MC3T3-E1 preosteoblasts. ER 50891 rescues ATRA-inhibited osteocalcin (OCN) expression and extracellular matrix mineralization, and suppresses alkaline phosphatase (ALP) activity synergistically. ER 50891 can be used for the study of osteoporosis related to ATRA-induced inhibition of osteoblastogenesis.

AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds 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.

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.

AGN 193109-d₇ is the deuterium labeled AGN 193109. AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with Kds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.

RXR antagonist 2 (compound 6b) is a potent antagonist of RXR with a K_i and K_d of 0.391 and 0.281 μM. RXR antagonist 2 has the potential for the research of RXR related diseases.

β-Apo-13-carotenone (Standard) is the analytical standard of β-Apo-13-carotenone (HY-101953). This product is intended for research and analytical applications. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.

PA452 (Standard) is the analytical standard of PA452 (HY-108522). This product is intended for research and analytical applications. PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development.

AR7 (Standard) is the analytical standard of AR7 (HY-101106). This product is intended for research and analytical applications. AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.

RXR antagonist 6 (Compound 34) is a selective partial retinoid X receptor (RXR) antagonist. RXR antagonist 6 shows no agonistic activity for any of the human RXRα/β/γ subtypes but it can strongly inhibit the receptor activation induced by full agonists of RXR (such as Bezafibrate (HY-B0637)) with an IC₅₀ of 2.7 μM. RXR antagonist 6 can enhance PMA (HY-18739)-induced THP-1 cell differentiation. RXR antagonist 6 can be used for the research of cancer, metabolic and neurological disease, such as lymphoma.

MM11253 (Standard) is the analytical standard of MM11253 (HY-108530). This product is intended for research and analytical applications. 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.

BMS-185411 is a selective retinoic acid receptor alpha (RARα) antagonist, with an IC₅₀ value of 140 nM.