RAR/RXR Antagonist

RARγ antagonist 1 (Compound in claim 4, P20) is a RARγ antagonist. RARγ antagonist 1 can be used for the researches of inflammation and immunology.

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.

HX531 is an orally active RXR antagonist with an IC₅₀ of 18 nM. HX531 upregulates the p53-p21Cip1 pathway. HX531 abrogates the anti-apoptotic effect of t-RA. HX531 exerts anti-obesity, anti-diabetic and anti-melanoma activities.

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

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.

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.

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.

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

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.

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.

BMS-195614 (BMS 614) is an orally active neutral RARα-selective antagonist with a K_i of 2.5 nM. BMS-195614 restores the expression of Bcl2. BMS-195614 inhibits the transactivation of NF-κB, AP-1 and PPAR. BMS-195614 downregulates the expression of IL-6 and VEGF. BMS-195614 reduces blue light-induced phototoxicity and inhibits cell migration. BMS-195614 modulates inflammation and angiogenesis.

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

ER 50891 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 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).

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.

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.

K-8012 is a Sulindac (HY-B0008) analog and RXRα antagonist with an IC₅₀ of 9.2 µM. K-8012 inhibits the activation of AKT. K-8012 induces Apoptosis, redirecting the TNFα signaling pathway from survival to death. K-8012 exerts anticancer activity against lung cancer, prostate cancer, and breast cancer. K-8012 can be used in research related to lung cancer, prostate cancer, breast cancer, and hepatocellular carcinoma.

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.