Anticancer agent 168 is an orally active retinoic acid receptor (RAR/RXR) beta2 agonist with ameliorating effects on spinal cord injury (SCI)[1].
AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.)Target: RARα agonistCompound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation.Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, compound 4 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients.
LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki 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[1][2].
CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
HX600 is a synthetic agonist for RXR (Retinoid X Receptor) heterodimer complex. HX600 prevents ischemia-induced neuronal damage. HX600 has orally bioactivity[1].
Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene[1].
K-80001 is an RXRα-binder and COX-1/2 inhibitor, with IC50s of with an IC50 of 82.9μM, 3.4μM, 1.2μM for RXRα, COX-1 and COX-2, respectively[1].
16α-Hydroxytrametenolic acid, a natural triterpene, is a potential retinoid X receptor (RXR) selective agonist[1].
Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
(+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ.IC50 value: 3 nM/ 0.6 nM(Ki/IC95)Target: RARγ antagonistMore information can be found in the following patent, Compound 7a.Preparation of disubstituted chalcone oximes having RARγ retinoid receptor antagonist activityBy Tsang, Kwok Yin; Sinha, Santosh; Liu, Xiaoxia; Bhat, Smita; Chandraratna, Roshantha A.From PCT Int. Appl. (2005), WO 2005066115 A2 20050721.
AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions[1][2].
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].
Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist, showing high selectivity over RARγ.
AR7 is a retinoic acid receptor α (RARα) antagonist.
CD2314 is a potent and selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells[1].
Fenretinide is a synthetic retinoid deriverative, binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.
AGN 194310(VTP-194310) is a potent and selective pan-RARs agonist with Kd values of 3/2/5 nM for RARα/β/γ respectively.IC50 value: 3/2/5 nM (Kd for RARα/β/γ) [1][2]Target: RARs agonistin 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 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 whole-body luminescence [3]. Mice were treated with AGN194310, a synthetic retinoid that antagonises the physiological function of the three RAR isotypes (alpha, beta, gamma) but does not interact with RXRs. Analyses of the granulocytic lineage using Gr-1, c-Kit and CD11b antibodies, demonstrated that granulocyte numbers were strikingly increased across haemopoietic compartments in all AGN194310-treated mice. A significant increase in the frequency of progenitor cells containing granulocytes was observed in the bone marrow of mice following treatment with AGN194310 [4].
AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0[1].
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation[1].
ATRA-biotin (Biotin-ATRA-conjugate) is a biotin-conjugated ATRA. ATRA-biotin can be used to track ATRA in cells or a given tissue[1].
Ch55 is a potent synthetic retinoid. Ch55 binds to RAR-α and RAR-β receptors with high affinity. Ch55 displays low affinity for cellular retinoic acid binding protein (CRABP). Ch55 is a potent inducer of the differentiation of HL60 cells with an EC50 of 200 nM. Ch55 can be used for cancer research[1][2].
Bexarotene is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
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[1][2].
AGN 192870 is a RAR neutral antagonist with Kds 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[1].
Oxybenzone-d5 is the deuterium labeled Oxybenzone[1]. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells[2][3][4].
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ[1][2].
MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the expression of iNOS and p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity. MSU-42011 can be used for cancer research[1].