rarβ

Compound 21, an orally active and selective RARα antagonist, exhibits a potent inhibition of the retinoic acid receptor α with an IC50 of 4.6 nM [1].

PROTAC RAR Degrader-1, an RAR degrader, consists of a cIAP1 ligand binding group, a linker, and an RAR ligand binding group. It achieves maximal RAR degradation at a concentration of 30 μM in HT1080 cells. Degradation inducers that utilize cIAP1 are known as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

Retinoic acid (Tretinoin), a metabolite of vitamin A, is a natural agonist of the retinoic acid receptor RAR and inhibits RARα/β/γ (IC50=14 nM). Retinoic acid induces cellular differentiation, reduces cellular proliferation, and inhibits tumorigenesis.

Adapalene (CD271) is a dual RAR and RXR agonist, utilized in the treatment of skin conditions.

Amsilarotene (TAC101) inhibits the phosphorylation of retinoblastoma gene product (RB) and increases the presence of 2 cyclin-dependent kinases (CDK) inhibitors resulting in cell cycle arrest. This agent also causes a cytotoxic decline in the thymidylate synthase and cyclin A expression.

AGN 192870 is a potent retinoic acid receptor (RAR) antagonist.AGN 192870 can be used to study cell growth arrest, differentiation and apoptosis.

Trifarotene (CD5789) is a potent and selective RARγ agonist with 65-fold and 16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM).

MM 11253 is a RARγ antagonist with IC50 of 44nM.

Adapalene (CD 271; Differin) sodium salt is a synthetic retinoid and a Retinoic acid receptor agonist.

AGN 193109, a retinoid analog, is a potent and specific antagonist of RARs (Kds: 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ).

Ro 41-5253 is an orally active RARα antagonist, ligand and partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ. It exhibits antitumor activity, inhibits proliferation and induces apoptosis in MCF-7 and ZR-75.1 estrogen receptor positive breast cancer cells.

BMS453 (BMS-189453), a synthetic retinoid, is a potent and selective agonist of RARβ and a potent testicular toxin. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.

TTNPB (Ro 13-7410,AGN-191183), a potent RAR agonist, inhibits binding of [3H]tRA of human RARα (IC50: 5.1 nM), β (IC50: 4.5 nM), and γ (IC50: 9.3 nM), respectively.

CD2665 is an orally active antagonist of retinoic acid receptor (RAR). For RARγ and RARβ, the Kis are 110 nM and 306 nM.

AGN 205728 is a potent and selective RARγ antagonist (Ki: 3 nM; IC95: 0.6 nM) and has no inhibition on RARα and RARβ.

6-Hydroxy Bexarotene, an oxidative metabolite of bexarotene, serves as a high-affinity ligand for retinoid X receptors (RXRs), specifically binding to RXRα, RXRβ, and RXRγ, as well as to the retinoic acid receptor α (RARα) with dissociation constants (Kds) of 3.46, 4.21, 4.83, and 8.17 μM, respectively. It demonstrates selective activation of RXRα, RXRβ, and RXRγ over RARα, RARβ, and RARγ in vitro, with half-maximal effective concentrations (EC50s) of 398, 356, 420, 4,414, 2,121, and 2,043 nM, respectively.

CD564 is a novel selective inhibitor of RARβ/γ.

CD2314 is a potent and subtype-selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells [1].

AGN 196996 is a potent and selective inhibitor of RARα (Ki: 2 nM).AGN 196996 has very low affinity for RARβ and RARγ, with a Ki of 1087 nM and 8523 nM, respectively.

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 agonist Compound 4(AGN-195183) inhibited the growt

BMS641 (BMS-209641) is a selective and potent RARβ agonist.BMS641 has a high affinity for RARβ and synergistically activates RARβ and RARgamma to induce cellular maturation into specialized neuronal subtypes.

AGN 194310 (VTP-194310) is retinioic acid receptors (RARs) pan-antagonist. The Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively[1][2].

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.

Methyl 13-cis-4-Oxoretinoate (13-cis-4-Oxo-retinoic acid Methyl Ester) is a retinoic acid metabolite in neuroblastoma.