rarγ

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.

Tamibarotene (Amnolake) is an orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity.

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

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

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

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

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.

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

LY2955303 is an effective and selective antagonist of retinoic acid receptor gamma (RARγ, Ki = 1.09 nM).

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).

BMS270394 is a RARγ agonist used in the study of breast cancer and dermatologic diseases.

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.

CD437 (AHPN) is a specifc Retinoic Acid Receptor γ (RARγ) agonist.

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

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.

AGN 205327 is a potent synthetic RAR agonist with EC50 values of 3766, 734, and 32 nM for RARα, RARβ, and RARγ respectively, without inhibiting RXR. [IC50 value: 3766 734 32 nM for RARα β γ] [Target: RAR agonist]

CD 1530 is a selective and potent RARγ agonist (Kd:150 nM) with potential anticancer activity, shows insecticidal activity against Cryptobacterium hidradii nematodes, and can be used to study oral carcinogenesis.

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.

NRX-204647 is a RARγ-selective inverse agonist.

BMS961 is a potent and selective retinoic acid receptor gamma (RARγ) agonist (IC50: 30 nM).

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

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

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

AGN 194310 (VTP-194310) is a pan-antagonist for retinoic acid receptors (RARs), with Kd values of 3 nM, 2 nM, and 5 nM for RARα, RARβ, and 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), showing higher affinity for RARβ. It is highly selective over RARγ, RXRα, RXRβ, and RXRγ. LE135 also acts as a potent TRPV1 and TRPA1 receptor 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.