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Nuclear Receptor/Transcription Factor

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Cat. No. Product Name Field of Application Chemical Structure
DC72132 SR12418 SR12418 is a REV-ERB-specific synthetic ligand with IC50s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research.
DC72233 Norgestrienone Norgestrienone, progestin or synthetic progestin, is a progestin receptor agonist. Norgestrienone is often used as a progestational compound in birth control pills and can be used in combination with ethinyl estradiol.
DC72268 Larsucosterol (trimethylamine) Larsucosterol (DUR-928) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
DC72414 Steppogenin Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.
DC72415 Oct4 inducer-1 Featured Oct4 inducer-1 (compound OAC-3) is a potent Oct4 activator. Oct4 inducer-1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. Oct4 inducer-1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.
DC72561 DS69910557 Featured DS69910557 is a potent, selective and orally activehuman parathyroid hormone receptor 1 (hPTHR1) antagonist. DS69910557 has antagonistic activity for PTHR1 with an IC50 value of 0.08 μM.
DC72562 MeTC7 MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects.
DC72682 Palazestrant Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant in combination with a HER2 inhibitor, works on ER+/HER2+ cancer.
DC72683 Izumerogant Izumerogant is an inverse agonist of retinoid-related orphan receptor-gamma (RORγ). Izumerogant (compound 123) also potently inhibits IL-17A, IL-17F and IFN-γ activity with IC50s <50 nM.
DC72758 Gumelutamide Gumelutamide is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide is an androgen antagonist.
DC72759 RLA-5331 RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castrated tolerant prostate cancer (mCRPC) cell line and can stably exist in vivo.
DC72796 dextrothyroxine sodium Dextrothyroxine (D-T4) sodium, a sodium salt of D-T4, is a laevorotatory isomer of thyroxine used for thyroid related studies.
DC72797 Prepro-TRH-(160-169) Prepro-TRH-(160-169) is one of the connecting peptides of thyrotropin-releasing hormone prohormone (pro-TRH), potentiates TRH-induced thyrotropin (TSH) release.
DC72798 2MD 2MD is an orally active vitamin D analog. 2MD stimulates periosteal bone formation and decreases trabecular bone resorption. Thus 2MD restores trabecular and cortical bone mass and strength. 2MD also regulates intraocular pressure (IOP)-relative genes and reduces IOP in non-human primates.
DC72867 Belzutifan Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay). PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells. PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.
DC72900 HP210 HP210 is a selective glucocorticoid receptor modulator (SGRM). HP210 can inhibit the mRNA expression of IL-1β and IL-6. HP210 has the potential to study inflammation-related diseases.
DC72912 IK-930 Featured IK930 (compound I-32) is a potent and orally active TEAD inhibitor with an EC50 value of <0.1 µM.
DC73800 ET516 ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expre
DC73801 Faznolutamide Faznolutamide is a potent, selective androgen receptor (AR) antagonist.
DC73802 JJ-450 JJ-450 is a novel analogue of IMTPPE and direct and specific inhibitor of androgen receptor (AR) transcriptional activity, blocks AR recruitment to androgen-responsive elements and suppresses AR target gene expression.
DC73803 M17-B15 M17-B15 is a potent, specific small molecule inhibitor of androgen receptor (AR) targeting the dimer interface pocket (DIP), inhibits AR transcriptional inhibition with IC50 of 0.03 uM.
DC73804 MK-0773 Featured MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.
DC73805 SC428 SC428 (SC-428) is a small molecule androgen receptor (AR) signaling inhibitor, directly binds to the AR N-terminal domain (NTD) and exhibits pan-AR inhibitory effect.
DC73806 UT-105 UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).
DC73807 UT-215 UT-215 (UT215) is a small-molecule selective androgen receptor (AR) irreversible covalent antagonist, covalently and selectively bind to C406 and C327 in the AF-1 region of AR.
DC73808 GDU-952 GDU-952 is a novel small molecule aryl hydrocarbon receptor (AhR) agonist, activates and induces nuclear translocation of AhR.
DC73809 ITE Featured A endogenous ligand, potent aryl hydrocarbon receptor (AhR) agonist in vitro.
DC73810 D089 D089 is a selective small molecule stabilizer of the MYC G4-quadruplex, not only inhibits MYC expression in myeloma cell lines, but also selectively induces G1 arrest in MYC-driven cancer cell lines containing the MYC-G4 sequence.
DC73811 Isopomiferin Isopomiferin is a prenylated isoflavonoid, collapses the tumor checkpoint module (TCM) and suppresses both MYCN and TEAD4 in MYCN-amplified NBL cells.
DC73812 KSI-3716 KSI-3716 is a small molecule c-MYC inhibitor that blocks c-MYC/MAX binding to target gene promoters, inhibits c-MYC mediated transcriptional activity at concentrations as low as 1 uM.

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