2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. HIF-2α-IN-18

HIF-2α-IN-18 is a selective HIF-2α inhibitor with a human IC50 of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the HIF-2α/ARNT dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting HIF-1α target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma[1].

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HIF-2α-IN-18

HIF-2α-IN-18 構造式

CAS 番号 : 2709068-47-1

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HIF-2α-IN-18 関連抗体

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製品説明

HIF-2α-IN-18 is a selective HIF-2α inhibitor with a human IC50 of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the HIF-2α/ARNT dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting HIF-1α target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma[1].

IC50 & Target[1]

HIF-2α

8.1 nM (IC50)

体外実験

HIF-2α-IN-18 (Compound 13) (1 h; 45 min) potently inhibits binding to recombinant human HIF-2α PAS-B protein with an SPA IC50 of 14.8 nM[1].
HIF-2α-IN-18 (20 h) potently inhibits HIF-2α-mediated transcriptional activity in 786-O ccRCC cells with a cellular luciferase IC50 of 8.1 nM[1].
HIF-2α-IN-18 (20 h) inhibits HIF-2α-mediated transcriptional activity in 786-O ccRCC cells in 100% human serum with a cellular luciferase IC50 of 0.82 μM[1].
HIF-2α-IN-18 (0-50 μM; 20 h) inhibits HIF-2α-regulated VEGF-A secretion in 786-O ccRCC cells with an IC50 of 60 nM[1].
HIF-2α-IN-18 (0.01-10 μM; 20 h) potently and selectively inhibits hypoxia-induced HIF-2α target gene (EPO, SERPINE1) expression in Hep3B hepatocellular carcinoma cells without inhibiting HIF-1α target gene (PGK1, PDK1) expression[1].
HIF-2α-IN-18 (0.5 μM) has an in vitro intrinsic clearance of 29.2 μL/min/106 cells in human hepatocytes and 141 μL/min/106 cells in rat hepatocytes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HIF-2α-IN-18 関連抗体

Real Time qPCR[1]

Cell Line: Hep3B hepatocellular carcinoma cells (intact VHL, functional HIF-1α and HIF-2α)
Concentration: 0.01 μM; 0.1 μM; 10 μM
Incubation Time: 20 h
Result: Dose-dependently inhibited hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1.
No robust or dose-dependent inhibition of HIF-1α target genes PGK1 and PDK1 was observed.
Maintained cell viability throughout the assay.
Parmacokinetics
Species Dose Route CL Vss T1/2 MRTINF_obs
Rat[1] 0.25 mg/kg i.v. 6.31 L/h/kg 9.60 L/kg 2.15 h 1.53 h
体内実験

HIF-2α-IN-18 (Compound 13) (0.25 mg/kg; i.v.; single dose) exhibits an in vivo clearance of 6.31 L/h/kg, elimination half-life of 2.15 h, and 93.1% plasma protein binding in male Sprague-Dawley rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, weight 200-250 g)[1]
Dosage: 0.25 mg/kg
Administration: i.v.; single dose
Result: Achieved an in vivo clearance (CL) of 6.31 L/h/kg.
Reached a volume of distribution at steady state (Vss) of 9.60 L/kg.
Had an elimination half-life (T1/2) of 2.15 h.
Exhibited a mean residence time (MRTINF) of 1.53 h.
Showed plasma protein binding (PPB) of 93.1% bound.
分子量

399.27

分子式

C18H8F7N3
CAS 番号
SMILES

F[C@@H]1C(C=C(F)C=C2C#N)=C2N(C3=CC=C(C(F)(F)F)C(F)=C3C#N)C[C@@H]1F
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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Keywords:

HIF-2α-IN-182709068-47-1HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHARNTclear cell renal cell carcinoma786-O ccRCC cellsHIF-2α PAS-B domainEPOHIF-1αVEGF-APGK1PDK1SERPINE1Inhibitorinhibitorinhibit

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