A HIF-2α translation inhibitor
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HIF-2α Translation Inhibitor 76

Item No. 42446

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[cyano(methylsulfonyl)methylene]hydrazinyl]-2-thiophenecarboxylic acid, methyl ester
CAS Number
882268-69-1
Synonyms
  • Hypoxia-Inducible Factor-2α Translation Inhibitor 76
Molecular Formula
C9H9N3O4S2
Formula Weight
287.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
CS(=O)(C(C#N)=NNC1=C(C(OC)=O)SC=C1)=O
InChi Code
InChI=1S/C9H9N3O4S2/c1-16-9(13)8-6(3-4-17-8)11-12-7(5-10)18(2,14)15/h3-4,11H,1-2H3
InChi Key
OOGAPDPPVHJYGJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    HIF-2α translation inhibitor 76 is an inhibitor of hypoxia-inducible factor-2α (HIF-2α) translation.1 It inhibits constitutive gene expression in a hypoxia-response element (HRE) reporter assay using VHL-deficient 786-O renal cell carcinoma (RCC) cells (IC50 = 5 µM). HIF-2α translation inhibitor 76 reduces the translation of nascent HIF-2α mRNA in 786-O cells. Conditioned medium from 786-O cells preincubated with HIF-2α translation inhibitor 76 inhibits the proliferation of human umbilical vein endothelial cells (HUVECs). HIF-2α translation inhibitor 76 (10 nM) inhibits erythrocytosis and angiogenesis induced by DMOG (Item No. 71210) in zebrafish.2 It increases survival and right ventricle contractility and inhibits right ventricle hypertrophy in a rat model of pulmonary arterial hypertension induced by monocrotaline (Item No. 16666).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zimmer, M., Ebert, B.L., Neil, C., et al. Small-molecule inhibitors of HIF-2a translation link its 5'UTR iron-responsive element to oxygen sensing. Mol. Cell. 32(6), 838-848 (2008).

    2. Metelo, A.M., Noonan, H.R., Li, X., et al. Pharmacological HIF2α inhibition improves VHL disease-associated phenotypes in zebrafish model. J. Clin. Invest. 125(5), 1987-1997 (2015).

    3. Dai, Z., Zhu, M.M., Peng, Y., et al. Therapeutic targeting of vascular remodeling and right heart failure in pulmonary arterial hypertension with a HIF-2α inhibitor. Am. J. Respir. Crit. Care Med. 98(11), 1423-1434 (2018).