M1002

Names

[ Name ]:
M1002

[Synonym ]:
1,2-Benzisothiazol-3-amine, N-[3,5-bis(trifluoromethyl)phenyl]-, 1,1-dioxide
MFCD05999002
N-[3,5-Bis(trifluoromethyl)phenyl]-1,2-benzothiazol-3-amine 1,1-dioxide

Biological Activity

[Description]:

M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

[In Vitro]

M1002 (10 μM; 24 h) enhances the expression of HIF-2 target genes with great efficacy[1]. M1002 (5 μM; 24 h) treatment shows synergy with prolyl hydroxylase domain (PHD) inhibitors[1]. RT-PCR[1] Cell Line: 786-O cells Concentration: 10 μM Incubation Time: 24 hours Result: Showed clear agonistic effects on the expression of HIF-2 target genes in 786-O cells as compared with the control. RT-PCR[1] Cell Line: Hep3B cells Concentration: 5 μM Incubation Time: 24 hours Result: Elevated the expression of EPO and NDRG1 by co-treatment of M1002 together with PHD inhibitors, compared with M1002 alone treatment.

[References]

[1]. Dalei Wu, et al. Bidirectional modulation of HIF-2 activity through chemical ligands. Nat Chem Biol. 2019 Apr;15(4):367-376.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
414.6±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₅H₈F₆N₂O₂S

[ Molecular Weight ]:
394.292

[ Flash Point ]:
204.6±31.5 °C

[ Exact Mass ]:
394.021057

[ LogP ]:
5.15

[ Vapour Pressure ]:
0.0±1.0 mmHg at 25°C

[ Index of Refraction ]:
1.564