Omvitrastat (OP-3136) | KAT6 inhibitor

Chemical Structure : OP-3136

CAS No.: 3056105-63-3

OP-3136 (Omvitrastat, OP3136)

Catalog No.: PC-26758Not For Human Use, Lab Use Only.

Omvitrastat (OP-3136, OP3136) is a potent, selective and orally bioavailable histone lysine acetyltransferase (KAT6, KAT6A/B) inhibitor, demonstrates robust anti-tumor activity in preclinical models of prostate cancer, ovarian cancer, and non-small cell lung cancer (NSCLC), both in vitro and in vivo.

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Biological Activity

Omvitrastat (OP-3136, OP3136) is a potent, selective and orally bioavailable histone lysine acetyltransferase (KAT6, KAT6A/B) inhibitor, demonstrates robust anti-tumor activity in preclinical models of prostate cancer, ovarian cancer, and non-small cell lung cancer (NSCLC), both in vitro and in vivo.

OP-3136 decreases the proliferation of breast cancer cell lines in vitro and inhibits tumor growth in ZR-75-1 (KAT6-amplified ER+ BC cell line), T47D (KAT6-overexpressed ER+ BC cell line), and ST340 (ER+, HER2+ BC PDX cell line) mouse xenografts.

OP-3136 combined with complete estrogen receptor antagonists (CERANs) such as fulvestrant and palazestrant and/or with cyclin-dependent kinase 4/6 (CDK4/6) inhibitors such as ribociclib show strong synergistic effects.

Physicochemical Properties

M.Wt	462.48
Formula	C20H22N4O7S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-((1H-Pyrazol-1-yl)methyl)-6-methoxy-N-((2,4,6-trimethoxyphenyl)sulfonyl)picolinamide

References

1. Gopinath S. Palanisamy, et al. Cancer Res (2025) 85 (8_Supplement_2): LB166.

OP-3136 (Omvitrastat, OP3136)

Biological Activity

Physicochemical Properties

References

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