OP-3136 free base · Synonyms: OP 3136 · OP3136

OP-3136 is a novel, orally available small molecule that potently and selectively inhibits lysine acetyltransferase 6 (KAT6), an epigenetic target…

For research use only. Not for human or veterinary use.

Target Histone Acetyltransferase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

OP-3136 structure

CAS No.: 3056105-63-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 mg	USD 510.00	BP-02283-5mg	In stock	Get quote
10 mg	USD 798.00	BP-02283-10mg	In stock	Get quote
25 mg	USD 1,480.00	BP-02283-25mg	In stock	Get quote
50 mg	USD 2,680.00	BP-02283-50mg	In stock	Get quote
100 mg	Inquire	BP-02283-100mg	In stock	Inquire

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Description

OP-3136 is a novel, orally available small molecule that potently and selectively inhibits lysine acetyltransferase 6 (KAT6), an epigenetic target that is dysregulated in breast and other cancers. In preclinical studies, OP-3136 has demonstrated significant anti-proliferative activity in ER+ breast cancer models and is combinable and synergistic with endocrine therapies, including palazestrant and cyclin-dependent kinase 4/6 (CDK4/6) inhibitors.

Biological activity

In Vitro Omvitrastat (OP-3136) inhibits proliferation of VCAP, OAW28, OVCAR3, and LCLC-97TM1 cell lines. Omvitrastat reduces the proliferation of breast cancer cell lines and inhibits growth in KAT6-overexpressing ER+ breast cancer cell models. In Vivo Omvitrastat (OP-3136) (0.5-1 mg/kg; p.o.) monotherapy induces tumor regression in OVCAR3 ovarian cancer xenografts with TGIs of 104.5% and 105.4% at doses of 0.5 mg/kg and 1 mg/kg, respectively. Omvitrastat (1 mg/kg; p.o.) monotherapy inhibits tumor growth in LCLC-97TM1 NSCLC xenografts with a TGI of 62% at a dose of 1 mg/kg.

Identifiers

SMILES: O=C(NS(=O)(=O)C=1C(OC)=CC(OC)=CC1OC)C2=NC(OC)=C(C=C2)CN3N=CC=C3
InChIKey: KZSVPOQXJZQAQQ-UHFFFAOYSA-N

Specifications

MW (average): 462.4760
Formula: C₂₀H₂₂N₄O₇S
CAS No.: 3056105-63-3
Physical state: Solid
Color: White to off-white
Shipping: Shipping with dry ice.
Storage: Powder -80℃

Solubility

soluble in DMSO

In vitro: DMSO : 25 mg/mL

Documents

References

[1]. Gopinath S. Palanisamy, et al. Abstract LB166: OP-3136, a selective KAT6 inhibitor, demonstrates anti-tumor activity in prostate, ovarian, and non-small cell lung cancer preclinical models. Cancer Res (2025) 85 (8_Supplement_2): LB166.

[2]. Roussel-Simonin C, et al. Exploring KAT6 as a therapeutic target in breast cancer: epigenetic approaches for precision medicine. NPJ Breast Cancer. 2025 Dec 19;11(1):146.approaches for precision medicine. NPJ Breast Cancer. 2025 Dec 19;11(1):146.

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