BRM/BRG1 ATP Inhibitor-1 free base · Synonyms: brm-brg1 atp inhibitor-1

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin…

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

Target SWI/SNF Complex

Research area Cancer

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Data Sheet SDS COA

BRM/BRG1 ATP Inhibitor-1 structure

CAS No.: 2270879-17-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 900.00	BP-02223-100mg	In stock	Get quote
250 mg	USD 1,788.00	BP-02223-250mg	In stock	Get quote
500 mg	USD 2,385.00	BP-02223-500mg	In stock	Get quote
1 g	USD 3,300.00	BP-02223-1g	In stock	Get quote
2 g	Inquire	BP-02223-2g	In stock	Inquire
5 g	Inquire	BP-02223-5g	In stock	Inquire

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Description

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM.

Biological activity

In Vitro BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM, 5 days) can inhibit the proliferation of cancer cells. BRM/BRG1 ATP Inhibitor-1 inhibits KRT80 gene expression in H1299 cells with the AAC50 (absolute AC50) value of 0.01 μM and in RERF-LC-AI cells with an AAC50 value of 0.01 μM. In Vivo BRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner.

Identifiers

SMILES: C1=C(C(=CN=C1F)CO)NC(=O)NC2=CC(=NS2)C(F)F
InChIKey: CKYCAIAVJIFWPE-UHFFFAOYSA-N

Specifications

MW (average): 318.2750
Formula: C₁₁H₉F₃N₄O₂S
CAS No.: 2270879-17-7
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 200 mg/mL

Documents

References

[1]. Papillon JPN, et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61(22):10155-10172

Same research area

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