A dual inhibitor of BRM and BRG1 ATPase activities
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Product Type

Small Molecule Modulators
Small Molecule Inhibitors
ATPases

Research Area

Cancer

BRM/BRG1 ATP Inhibitor 1

Item No. 36138

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-(difluoromethyl)-5-isothiazolyl]-N′-[2-fluoro-5-(hydroxymethyl)-4-pyridinyl]-urea
CAS Number
2270879-17-7
Synonyms
  • Brahma Homologue/Brahma-related Gene 1 Adenosine 5'-triphosphate Inhibitor 1
Molecular Formula
C11H9F3N4O2S
Formula Weight
318.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
276 nm
SMILES
O=C(NC1=CC(F)=NC=C1CO)NC2=CC(C(F)F)=NS2
InChi Code
InChI=1S/C11H9F3N4O2S/c12-8-1-6(5(4-19)3-15-8)16-11(20)17-9-2-7(10(13)14)18-21-9/h1-3,10,19H,4H2,(H2,15,16,17,20)
InChi Key
CKYCAIAVJIFWPE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $109

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    1 mg

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    5 mg

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    10 mg

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    Cayman Chemical
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    Product Description

    BRM/BRG1 ATP inhibitor 1 is an allosteric dual inhibitor of brahma homologue (BRM), also known as SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin, subfamily A, member 2 (SMARCA2), and brahma-related gene 1 (BRG1), also known as SMARCA4, ATPase activities (IC50s = <0.005 µM for both).1 It reduces the expression of keratin 80 (KRT80) in H1299 and RERF-LC-A1 cells. BRM (20mg/kg) reduces tumor growth in a RERF-LC-A1 lung cancer mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Papillon, J.P.N., Nakajima, K., Adair, C.D., 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. 61(22), 10155-10172 (2018).