Cookie Policy: This site uses cookies to improve your experience. You can find out more about our use of cookies in our Privacy Policy. By continuing to browse this site you agree to our use of cookies.
BellBrook
BRM014 (SMARCA2 & SMARCA4 Inhibitor)
As low as
592
CHF
CHF 592.00
In stock
Only %1 left
BBL-5003-M0011 mgCHF 592.00
BBL-5003-M0055 mgCHF 1’333.00
NEW
| Product Details | |
|---|---|
| Synonyms | Brahma Homologue/Brahma-related Gene 1 Adenosine 5'-triphosphate Inhibitor 1; NVP-RXI570 |
| Product Type | Chemical |
| Properties | |
| Formula |
C11H9F3N4O2S |
| MW | 318.3 |
| CAS | 2270879-17-7 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white powder. |
| Solubility | Soluble in DMSO (70mg/ml). |
| Biological Activity |
BRM014 is a SMARCA2 (BRM) and SMARCA4 (BRG1) inhibitor that has been fully validated using the Transcreener ADP Assay. An IC50 of 2.8 nM (SMARCA2) 1.79 nM (SMARCA4) was obtained using a 12-point dose-response assay. |
| Identity | Determined by 1H-NMR |
| InChi Key | CKYCAIAVJIFWPE-UHFFFAOYSA-N |
| Smiles | O=C(NC1=CC(F)=NC=C1CO)NC2=CC(C(F)F)=NS2 |
| Shipping and Handling | |
| Shipping | BLUE ICE |
| Short Term Storage | -20°C |
| Long Term Storage | -20°C |
| Handling Advice | After opening, prepare aliquots and store at -20°C. |
| Use/Stability | Stable for at least 1 year after receipt when stored at -20°C. |
| Documents | |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), also known as Brahma homolog (BRM), together with its close homolog Brahma-related gene 1 (BRG1), or SMARCA4, are ATPases of the large ATP-dependent SWI/SNF chromatin-remodeling complexes involved in transcriptional regulation of gene expression. BRM014 (2270879-17-7) is an allosteric dual inhibitor of BRM and BRG1 (IC50<5 nM for both). It downregulated BRM-dependent gene expression and displayed antiproliferative activity in a BRG1-mutant-lung-tumor xenograft model after oral administration. Inhibition of BRG1/BRM ATPase by BRM014 inhibits chromatin openness. For example, it reduced DNA accessibility to core regulatory factors (RUNX1, LM01, and MEIS1) at transcription factor PU.1 sites in AML cells. P583 cells formed markedly large spheroids when treated with BRM014. Cell permeable and active in vivo.
Product References
- 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.P.N. Papillon, et al.; Med. Chem. 61, 10155 (2018)
- Chromatin openness requires continuous SW1/SNF activity; D.C. Hargreaves; Genet. 53, 263 (2021)
- SW1/SNF Blockade Disrupts PU.1-Directed Enhancer Programs in Normal Hematopoietic Cells and Acute Myeloid Leukemia: C. Chambers, et al.; Cancer Res. 83, 983 (2023)
- Chemical inhibition of SWI/SNF induces transformed growth in non-mutant cells, mimicking the effects of a SMARC4 mutation associated with small cell carcinoma of the ovary, hypercalcemic type: A.J. Krieg, et al.; Oncol. Rep. 48, S32 (2023) (Poster Presentation)
Related Products
-
Transcreener ADP2 FP Assay BBL-3010 -
Transcreener ADP2 FI Assay BBL-3013
