SMARCA2/SMARCA4 ligand-1
SMARCA2/SMARCA4 ligand-1 is a SMARCA2/SMARCA4 ligand with KD values of 1.2 and 10.3 nM. SMARCA2/SMARCA4 ligand-1 binds SMARCA2/4 bromodomain via hydrogen bonds with asparagine and tyrosine residues, and a salt bridge with a glutamate residue. SMARCA2/SMARCA4 ligand-1 shows antiproliferative activity against cancer cells. SMARCA2/SMARCA4 ligand-1 can be used for the research of cancer, such as smarca4 mutant nonsmall cell lung cancer.
For research use only. We do not sell to patients.
- Formula: C20H17BrN4O
- Molecular Weight:409.28
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All SWI/SNF Complex Isoforms
More
Biological Activity
|
SMARCA2 1.2 nM (Kd) |
SMARCA4 10.3 nM (Kd) |
SMARCA2 98.5 nM (IC50) |
SMARCA4 285 nM (IC50) |
PBRM1 |
SMARCA2/SMARCA4 ligand-1 (Compound 4p) potently binds to purified SMARCA2 bromodomain with an IC50 of 95.8 nM[1].
SMARCA2/SMARCA4 ligand-1 binds to purified SMARCA4 bromodomain with potency with an IC50 of 285 nM[1].
SMARCA2/SMARCA4 ligand-1(0.064-200 μM) binds to purified SMARCA2 bromodomain with a Kd of 1.2 nM[1].
SMARCA2/SMARCA4 ligand-1 (0.625-10 μM) binds to purified SMARCA4 bromodomain with a Kd of 10.3 nM[1].
SMARCA2/SMARCA4 ligand-1 demonstrates high stability in aqueous solutions at pH 1 and pH 7 and in cell culture medium, retaining >99% purity over 24 h[1].
SMARCA2/SMARCA4 ligand-1 (compound 4p) shows antiproliferative activity in NCI-H1568 and HEK-293 cells with IC50 values of 13.94 and 11.76 μM[1].
SMARCA2/SMARCA4 ligand-1 (20 μM; 2 h) rescues SMARCA2 and PBRM1 in NCI-H1568 cells, confirming target engagement dependency of the PROTAC effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:NCI-H1568
-
Concentration:20 μM
-
Incubation Time:2 h (pre-incubation); 2 h (PROTAC 14 treatment)
-
Result:Effectively restored SMARCA2 and PBRM1 protein levels reduced by PROTAC 14 (HY-183007) treatment.
Chemical Information
-
Molecular Weight 409.28
-
Formula C20H17BrN4O
-
SMILES
O=C1[N-][N+]2=CC3=CC=C(C=C3C=C2C4=CC=CC(Br)=C14)N5CCNCC5
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SMARCA2/SMARCA4 ligand-1 Related Classifications
HY-182987 Related Classifications
Powered by Bioz