SJ46421
SJ46421 is a BRD3BD2 PROTAC degrader. SJ46421 induces a cooperative ternary complex of KLHDC2 and BRD3BD2 with an IC50 of 7.8 nM. SJ46421 binds to the substrate-binding pocket of KLHDC2, forms cooperative ternary complexes with BRD3BD2, BRD2BD2 and BRD4BD2, disrupts the autoinhibitory tetramer assembly of KLHDC2, drives selective ubiquitination of BRD3BD2, and inhibits the ubiquitination of endogenous KLHDC2 diglycine substrates. SJ46421 can be used in cancer research.
(Pink: BRD3 BD2 ligand (HY-13030); Blue: KLHDC2 ligand (HY-168536); Black: linker (HY-20797)).
For research use only. We do not sell to patients.
- Formula: C42H41ClN8O5S2
- Molecular Weight:837.41
-
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 PROTACs Isoforms
More
Biological Activity
|
BRD3 BD2 987 nM (Kd) |
BRD4 BD2 1020 nM (Kd) |
BRD2 BD2 2090 nM (Kd) |
SJ46421 (0.6 μM; 0-60 seconds) promotes efficient polyubiquitylation of BRD2BD2, BRD3BD2, and BRD4BD2 via neddylated CRL2KLHDC2 in vitro[1].
SJ46421 (0.001-10 μM; 15 minutes pre-incubation) forms a high-affinity ternary complex with neddylated CRL2KLHDC2 and BRD3BD2, potently inhibiting KLHDC2 substrate ubiquitylation with a Ki(app) of 7.84 nM[1].
SJ46421 forms a highly positively cooperative ternary complex with KLHDC2SBD and BRD3BD2 (α=16) with a Kd of 19 nM, while forming only moderately cooperative complexes with BRD2BD2 (α=1.4) and BRD4BD2 (α=2.8)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
Molecular Weight 837.41
-
Formula C42H41ClN8O5S2
-
SMILES
O=C(O)CNC(CC1=CSC(C2=CC=C3C=CC=C(OCCN4CCN(C(C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5)=O)CC4)C3=C2)=N1)=O
-
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)
SJ46421 Related Classifications
HY-168634 Related Classifications
Powered by Bioz