SJ44236
SJ44236 is the PROTAC degrader for BET that degrades BRD2 (DC50 = 0.127 nM), BRD3 and BRD4. SJ44236 exhibits cytotoxicity in cell MV4-11 and HD-MB03 with IC50s of 0.12 nM and 0.92 nM. SJ44236 downregulates the expression of c-Myc, upregulates the expression of p53. SJ44236 exhibits a good orally bioavailability of 45% in mice[1]. (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695) ; Black: linker (HY-W012935) ; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 54 (HY-W890189) )
Product Specifications
UNSPSC
12352005
Target
Epigenetic Reader Domain; PROTACs
Related Pathways
Epigenetics; PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Smiles
O=C(C[C@@H]1N=C(C2=C(N3C1=NN=C3C)SC(C)=C2C)C4=CC=C(Cl)C=C4)N5CCC(CC5)CN6CCN(C7=CC=C(C=C7)C8C(NC(CC8)=O)=O)CC6
Molecular Formula
C40H45ClN8O3S
Molecular Weight
753.36
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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