SJ44236
SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC50 = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma.
(Pink: BET ligand (HY-78695); Blue: Cereblon ligand (HY-W890189); Black: linker (HY-W012935)).
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- Fòrmula: C40H45ClN8O3S
- Peso molecular:753.36
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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BRD4 127 pM (DC50) |
BRD2 |
BRD3 |
Cereblon |
SJ44236 (1×10-10 to 1×102 μM; 24 h) potently degrades BRD4 in HiBiT-BRD4 HEK293 LgBiT stable cells with a Dmax50 of 0.19 nM, achieving 96.9% maximal degradation sustained for over 20 h with no impact on cell viability[1].
SJ44236 (0.001-100 nM; 4 h) degrades endogenous BRD4 in MV4-11 cells with a DC50 of 0.127 nM after 4 h of treatment, consistent with its potency in engineered HEK293 cells[1].
SJ44236 (72 h) potently inhibits the proliferation of MV4-11 cells with an IC50 of 0.12 nM and HD-MB03 cells with an IC50 of 0.92 nM after 72 h of treatment[1].
SJ44236 (100 nM; 4 h) induces over 90% degradation of BRD2, BRD3, and BRD4 in MV4-11 cells after 4 h of treatment at 100 nM, alongside expected downstream regulation of c-Myc (down) and p53 (up)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 753.36
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Fòrmula C40H45ClN8O3S
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SJ44236 Related Classifications
HY-170900 Related Classifications
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