BRD4-IN-41
BRD4-IN-41 is a BRD4 inhibitor with an IC50 of 34 nM. BRD4-IN-41 also inhibits JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC50 values ranging from 0.9 nM to 43 nM. BRD4-IN-41 inhibits acetyl-lysine binding site of BRD4, downregulates c-MYC, reduces phosphorylated STAT3 levels, induces G1 cell cycle arrest and apoptosis, thereby inhibiting cancer cells growth. BRD4-IN-41 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia.
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- No. CAS: 1877286-69-5
- Fòrmula: C26H34FN7O2S
- Peso molecular:527.66
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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 34 () |
JAK2 1.1 () |
PDGFRβ |
FGFR1 |
NTRK3 |
ROS1 |
STAT3 |
BRD4-IN-41 (Compound 3) potently inhibits the BRD4 bromodomain with an IC50 of 34 nM in an Alpha Screen binding assay[1].
BRD4-IN-41 (100 μM) binds to the BRD4-1 bromodomain, increasing the protein's melting temperature by 11.0°C in a DSF assay[1].
BRD4-IN-41 potently inhibits purified JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC50 values ranging from 0.9 nM to 43 nM in a 33P-ATP radiolabeled assay[1].
BRD4-IN-41 (1 nM-10 μM; 72 h) potently inhibits the growth of human multiple myeloma MM1.S cells with an IC50 of 0.15 μM in a 72 h CellTiter Blue viability assay[1].
BRD4-IN-41 (1 nM-10 μM; 72 h) potently inhibits the growth of human JAK2V617F mutant myeloproliferative neoplasm UKE-1 cells, MM1.S cells and HCC78 cells with IC50 values of 0.08, 0.1 and 0.66 μM in a 72 h CellTiter Blue viability assay[1].
BRD4-IN-41 (6 h) induces dose-dependent inhibition of JAK2 (via reduced phospho-STAT3) and BRD4 (via reduced c-MYC, increased p21Cip1) signaling, and triggers apoptosis (via cleaved PARP) in human multiple myeloma MM1.S cells after 6 h of treatment[1].
BRD4-IN-41 (0.5 μM; 24 h) induces G1 phase arrest[1].
BRD4-IN-41 (6 h) induces dose-dependent inhibition of JAK2 (via reduced phospho-STAT3) and BRD4 (via reduced c-MYC) signaling in human JAK2V617F mutant myeloproliferative neoplasm UKE-1 cells after 6 h of treatment[1].
BRD4-IN-41 (25 nM-500 nM; 14 days) potently inhibits erythroid colony formation in primary JAK2V617F-positive MPN cells, with IC50 values <50 nM[1].
BRD4-IN-41 (96 h) inhibits growth across 931 human cancer cell lines with a mean IC50 of 0.51 μM, showing highest potency against bone and blood cancer cell lines (mean IC50 values 0.18 μM and 0.25 μM, respectively)[1].
BRD4-IN-41 (1 nM-10 μM; 72 h) inhibits the growth of human erythroleukemia HEL cells with an IC50 of 0.37 μM in a 72 h CellTiter Blue viability assay[1].
BRD4-IN-41 (1 nM-10 μM; 72 h) potently inhibits the growth of JAK2V617F transformed BaF3 cells with an IC50 of 0.04 μM in a 72 h CellTiter Blue viability assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM1.S cells
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Concentration:0.5 μM
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Incubation Time:24 h
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Result:Increased cells in G1 phase.
Chemical Information
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No. CAS 1877286-69-5
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Peso molecular 527.66
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Fòrmula C26H34FN7O2S
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SMILES
CC(S(=O)(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C)CC4)C(F)=C3)=NC=C2C)=C1)=O)(C)C
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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)
BRD4-IN-41 Related Classifications
HY-115541 Related Classifications
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