BKT300
BKT300 is a potent and selective protein regulator of cytokinesis 1 (PRC1) inhibitor. BKT300 inhibits PRC1 dephosphorylation at T481, disrupts actin and microtubule formation, induces G2/M cell cycle arrest, triggers mitotic catastrophe, and promotes apoptosis, thereby inhibiting proliferation and migration of acute myeloid leukemia (AML) cells while sparing normal cells. BKT300 inhibits tumor growth in mouse xenograft AML models. BKT300 can be used for the research of AML.
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- CAS No.: 2551033-16-8
- Formule: C22H25NO6
- Masse moléculaire:399.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
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PRC1 |
Caspase-3 |
BKT300 binds recombinant PRC1 with Kd values of 28.3 nM (SPR assay) and 104 nM (MST assay)[1].
BKT300 (31.25-5000 nM; 3 h) inhibits migration of U937 and Jurkat cells toward CXCL12, and migration of THP-1 cells toward MCP-1[1].
BKT300 (62.5-500 nM; 24 h) dose-dependently inhibits actin filament formation in U937 cells, but not in normal peripheral blood mononuclear cells (PBMCs)[1].
BKT300 (1 µM; 24 h) disrupts microtubule organization and formation in U937 cells[1].
BKT300 (7.8-5000 nM; 2-24 h) induces G2/M arrest and cell death in U937, MV4-11, OCI-AML-2, OCI-AML-3, Molm14, and Marimo AML cells[1].
BKT300 (3.9-1000 nM; 24 h) induces dose-dependent apoptosis in U937 cells, accompanied by elevated cleaved caspase-3 expression[1].
BKT300 (50-1000 nM; 24 hours) downregulates CDC25C, upregulates p21, and induces dose/time-dependent PRC1 phosphorylation at T481 in U937 and MV4-11 cells[1].
BKT300 (31.2-500 nM; 24 h) increases pPRC1 (T481) levels in U937 cells but not in normal PBMCs[1].
BKT300 (24 h) inhibits OCI-AML-3, Marimo, OCI-AML-2, MOLM-14, U937, K562, MV4-11 and HL-60 cells with IC50s of 107, 135, 120, 122, 27, 98, 98, and 110 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U937 cells
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Concentration:19.5, 39, 62.5, 78, 156, 313, 625, 1250, 2500, 5000 nM
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Incubation Time:24 h; 2, 4, 6, 8, 24 h (at 62.5 nM)
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Result:Induced G2/M cell cycle arrest in U937 cells, in a dose- and time-dependent manner.
Induced cell death in U937 cells at 62.5 nM.
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Cell Line:OCI-AML-2, OCIAML-3, Molm14, Marimo
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Concentration:250 nM
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Incubation Time:24 h
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Result:Induced G2/M cell cycle arrest in all tested cells.
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Cell Line:U937 cells
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Concentration:3.9, 7.8, 15.6, 31.25, 62.5, 125, 250, 500, 1000 nM
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Incubation Time:24 h
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Result:Increased apoptotic cells in U937 cells in a dose-dependent manner.
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Cell Line:U937, Jurkat, and THP-1 leukemic cells
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Concentration:31.25, 62.5, 125, 250, 500, 1000 nM (U937 and THP1 cells); 125, 250, 500, 1000, 5000 nM (Jurkat cells)
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Incubation Time:3 h
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Result:Significantly inhibited the migration of U937 cells and Jurkat cells toward CXCL12 in a dose-dependent manner.
Inhibited the migration of AML THP-1 cells toward monocyte chemotactic protein-1 (MCP-1) in a dose-dependent manner.
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Cell Line:U937, REH, NB4, MV4-11cells
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Concentration:50, 100, 1000 nM (U937 cells); 1000 nM (REH, NB4, MV4-11cells)
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Incubation Time:24 h
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Result:Increased cleaved caspase-3 levels in U937 cells in a dose-dependent manner.
Increased cleaved caspase-3 levels in U937, REH, NB4, MV4-11cells at 1000 nM.
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Cell Line:U937, MV4-11 leukemic cell lines
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Concentration:50 nM, 100 nM, 1000 nM (24 h CDC25C/p21); 100 nM, 500 nM, 1000 nM (24 h pPRC1); 1000 nM (pPRC1 time course)
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Incubation Time:24 h (CDC25C/p21, pPRC1 dose-response); 4 h, 24 h (pPRC1 time course)
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Result:Downregulated CDC25C and upregulated p21 in U937/MV4-11 cells without affecting CDC2/cyclin B1.
Induced a dose-dependent increase in PRC1 phosphorylation at T481 within 4 h, peaking at 24 h, without altering total PRC1 levels.
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Cell Line:U937 cells, normal PBMCs
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Concentration:31.2, 62.5, 125, 250, 500 nM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in pPRC1 (T481) levels in U937 cells.
Had no effect on pPRC1 or total PRC1 levels in normal PBMCs.
BKT300 (2.5 mg/mouse; s.c.;twice daily from day 10 to day 12) inhibits tumor growth and induces tumor regression in the U937 xenograft mouse model[1].
BKT300 (2.5 mg/mouse; s.c.; on day 12 to day 16 and day 19 to day 20) reduces AML cell levels in blood and bone marrow in the MV4-11 intravenous xenograft mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD scid gamma (NSG) mice (6-8-week-old) subcutaneously injected with U937 cells[1]
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Dosage:1, 1.5, 2, 2.5 mg/mouse
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Administration:s.c.; once daily from day 3 to day 7
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Result:Achieved 98% tumor growth inhibition, with 6/7 treated mice exhibiting complete tumor growth inhibition by day 11.
Induced apoptosis of tumor cells.
Decreased CDC25C and increased pPRC1 T481 expression in the tumors.
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Animal Model:NOD scid gamma (NSG) mice (6-8-week-old) subcutaneously injected with U937 cells[1]
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Dosage:2.5 mg/mouse
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Administration:s.c.; twice daily from day 10 to day 12
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Result:Reached 95.9% tumor growth inhibition and 89.4% tumor regression by day 17.
Showed no effect on body weight.
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Animal Model:NOD scid gamma (NSG) mice (6-8-week-old) intravenously injected with MV4-11 cells[1]
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Dosage:2.5 mg/mouse
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Administration:s.c.; on day 12 to day 16 and day 19 to day 20
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Result:Reduced the percentage of AML cells in the blood by 74.8% and in bone marrow by 72%.
Increased the number of normal mouse cells in the bone marrow by 2-fold and in blood by 7-fold compared to control mice.
Chemical Information
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CAS No. 2551033-16-8
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Masse moléculaire 399.44
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Formule C22H25NO6
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SMILES
O=C1NC2=C(C(O)=C1CCCCC)C=C(OC)C=C2OC3=CC=C(C=C3OC)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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