MedChemExpress - Model Unesbulin -1610964-64-1
Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity[1][2].MCE products for research use only. We do not sell to patients.
Unesbulin
MCE China：Unesbulin
Brand：MedChemExpress (MCE)
Cat. No.HY-112041
CAS：1610964-64-1
Synonyms：PTC596
Purity：99.45%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity.
In Vitro：Unesbulin (PTC596; 20-200 nM; for 48 hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis[1]. Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase[1]. Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1[1]. Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1[2].
In Vivo：Unesbulin (PTC596; 5 mg/kg; oral gavage; every 3 days for 13 days) significantly prolongs mouse survival[1]. Unesbulin (20 mg/kg; oral gavage; once a week for 15 days) causes tumor volume significantly smaller than that of control SCID mice with K562 cells[1]. Unesbulin (10 or 12.5 mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells[1].
IC50 & Target：BMI-1[1] In Vitro Unesbulin (PTC596; 20-200 nM; for 48 hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis[1]. Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase[1]. Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1[1]. Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Unesbulin Related Antibodies Apoptosis Analysis[1] Cell Line: AML cell lines (MOLM-13, OCI-AML3, MOLM-14, MV4-11, U-937, HL-60)
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References：
[1]. Nishida Y, et al. The novel BMI-1 inhibitor PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells. Blood Cancer J. 2017 Feb 17;7(2):e527. [Content Brief]
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