IHMT-BMX-068
IHMT-BMX-068 is a BMX PROTAC degrader with a DC50 of 0.007 μM. IHMT-BMX-068 promotes ubiquitination and degradation of BMX. IHMT-BMX-068 increases the levels of cleaved PARP and cleaved Caspase-3, and induces Apoptosis. IHMT-BMX-068 exerts anti-cancer effects against prostate cancer. IHMT-BMX-068 can be used for the research of prostate cancer.
(Pink: BMX Kinase ligand (HY-184006); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Formula: C46H41F3N10O7
- Molecular Weight:902.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Caspase 3 |
Cereblon |
IHMT-BMX-068 potently degrades BMX protein in H446DDPR cells, with a DC50 of 0.007 μM[1].
IHMT-BMX-068 potently inhibits the proliferation of DU145, LNCaP clone FGC, 22Rv1 and VCaP prostate cancer cells, with GI50 values of 0.29 μM, 0.83 μM, 1.83 μM and 6.65 μM, respectively; it shows no significant cytotoxicity in normal CHO cells (GI50 > 10 μM)[1].
IHMT-BMX-068 (1-10 μM; 96 h) inhibits the growth of LNCaP clone FGC cells in a dose-dependent manner at concentrations of 1 μM, 3 μM and 10 μM following 96 h of treatment[1].
Treatment with IHMT-BMX-068 (0.001-1 μM; 20 h) induces dose-dependent degradation of BMX protein in LNCaP clone FGC cells, with a DC50 of 0.038 μM, and the degradation effect reaches maximum at 0.1 μM[1].
IHMT-BMX-068 (1-10 μM; 96 h) induces caspase-mediated apoptosis in LNCaP clone FGC cells in a dose-dependent manner. After 96 h of treatment, increased levels of cleaved PARP and cleaved caspase-3 are observed at concentrations of 1 μM, 3 μM, and 10 μM[1].
IHMT-BMX-068 (0.3-10 μM; 24 h) inhibits the proliferation of LNCaP clone FGC cells in a dose-dependent manner, which is evidenced by the reduced percentages of EdU-positive cells at concentrations of 0.3 μM, 1 μM, 3 μM and 10 μM after 24 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP clone FGC prostate cancer cells
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Concentration:1-10 μM
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Incubation Time:96 h
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Result:Dose-dependently inhibited LNCaP clone FGC cell growth.
Caused significant reductions in cell number observed at 3 μM, 1 μM, and 10 μM after 96 h compared to untreated cells.
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Cell Line:LNCaP clone FGC prostate cancer cells
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Concentration:0.001-1 μM
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Incubation Time:20 h
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Result:Induced BMX degradation at 0.01 μM.
Achieved maximal effects at approximately 0.1 μM.
Caused BMX levels to recover at 1 μM due to the "hook effect".
Had a DC50 for BMX degradation of 0.038 μM.
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Cell Line:LNCaP clone FGC prostate cancer cells
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Concentration:1-10 μM
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Incubation Time:96 h
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Result:Dose-dependently increased levels of cleaved PARP and cleaved caspase-3.
Maintained stable total PARP and total caspase-3 levels.
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Cell Line:LNCaP clone FGC prostate cancer cells
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Concentration:1-10 μM
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Incubation Time:96 h
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Result:Dose-dependently increased the percentage of apoptotic cells.
Caused significant increases observed at 3 μM and 10 μM compared to untreated cells.
Chemical Information
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Molecular Weight 902.88
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Formula C46H41F3N10O7
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SMILES
O=C(NC1=CC=C(C)C(N2CC3=CN=C(NC4=CC=C(C)C(NC(CCCNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)=C4)N=C3N(C)C2=O)=C1)C8=CC=CC(C(F)(F)F)=C8
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)