1. PROTAC Protein Tyrosine Kinase/RTK Apoptosis Cell Cycle/DNA Damage Epigenetics
  2. PROTACs BMX Kinase Apoptosis PARP Caspase
  3. 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.

IHMT-BMX-068

IHMT-BMX-068 Chemical Structure

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Description

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[1]. (Pink: BMX Kinase ligand (HY-184006); Blue: Cereblon ligand (HY-10984); Black: linker).

IC50 & Target[1]

Caspase 3

 

Cereblon

 

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: LNCaP clone FGC prostate cancer cells
Concentration: 1-10 μM
Incubation Time: 96 h
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.

Western Blot Analysis[1]

Cell Line: LNCaP clone FGC prostate cancer cells
Concentration: 0.001-1 μM
Incubation Time: 20 h
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.

Western Blot Analysis[1]

Cell Line: LNCaP clone FGC prostate cancer cells
Concentration: 1-10 μM
Incubation Time: 96 h
Result: Dose-dependently increased levels of cleaved PARP and cleaved caspase-3.
Maintained stable total PARP and total caspase-3 levels.

Apoptosis Analysis[1]

Cell Line: LNCaP clone FGC prostate cancer cells
Concentration: 1-10 μM
Incubation Time: 96 h
Result: Dose-dependently increased the percentage of apoptotic cells.
Caused significant increases observed at 3 μM and 10 μM compared to untreated cells.
Molecular Weight

902.88

Formula

C46H41F3N10O7

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
IHMT-BMX-068
Cat. No.:
HY-184005
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