HLC40
HLC40 is a MLL1 histone methyltransferase inhibitor with an IC50 of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model.
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- Formule: C38H33F6N3O6S
- Masse moléculaire:773.74
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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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Chemical Information
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Activité biologique
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Caspase 3 |
HLC40 potently inhibits MLL1 histone methyltransferase activity in in vitro cell-free biochemical assay with an IC50 of 0.82 μM[1].
HLC40 potently and selectively inhibits proliferation of MV4-11 and MOLM-13 MLL-rearranged AML cells with IC50 values of 8.92 μM and 7.07 μM, respectively, while showing minimal activity against MLL wild-type K562 cells (IC50 = 49.68 μM)[1].
HLC40 exhibits minimal antagonistic activity against the CysLT1 receptor in stable HEK-293 cells, with an IC50 = 5.28 μM[1].
HLC40 (2.5-10 μM; 72 h) induces concentration-dependent apoptosis in MV4-11 and MOLM-13 MLL-rearranged AML cells, with apoptosis rates reaching up to 30.31% in MV4-11 cells at 10 μM[1].
HLC40 (0.625-10 μM; 24 h) activates the apoptotic pathway in MOLM-13 MLL-rearranged AML cells, as shown by concentration-dependent upregulation of cleaved caspase-3[1].
HLC40 (0.625-10 μM; 24 h) suppresses global H3K4 mono-, di-, and trimethylation in a concentration-dependent manner in MOLM-13 MLL-rearranged AML cells[1].
HLC40 (20 μM; 2 h) directly engages intracellular WDR5 in MOLM-13 MLL-rearranged AML cells, as evidenced by pronounced thermal stabilization of WDR5 at temperatures up to 61°C[1].
HLC40 (10 μM; 24 h) disrupts WDR5-mediated transcriptional activation in MV4-11 MLL-rearranged AML cells, suppressing proliferative programs and upregulating negative cell cycle regulators[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11, MOLM-13 leukemia cell lines
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Concentration:2.5, 5, 10 μM
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Incubation Time:72 h
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Result:Induced statistically significant, concentration-dependent increases in apoptotic cells.
Ranged apoptosis rates from 17.67% to 30.31% in MV4-11 cells.
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Cell Line:MOLM-13 leukemia cell lines
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Concentration:0.625, 1.25, 2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Induced a clear concentration-dependent upregulation of cleaved caspase-3 levels.
Caused a pronounced, concentration-dependent reduction in H3K4me1/2/3 methylation marks.
Showed the most notable decrease observed at 5 μM where H3K4me1 and H3K4me3 levels were substantially suppressed.
| Species | Dose | Route | T1/2 | Cmax |
|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.p. | 16.7 h | 4138.19 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute myeloid leukemia mice (Female Balb/c-nu nude, 6-week injected with MV4-11 cells)[1]
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Dosage:20 mg/kg; 30 mg/kg
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Administration:i.p.; daily; 20 days
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Result:Exhibited dose-dependent tumor growth suppression.
Achieved 49.1% tumor weight growth inhibition (TGI) at 30 mg/kg compared to vehicle control.
Caused no significant body weight loss in any treatment group.
Showed no treatment-related tissue abnormalities in heart, liver, spleen, lung, and kidney relative to controls.
Chemical Information
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Masse moléculaire 773.74
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Formule C38H33F6N3O6S
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SMILES
O=C(NC1=CC2=C(N(CC3=CC=C(C(F)(F)F)C=C3)C=C2CC4=CC=C(C(NS(=O)(C5=CC=CC=C5C(F)(F)F)=O)=O)C=C4OC)C=C1)OC6CCCC6
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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)
HLC40 Related Classifications
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