2. Epigenetics Apoptosis
  3. Histone Methyltransferase WDR5 Apoptosis Caspase
  4. 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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HLC40

HLC40 Chemical Structure

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HLC40 Related Antibodies

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

IC50 & Target[1]

Caspase 3

 

In Vitro

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.

HLC40 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MV4-11, MOLM-13 leukemia cell lines
Concentration: 2.5, 5, 10 μM
Incubation Time: 72 h
Result: Induced statistically significant, concentration-dependent increases in apoptotic cells.
Ranged apoptosis rates from 17.67% to 30.31% in MV4-11 cells.

Western Blot Analysis[1]

Cell Line: MOLM-13 leukemia cell lines
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24 h
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.
Parmacokinetics
Species Dose Route T1/2 Cmax
Mice[1] 30 mg/kg i.p. 16.7 h 4138.19 ng/mL
In Vivo

HLC40 (20-30 mg/kg; i.p.; daily; 21 days) delivers significant dose-dependent antitumor efficacy in a murine MV4-11 xenograft model, achieving 49.1% tumor growth inhibition at 30 mg/kg with no observable toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Acute myeloid leukemia mice (Female Balb/c-nu nude, 6-week injected with MV4-11 cells)[1]
Dosage: 20 mg/kg; 30 mg/kg
Administration: i.p.; daily; 20 days
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.
Molecular Weight

773.74

Formula

C38H33F6N3O6S
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HLC40 Related Classifications

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Help & FAQs
  • 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.

Keywords:

HLC40HLC 40HLC-40Histone MethyltransferaseWDR5ApoptosisCaspaseWD repeat protein-5WD40 repeat domain protein 5mll-rearranged leukemiahematologic malignanciesxenograft modelsMV4-11 cellsMOLM-13 cellsMLL1 complexCysLT1 receptorK562 cellsAML cellsInhibitorinhibitorinhibit

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