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Cat. No.: HY-183354

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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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화학식: C₃₈H₃₃F₆N₃O₆S
분자량:773.74

보관:

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

HLC40 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

Caspase 3

All Histone Methyltransferase Isoforms :

All Caspase Isoforms :

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.

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	T_1/2	C_max
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.

Chemical Information

분자량 773.74
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. He L, et al. Structure-based design of the approved drug zafirlukast identifies HLC40 as a potent WDR5 WIN-site inhibitor with antitumor efficacy. Bioorg Chem. 2026;176:109869. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
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HLC40

All Histone Methyltransferase Isoforms

All Caspase Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

HLC40 Related Classifications

HY-183354 Related Classifications