HLC40
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.71%
- Formula: C38H33F6N3O6S
- Molecular Weight:773.74
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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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Appearance Solid
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Molecular Weight 773.74
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Formula C38H33F6N3O6S
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Color White to off-white
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (129.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2924 mL | 6.4621 mL | 12.9242 mL | 32.3106 mL |
| 5 mM | 0.2585 mL | 1.2924 mL | 2.5848 mL | 6.4621 mL | |
| 10 mM | 0.1292 mL | 0.6462 mL | 1.2924 mL | 3.2311 mL | |
| 15 mM | 0.0862 mL | 0.4308 mL | 0.8616 mL | 2.1540 mL | |
| 20 mM | 0.0646 mL | 0.3231 mL | 0.6462 mL | 1.6155 mL | |
| 25 mM | 0.0517 mL | 0.2585 mL | 0.5170 mL | 1.2924 mL | |
| 30 mM | 0.0431 mL | 0.2154 mL | 0.4308 mL | 1.0770 mL | |
| 40 mM | 0.0323 mL | 0.1616 mL | 0.3231 mL | 0.8078 mL | |
| 50 mM | 0.0258 mL | 0.1292 mL | 0.2585 mL | 0.6462 mL | |
| 60 mM | 0.0215 mL | 0.1077 mL | 0.2154 mL | 0.5385 mL | |
| 80 mM | 0.0162 mL | 0.0808 mL | 0.1616 mL | 0.4039 mL | |
| 100 mM | 0.0129 mL | 0.0646 mL | 0.1292 mL | 0.3231 mL |
HLC40 Related Classifications
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