HBI-2375
Based on 1 Customer Validation
HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8+ cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM.
For research use only. We do not sell to patients.
- Purity: 98.06%
- CAS No.: 2982574-79-6
- Formula: C29H36ClF2N9O2
- Molecular Weight:616.11
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
HBI-2375 inhibits the WDR5 WIN-site protein-protein interaction with an IC50 of 5 nM[1].
HBI-2375 reduces the viability of MV4:11 MLL-rearranged acute myeloid leukemia cells with a GI50 of 3200 nM[1].
HBI-2375 potently inhibits WDR5 in a cell-free biochemical assay with an IC50 of 4.48 nM[2].
HBI-2375 inhibits MV4-11 leukemia cell proliferation with an average IC50 of 3.17 µM in CTG assays[2].
HBI-2375 inhibits hERG in a cell-based assay with an IC50 of 17 µM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 2982574-79-6
-
Appearance Solid
-
Molecular Weight 616.11
-
Formula C29H36ClF2N9O2
-
Color White to off-white
-
SMILES
ClC1=C(C)C(F)=C(N)C=C1C(NC(C=C(N2C=C(C(N3CCN(C)CC3)=O)N=N2)C(F)=C4)=C4N5C[C@@H](C)N(C)[C@@H](C)C5)=O
-
Synonyms
HYBI-084
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 20 mg/mL (32.46 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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
-
Data Sheet (279 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
-
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. 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 | 1.6231 mL | 8.1154 mL | 16.2309 mL | 40.5772 mL |
| 5 mM | 0.3246 mL | 1.6231 mL | 3.2462 mL | 8.1154 mL | |
| 10 mM | 0.1623 mL | 0.8115 mL | 1.6231 mL | 4.0577 mL | |
| 15 mM | 0.1082 mL | 0.5410 mL | 1.0821 mL | 2.7051 mL | |
| 20 mM | 0.0812 mL | 0.4058 mL | 0.8115 mL | 2.0289 mL | |
| 25 mM | 0.0649 mL | 0.3246 mL | 0.6492 mL | 1.6231 mL | |
| 30 mM | 0.0541 mL | 0.2705 mL | 0.5410 mL | 1.3526 mL |
- HBI-2375
- 2982574-79-6
- HYBI-084
- HBI2375
- HBI 2375
- HYBI084
- HYBI 084
- WDR5
- Potassium Channel
- WIN-site
- MLL1-WDR5 complex
- glioblastoma
- acute myeloid leukemia
- MLL1 histone methyl transferase
- MV4:11 MLL-rearranged acute myeloid leukemia cells
- CD8+ cytotoxic T lymphocyte
- H3K4 methylation
- AML mouse models
- Inhibitor
- inhibitor
- inhibit