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HH-2853
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Catalog No. T202024Cas No. 2202678-04-2
Alias HH2853, HH 2853
HH-2853 is a potent inhibitor targeting EZH1/2, demonstrating significant antitumor activity. Its IC50 values for both wild-type and mutant EZH2 range from 2.21-5.36 nM, comparable to tazemetostat. HH-2853 is more effective against EZH1, with an IC50 of 9.26 nM, notably lower than tazemetostat's 58.43 nM. However, at concentrations up to 10 μM, it exhibits minimal inhibitory activity on 36 types of histone-modifying enzymes. On the cellular level, HH-2853 effectively inhibits mono-, di-, and tri-methylation of H3K27 in various cancer cell lines with wild-type or mutant EZH2, without affecting other methylation types on histone H3 at concentrations up to 10 μM. Additionally, HH-2853 significantly reduces cell viability in multiple cancer cell lines carrying EZH2 GOF mutations or SWI/SNF complex alterations, and demonstrates superior antitumor effects compared to tazemetostat in several tumor xenograft models at equivalent doses.
HH-2853
Copy Product Info😃Good
Catalog No. T202024Alias HH2853, HH 2853Cas No. 2202678-04-2
HH-2853 is a potent inhibitor targeting EZH1/2, demonstrating significant antitumor activity. Its IC50 values for both wild-type and mutant EZH2 range from 2.21-5.36 nM, comparable to tazemetostat. HH-2853 is more effective against EZH1, with an IC50 of 9.26 nM, notably lower than tazemetostat's 58.43 nM. However, at concentrations up to 10 μM, it exhibits minimal inhibitory activity on 36 types of histone-modifying enzymes. On the cellular level, HH-2853 effectively inhibits mono-, di-, and tri-methylation of H3K27 in various cancer cell lines with wild-type or mutant EZH2, without affecting other methylation types on histone H3 at concentrations up to 10 μM. Additionally, HH-2853 significantly reduces cell viability in multiple cancer cell lines carrying EZH2 GOF mutations or SWI/SNF complex alterations, and demonstrates superior antitumor effects compared to tazemetostat in several tumor xenograft models at equivalent doses.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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| Description | HH-2853 is a potent inhibitor targeting EZH1/2, demonstrating significant antitumor activity. Its IC50 values for both wild-type and mutant EZH2 range from 2.21-5.36 nM, comparable to tazemetostat. HH-2853 is more effective against EZH1, with an IC50 of 9.26 nM, notably lower than tazemetostat's 58.43 nM. However, at concentrations up to 10 μM, it exhibits minimal inhibitory activity on 36 types of histone-modifying enzymes. On the cellular level, HH-2853 effectively inhibits mono-, di-, and tri-methylation of H3K27 in various cancer cell lines with wild-type or mutant EZH2, without affecting other methylation types on histone H3 at concentrations up to 10 μM. Additionally, HH-2853 significantly reduces cell viability in multiple cancer cell lines carrying EZH2 GOF mutations or SWI/SNF complex alterations, and demonstrates superior antitumor effects compared to tazemetostat in several tumor xenograft models at equivalent doses. |
| Synonyms | HH2853, HH 2853 |
| Molecular Weight | 611.66 |
| Formula | C31H36F3N7O3 |
| Cas No. | 2202678-04-2 |
| Smiles | O=C(NCC=1C(=O)NC(=CC1OC)C)C2=CC3=C(C=CN3C(=C2C)C(N4CCN(CC4)CC(F)(F)F)C)C5=NN=C(C=C5)C |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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