WM-1119 |
| Catalog No.GC18154 |
A highly potent, selective KAT6A/B inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2055397-28-7
Sample solution is provided at 25 µL, 10mM.
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Target: lysine acetyltransferases, KAT6A(MOZ), KAT6B(MORF/QKF)
WM-1119 induces cell cycle exit and cellular senescence without causing DNA damage. Senescence is INK4A/ARF-dependent and is accompanied by changes in gene expression that are typical of loss of KAT6A function. WM-1119, which has increased bioavailability, arrests the progression of lymphoma in mice
Data:
Treatment with WM-1119 arrests lymphoma growth.
Growth inhibition assays of Eμ-Myc lymphoma cell line EMRK1184 treated with WM-1119 and WM-8014 at the doses indicated.
KD(KAT6A)=0.002μM KD(KAT5) = 2.2μM KD(KAT7) = 0.5 μM
References
1. Baell JB, et al. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257.
Animal experiment: | Mice[1]Male C57BL/6-albino (B6(Cg)-Tyrc-2J/J) mice are injected intravenously with 100,000 EMRK1184 cells transfected with a luciferase-expression construct. Lymphoma growth is monitored. Three days after the lymphomacell transplant, all mice show luciferase activity, which indicate the expansion of lymphoma cells. Mice are then divided randomly into WM-1119-treatment with different conentrations (1, 2.5, 5, 10 μM) and vehicle-control groups. Because WM-1119 is rapidly cleared after intraperitoneal injection, with the plasma concentration decreasing to below 1 μM after 4-6 h cohorts of mice are injected every 8 h (three times per day, two cohorts of three mice per treatment group) or every 6 h (four times per day, two cohorts of three and six mice per treatment group)[1]. |
References: [1]. Baell JB et al. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257. | |
| Cas No. | 2055397-28-7 | SDF | |
| Chemical Name | 2-fluoro-N'-(3-fluoro-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide | ||
| Canonical SMILES | O=C(NNS(=O)(C1=CC=CC=C1F)=O)C2=CC(C3=NC=CC=C3)=CC(F)=C2 | ||
| Formula | C18H13F2N3O3S | M.Wt | 389.38 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.25 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5682 mL | 12.8409 mL | 25.6819 mL |
| 5 mM | 0.5136 mL | 2.5682 mL | 5.1364 mL |
| 10 mM | 0.2568 mL | 1.2841 mL | 2.5682 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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