| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
WM-1119 (WM1119) is a novel, highly potent, and selective inhibitor of histone acetyltransferase KAT6A/B (lysine acetyltransferase) with potential anticancer activity. It competes with Ac-CoA by binding to the Ac-CoA binding site, and has a high oral bioavailability (F) of 56% in rats. WM-1119 inhibits KAT6A with an IC50 value of of 0.25 μM, and a KD value of 2 nM for KAT6A. 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.
| ln Vitro |
Without causing damage to DNA, WM-1119 triggers cell cycle exit and cellular senescence. Compared to KAT5 or KAT7, WM-1119 is 1,100- and 250-fold more active against KAT6A, respectively. As a result, it exhibits higher specificity for KAT6A than WM-8014. When MEFs are treated with WM-1119, they experience a G1 cell cycle arrest and a senescence phenotype resembling that of WM-8014. WM-1119 exhibits significantly higher activity in this cell-based assay compared to WM-8014, and at 1 μM, it can induce cell cycle arrest. As anticipated based on decreased protein binding, WM-1119 (IC50=0.25 μM) is nine times more potent than WM-8014 (IC50=2.3 μM) in suppressing the growth of EMRK1184 lymphoma cells in vitro[1].
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| ln Vivo |
With the exception of one mouse that does not respond, the cohorts that get WM-1119 four times a day have stopped the growth of their tumors by day 14. The spleen weights of the four times daily treated WM-1119 treatment group are significantly less than those of the vehicle-treated group. While administering WM-1119 three times a day reduces the tumour burden and spleen weight significantly, it is not as effective as administering it four times a day. WM-1119 is well-tolerated in mice; no widespread negative effects are seen, and there is no evidence of weight loss. Four times a day of WM-1119 treatment significantly reduces the proportion and total quantity of tumor cells[1].
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| References |
| Molecular Formula |
C18H13F2N3O3S
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| Molecular Weight |
389.37592959404
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| Exact Mass |
389.064
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| CAS # |
2055397-28-7
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| Related CAS # |
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| PubChem CID |
133080719
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
614
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=CC=CC=1F)(NNC(C1C=C(C=C(C2C=CC=CN=2)C=1)F)=O)(=O)=O
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| InChi Key |
QLXULUNLCRKWRD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H13F2N3O3S/c19-14-10-12(16-6-3-4-8-21-16)9-13(11-14)18(24)22-23-27(25,26)17-7-2-1-5-15(17)20/h1-11,23H,(H,22,24)
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| Chemical Name |
3-fluoro-N'-(2-fluorophenyl)sulfonyl-5-pyridin-2-ylbenzohydrazide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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