WM-1119 |
رقم الكتالوجGC18154
One-Click Copy Product Info
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WM-1119 هو مثبط قوي للغاية وانتقائي KAT6A ، مع IC من 0.25 ميكرومتر لـ KAT6A في خلايا الليمفوما ، قيم KD الملزمة لـ WM-1119 مع KAT6A ، KAT5 و KAT7 هي 2 نانومتر ، 2.2 ميكرومتر ، 0.5 ميكرومتر ، على التوالي
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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WM-1119, a potent KAT6 inhibitor with an IC50 value of 6.3µM, has KD values of 0.002µM, 2.2µM, and 0.5µM for KAT6A, KAT5, and KAT7, respectively [1]. WM-1119 demonstrates effective inhibitory potency for KAT6 through unique hydrophobic interactions enabled by the 3-fluoro-5-(pyridine-2-yl)benzoyl moiety, which engages Ile647 and Gly687 in addition to the conserved contacts with Arg660, Ser690, Ser693, Leu686, and Ile649[2]. WM-1119 has been widely used to increase CDKN2A expression and inhibit leukemic cell proliferation[3].
In vitro, WM-1119 treatment for 1 hour significantly inhibited IgE-stimulated β-hexosaminidase (β-hex) release from rat basophilic leukemia-2H3 (RBL-2H3) cells with an IC50 value of 33.57μM[4]. Treatment with 10µM WM-1119 for 48h significantly inhibited the viability of HepG2 and Huh7 cells, resulting in a decrease in the number of Edu-positive cells[5]. Treatment with WM-1119 at 1µM for 7 days significantly induced proliferation arrest of MT2 cells accompanied by a significant reduction in the number of cells in S and G2 phases[6].
In vivo, Intraperitoneal injection of WM-1119 at a dose of 50mg/kg four times daily for 14 days significantly inhibited lymphoma growth and reduced tumor burden and spleen weight in C57BL/6 mice[7]. For 21 consecutive days, 60mg/kg of WM-1119 was administered intraperitoneally four times a day, in combination with cisplatin (administered intraperitoneally once every three days; 5mg/kg), which significantly inhibited tumor growth in A2780 xenografts in mice and led to a reduction in nuclear β-catenin levels in tumor tissues[8].
References:
[1] Zheng T, Wang S, Liu W, et al. Targeting KAT6A/B as a new therapeutic strategy for cancer therapy[J]. Journal of Medicinal Chemistry, 2025, 68(2): 1002-1020.
[2] Xi Z, Wang J, Ge X, et al. Dancing with KAT6A: Current advances and therapeutic potential in oncology of KAT6A inhibitors[J]. Bioorganic Chemistry, 2026: 109533.
[3] Ling V Y, Jacquelin S, Straube J, et al. Targeting Control of Cell Cycle Enhances the Activity of Conventional Chemotherapy in Chemotherapy-Resistant Acute Myeloid Leukemia[J]. Blood, 2021, 138: 2241.
[4] Baell J B, Leaver D J, Hermans S J, et al. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth[J]. Nature, 2018, 560(7717): 253-257.
[5] Jin Y, Yang R, Ding J, et al. KAT6A is associated with sorafenib resistance and contributes to progression of hepatocellular carcinoma by targeting YAP[J]. Biochemical and Biophysical Research Communications, 2021, 585: 185-190.
[6] Sheridan M, Maqbool M A, Largeot A, et al. The small inhibitor WM-1119 effectively targets KAT6A-rearranged AML, but not KMT2A-rearranged AML, despite shared KAT6 genetic dependency[J]. Journal of hematology & oncology, 2024, 17(1): 91.
[7] Baell J B, Leaver D J, Hermans S J, et al. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth[J]. Nature, 2018, 560(7717): 253-257.
[8] Liu W, Zhan Z, Zhang M, et al. KAT6A, a novel regulator of β-catenin, promotes tumorigenicity and chemoresistance in ovarian cancer by acetylating COP1[J]. Theranostics, 2021, 11(13): 6278.
| Cell experiment [1]: | |
Cell lines | SW480 cells |
Preparation Method | SW480 cells were cultured in DMEM medium containing 10% fetal bovine serum (FBS) and 1% penicilin-streptomycin at 37℃ in the presence of 5% CO2. WM-1119 (1µM) was added to the culture medium and cultured for 24 hours, while an equal volume of DMSO was added to the control group, and cell viability was analyzed. |
Reaction Conditions | 1µM; 24h |
Applications | WM-1119 treatment significantly decreased the cell viability of SW480 cells. |
| Animal experiment [2]: | |
Animal models | Female nu/nu mice |
Preparation Method | Female nu/nu mice were housed in a specific pathogen-free (SPF) animal house maintained at 23°C with a 12h light/dark cycle and free access to water and food. A total of 1×106 A2780 cells were subcutaneously inoculated into the hind flanks of 5-week-old female nu/nu mice. Cisplatin and WM-1119 were intraperitoneally injected into mice 7 days after tumor cell inoculation at 5mg/kg and 60mg/kg, respectively. Cisplatin was injected every three days for 21 days, and WM-1119 was injected 4 times per day. The lengths and widths of the tumors were measured every 5 days, and the tumor volume was calculated according to the formula: volume= (length×width2)/2. |
Dosage form | 60mg/kg; four times a day for 21 days; i.p. |
Applications | WM-1119 treatment in combination with cisplatin led to a significant reduction in tumor burden in mice with A2780 xenografts, without affecting body weight loss. |
References: | |
| 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 |
| الذوبان | 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 | 513.6 μL | 2.5682 mL | 5.1364 mL |
| 10 mM | 256.8 μL | 1.2841 mL | 2.5682 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 saline, 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
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)