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WM-3835 (WM3835) is a novel and potent lysine acetyltransferase HBO1 (KAT7) inhibitor with potential anticancer activity. It binds directly to the acetyl-CoA binding site of HBO1 33. HBO1 (KAT7 or MYST2) is a histone acetyltransferase that acetylates H3 and H4 histones. HBO1 overexpression promotes OS cell growth in vitro and in vivo. WM-3835 was able to potently suppressed OS cell proliferation and migration, and led to apoptosis activation. Furthermore, intraperitoneal injection of a single dose of WM-3835 potently inhibited OS xenograft growth in SCID mice.
| ln Vitro |
pOS-1 cell viability is inhibited by WM-3835 (1-25 uM; 24-96 hours) in a concentration-dependent manner [1]. In pOS-1 cells, WM-3835 (5 uM; 72 h) dramatically raises the proportion of TUNEL-positive nuclei and initiates apoptosis [1]. In pOS-1 cells, WM-3835 (5 μM; 24 hours) reduces the expression of MYLK-HOXA9 mRNA [1]. Inhibiting H4K12ac-H3K14ac in a dose-dependent manner is WM-3835 (1-25 uM). Total H3 and H4 histones as well as the expression of the HBO1 protein are not altered by WM-3835 [1]. When it comes to HBO1-KO pOS-1 cells, koHBO1-1 and koHBO1-2, and HBO1-low human osteoblasts, WM-3835 (5 μM) cannot cause apoptosis or decreased viability [1].
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| ln Vivo |
The growth of pOS-1 xenografts in SCID mice is effectively inhibited by WM-3835 (10 mg/kg/day; i.p.; for 21 days) [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: primary human OS (pOS-1) Cell Tested Concentrations: 1, 5, 10, 25 uM Incubation Duration: 24, 48, 72, 96 hrs (hours) Experimental Results: A certain concentration inhibits pOS-1 cells Vitality-dependent manner. Exhibits significant anti-survival activity for at least 48 hrs (hours), showing time dependence. Apoptosis analysis[1] Cell Types: pOS-1 Cell Tested Concentrations: 5 uM Incubation Duration: 72 hrs (hours) Experimental Results: Activation of apoptosis and significant increase in TUNEL-positive nuclei. RT-PCR[1] Cell Types: pOS-1 Cell Tested Concentrations: 5 uM Incubation Duration: 24 hrs (hours) Experimental Results: MYLK-HOXA9 mRNA expression was downregulated. |
| Animal Protocol |
Animal/Disease Models: SCID (severe combined immunodeficient) mouse (18-19 g, female) [1] with pOS1 cells
Doses: 10 mg/kg Route of Administration: IP; daily; continued for 21 days Experimental Results: Effective inhibition of pOS-1 xenografts grow. |
| References |
[1]. Yan-Yang Gao, et al. The histone acetyltransferase HBO1 functions as a novel oncogenic gene in osteosarcoma. Theranostics. 2021 Mar 4;11(10):4599-4615.
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| Molecular Formula |
C20H17FN2O4S
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|---|---|
| Molecular Weight |
400.4234
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| CAS # |
2229025-70-9
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| SMILES |
S(C1=C([H])C([H])=C([H])C(=C1[H])O[H])(N([H])N([H])C(C1=C(C(C([H])([H])[H])=C([H])C(C2C([H])=C([H])C([H])=C([H])C=2[H])=C1[H])F)=O)(=O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~250 mg/mL (~624.34 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.19 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.19 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.19 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 | 2.4974 mL | 12.4869 mL | 24.9738 mL | |
| 5 mM | 0.4995 mL | 2.4974 mL | 4.9948 mL | |
| 10 mM | 0.2497 mL | 1.2487 mL | 2.4974 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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