2. Epigenetics Apoptosis
  3. Histone Acetyltransferase Apoptosis
  4. WM-3835

WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.

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WM-3835 Chemical Structure

WM-3835 Chemical Structure

CAS No. : 2229025-70-9

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Based on 2 publication(s) in Google Scholar

WM-3835 Related Antibodies

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

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Description

WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice[1].

IC50 & Target

HBO1

 

In Vitro

WM-3835 (1-25 uM; 24-96 hours) inhibits pOS-1 cell viability in a concentration-dependent manner[1].
WM-3835 (5 uM; 72 h) activates cell apoptosis and significantly increases TUNEL-positive nuclei in pOS-1 cells[1].
WM-3835 (5 μM; 24 hours) downregulates MYLK-HOXA9 mRNA expression in pOS-1 cells[1].
WM-3835 (1-25 uM) suppresses H4K12ac-H3K14ac in a dose-dependent manner. WM-3835 does not alter the expressions of HBO1 protein and total H3, H4 histones[1].
WM-3835 (5 μM) fails to induce apoptosis and reduction of viability in HBO1-KO pOS-1 cells, koHBO1-1 and koHBO1-2, HBO1-low human osteoblasts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

WM-3835 Related Antibodies

Cell Viability Assay[1]

Cell Line: Primary human OS (pOS-1) cells
Concentration: 1, 5, 10, 25 uM
Incubation Time: 24, 48, 72, 96 hours
Result: Inhibited pOS-1 cell viability in a concentration-dependent manner.
Exerted a significant anti-survival activity at least 48 h, displaying a time-dependent manner.

Apoptosis Analysis[1]

Cell Line: pOS-1 cells
Concentration: 5 uM
Incubation Time: 72 hours
Result: Activated cell apoptosis and significantly increases TUNEL-positive nuclei.

RT-PCR[1]

Cell Line: pOS-1 cells
Concentration: 5 uM
Incubation Time: 24 hours
Result: Downregulated MYLK-HOXA9 mRNA expression.
In Vivo

WM-3835 (10 mg/kg/day; ip; for21 days) potently inhibits pOS-1 xenograft growth in SCID mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice (18-19 g, female) with pOS1 cells[1]
Dosage: 10 mg/kg
Administration: IP; daily; for 21 days
Result: Potently inhibited pOS-1 xenograft growth.
Molecular Weight

400.42

Formula

C20H17FN2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(C2=CC=CC=C2)=CC(C)=C1F)NNS(=O)(C3=CC=CC(O)=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (624.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.78%

SDS (393 KB)

COA (247 KB) HNMR (249 KB) RP-HPLC (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4974 mL 12.4869 mL 24.9738 mL 62.4344 mL
5 mM 0.4995 mL 2.4974 mL 4.9948 mL 12.4869 mL
10 mM 0.2497 mL 1.2487 mL 2.4974 mL 6.2434 mL
15 mM 0.1665 mL 0.8325 mL 1.6649 mL 4.1623 mL
20 mM 0.1249 mL 0.6243 mL 1.2487 mL 3.1217 mL
25 mM 0.0999 mL 0.4995 mL 0.9990 mL 2.4974 mL
30 mM 0.0832 mL 0.4162 mL 0.8325 mL 2.0811 mL
40 mM 0.0624 mL 0.3122 mL 0.6243 mL 1.5609 mL
50 mM 0.0499 mL 0.2497 mL 0.4995 mL 1.2487 mL
60 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0406 mL
80 mM 0.0312 mL 0.1561 mL 0.3122 mL 0.7804 mL
100 mM 0.0250 mL 0.1249 mL 0.2497 mL 0.6243 mL
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WM-3835 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WM-38352229025-70-9WM3835WM 3835Histone AcetyltransferaseApoptosisHATsHATHBO1KAT7MYST2acetyl-CoAosteosarcomaOS) cell proliferationmigrationinvasionpOS-1MYLK-HOXA9H4K12acH3K14acInhibitorinhibitorinhibit

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