1. Epigenetics
  2. Histone Acetyltransferase

WM-1119 

Cat. No.: HY-102058 Purity: >98.0%
Handling Instructions

WM-1119 is a highly potent, selective KAT6A/B inhibitor, with an IC50 of 0.25 μM for KAT6A, a KD of 2 nM for KAT6A, a KD of 2.2 μM for KAT5, and a KD of 0.5 μM for KAT7.

For research use only. We do not sell to patients.

WM-1119 Chemical Structure

WM-1119 Chemical Structure

CAS No. : 2055397-28-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 209 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 290 In-stock
Estimated Time of Arrival: December 31
25 mg USD 590 In-stock
Estimated Time of Arrival: December 31
50 mg USD 890 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

WM-1119 is a highly potent, selective KAT6A/B inhibitor, with an IC50 of 0.25 μM for KAT6A, a KD of 2 nM for KAT6A, a KD of 2.2 μM for KAT5, and a KD of 0.5 μM for KAT7.

IC50 & Target

IC50: 0.25 μM (KAT6A), KD: 2 nM (KAT6A), 2.2 μM (KAT5), 0.5 μM (KAT7)[1].

In Vitro

WM-1119 induces cell cycle exit and cellular senescence without causing DNA damage. WM-1119 is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively, and so shows greater specificity for KAT6A than does WM-8014. The testing of WM-1119 at 1 μM and 10 μM against a pharmacological panel of 159 diverse biological targets reveal no affinity. Treatment of MEFs with WM-1119 results in cell cycle arrest in G1 and a senescence phenotype similar to that seen upon treatment with WM-8014. Notably, the activity of WM-1119 in this cell-based assay is an order of magnitude greater than WM-8014 and WM-1119 is able to induce cell cycle arrest at 1 μM. Treatment with WM-8014 or WM-1119 inhibits the proliferation of the EMRK1184 lymphoma cells in vitro, WM-1119 (IC50=0.25 μM) is ninefold more active than WM-8014 (IC50=2.3 μM), as expected on the basis of reduced protein binding[1].

In Vivo

By day 14, the cohorts that are treated four times per day with WM-1119 have arrested tumour growth, with the exception of one mouse that does not respond. Spleen weights in the WM-1119-treatment group (treated four times per day) are substantially lower than spleen weights in the vehicle-treated group, and not significantly different from those of tumour-free eight-weekold mice. Treatment with WM-1119 three times per day leads to a significant reduction in tumour burden and spleen weight, but is not as effective as treatment four times per day. WM-1119 is well-tolerated; mice show no generalized ill effects and weight loss is not observed. WM-1119 treatment has no effect on haematocrit, erythrocytes or platelet numbers, but there is overall leukopenia. The proportion and overall number of tumour cells is substantially reduced by WM-1119 treatment (four times per day)[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (385.23 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

References
Animal Administration
[1]

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].

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

References
Molecular Weight

389.38

Formula

C₁₈H₁₃F₂N₃O₃S

CAS No.

2055397-28-7

SMILES

O=C(NNS(=O)(C1=CC=CC=C1F)=O)C2=CC(C3=NC=CC=C3)=CC(F)=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
WM-1119
Cat. No.:
HY-102058
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WM-1119

Cat. No.: HY-102058