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WM-1119 Histone Acetyltransferase inhibitor

Cat.No.S8776

WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively.
WM-1119 Histone Acetyltransferase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 389.38

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Quality Control

Batch: S877601 DMSO]78 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.89%
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99.89

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (200.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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 ddH2O, 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.
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Chemical Information, Storage & Stability

Molecular Weight 389.38 Formula

C18H13F2N3O3S

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2055397-28-7 -- Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C(C(=C1)F)S(=O)(=O)NNC(=O)C2=CC(=CC(=C2)C3=CC=CC=N3)F

Mechanism of Action

Targets/IC50/Ki
KAT6A
(Cell-free assay)
0.002 μM(Kd)
KAT7
(Cell-free assay)
0.5 μM(Kd)
KAT5
(Cell-free assay)
2.2 μM(Kd)
In vitro

Treatment of MEFs with WM-1119 resulted in cell cycle arrest in G1 and a senescence phenotype. Treatment with this compound inhibits the proliferation of the EMRK1184 lymphoma cells in vitro. This treatment results in increased levels of Cdkn2a and Cdkn2b mRNA and p16INK4a and p19ARF proteins, as well as a delayed increase in Cdkn1a mRNA.

In vivo

WM-1119 is effective in treating lymphoma in vivo while its treatment has no effect on haematocrit, erythrocytes or platelet numbers, but there was overall leukopenia.

References

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