WM-1119

SKU: orb1225730

Description

WM-1119 (WM1119) is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with Kd of 2 nM, shows greate bioavailability and specificity for KAT6A than WM-8014; displays 1,100-fold and 250-fold selectivity over KAT5 and KAT7, respectively; causes cell cycle arrest in G1 and senescence phenotype similar to WM-8014; demonstrates growth inhibition assays in lymphoma cell line EMRK1184 (IC50=0.25 uM, 10-fold potency than WM-8014), increases levels of Cdkn2a and Cdkn2b mRNA and p16INK4a and p19ARF protein, as well as a delayed increase in Cdkn1a mRNA; arrests lymphoma growth in vivo without effect on haematocrit, erythrocytes or platelet numbers.

Key Properties

• CAS Number: 2055397-28-7
• MW: 389.377
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₃F₂N₃O₃S
• SMILES: O=C(NNS(=O)(C1=CC=CC=C1F)=O)C2=CC(C3=NC=CC=C3)=CC(F)=C2
• Target: HAT
• Solubility: DMSO: ≥150 mg/mL (385.23 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• 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. 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. The proportion and overall number of tumour cells is substantially reduced by WM-1119 treatment (four times per day).
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• 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. 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-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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

WM1119 | WM 1119

Quick Database Links

Gene Symbol

HAT