WM-1119 | CAS#2055397-28-7 | KAT6A inhibitor

MedKoo Cat#: 407946 | Name: WM-1119

Description:

WARNING: This product is for research use only, not for human or veterinary use.

WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with Kd of 2 nM, WM-1119 is a reversible competitor of acetyl coenzyme A and inhibits MYST-catalysed histone acetylation. WM-1119 induces cell cycle exit and cellular senescence without causing DNA damage. WM-1119 arrests the progression of lymphoma in mice.

Chemical Structure

WM-1119

CAS#2055397-28-7

Theoretical Analysis

MedKoo Cat#: 407946

Name: WM-1119

CAS#: 2055397-28-7

Chemical Formula: C18H13F2N3O3S

Exact Mass: 389.0646

Molecular Weight: 389.38

Elemental Analysis: C, 55.52; H, 3.37; F, 9.76; N, 10.79; O, 12.33; S, 8.23

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 200.00	Ready to ship
50mg	USD 350.00	Ready to ship
100mg	USD 600.00	Ready to ship
200mg	USD 1,050.00	Ready to ship
500mg	USD 2,150.00	Ready to ship

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Related CAS #

No Data

Synonym

WM-1119; WM 1119; WM1119;

IUPAC/Chemical Name

Benzoic acid, 3-fluoro-5-(2-pyridinyl)-, 2-[(2-fluorophenyl)sulfonyl]hydrazide

InChi Key

QLXULUNLCRKWRD-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H13F2N3O3S/c19-14-10-12(16-6-3-4-8-21-16)9-13(11-14)18(24)22-23-27(25,26)17-7-2-1-5-15(17)20/h1-11,23H,(H,22,24)

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Acetylation of histones by lysine acetyltransferases (KATs) is essential for chromatin organization and function1. Among the genes coding for the MYST family of KATs (KAT5-KAT8) are the oncogenes KAT6A (also known as MOZ) and KAT6B (also known as MORF and QKF). KAT6A has essential roles in normal haematopoietic stem cells and is the target of recurrent chromosomal translocations, causing acute myeloid leukaemia. Similarly, chromosomal translocations in KAT6B have been identified in diverse cancers8. KAT6A suppresses cellular senescence through the regulation of suppressors of the CDKN2A locus, a function that requires its KAT activity. Loss of one allele of KAT6A extends the median survival of mice with MYC-induced lymphoma from 105 to 413 days11. These findings suggest that inhibition of KAT6A and KAT6B may provide a therapeutic benefit in cancer

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A21T06K08

View CoA: current batch, Lot#A20T12K10

QC Data

View QC data: current batch, Lot#A21T06K08

View QC data: current batch, Lot#A20T12K10

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

WM-1119 is a KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells.

In vitro activity:

Treatment of MEFs with WM-1119 resulted in cell cycle arrest in G1 and a senescence phenotype similar to that seen upon treatment with WM-8014 (Extended Data Fig. 8). 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. Reference: Nature. 2018 Aug;560(7717):253-257. https://pubmed.ncbi.nlm.nih.gov/30069049/

In vivo activity:

Treatment with WM-1119 three times per day led to a significant reduction in tumour burden and spleen weight, but was not as effective as treatment four times per day (Fig. 4d, f). WM-1119 was well-tolerated; mice showed no generalized ill effects and weight loss was not observed (Extended Data Fig. 10). WM-1119 treatment had no effect on haematocrit, erythrocytes or platelet numbers, but there was overall leukopenia (Extended Data Fig. 10). The proportion and overall number of tumour cells was substantially reduced by WM-1119 treatment (four times per day; Fig. 4g). Analysis by intracellular flow cytometry demonstrated a reduction in H3K9ac in tumour cells (P = 0.03; Extended Data Fig. 10). These results demonstrate that WM-1119 is effective in treating lymphoma in vivo. Reference: Nature. 2018 Aug;560(7717):253-257. https://pubmed.ncbi.nlm.nih.gov/30069049/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	30.0	76.97

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 389.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan BJ, Voss AK, Thomas T. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. PMID: 30069049.

In vitro protocol:

In vivo protocol:

1: A KAT6A/B Inhibitor Induces Senescence to Suppress Tumorigenesis. Cancer Discov. 2018 Sep;8(9):1061. doi: 10.1158/2159-8290.CD-RW2018-136. Epub 2018 Aug 10. PubMed PMID: 30097427. 2: Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan BJ, Voss AK, Thomas T. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. PubMed PMID: 30069049.