WM-8014 (WM8014; MOZ-IN3; MOZ-IN-3) is a novel, potent and prototypical inhibitor of MOZ (IC50 = 55 nM) which is a member of histone acetyltransferases with anticancer activity. It is also a highly potent inhibitor of KAT6A with IC50 of 0.008 μM. WM-8014 competes with acetyl-CoA (Ac-CoA) for binding to the Ac-CoA binding site.

Physicochemical Properties

Molecular Formula	C20H17FN2O3S
Molecular Weight	384.423987150192
Exact Mass	384.094
CAS #	2055397-18-5
PubChem CID	133053564
Appearance	White to off-white solid powder
LogP	4.1
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	5
Heavy Atom Count	27
Complexity	595
Defined Atom Stereocenter Count	0
SMILES	S(C1C=CC=CC=1)(NNC(C1=C(C(C)=CC(C2C=CC=CC=2)=C1)F)=O)(=O)=O
InChi Key	PHHZKBMVRPULAW-UHFFFAOYSA-N
InChi Code	InChI=1S/C20H17FN2O3S/c1-14-12-16(15-8-4-2-5-9-15)13-18(19(14)21)20(24)22-23-27(25,26)17-10-6-3-7-11-17/h2-13,23H,1H3,(H,22,24)
Chemical Name	[1,1'-Biphenyl]-3-carboxylic acid, 4-fluoro-5-methyl-, 2-(phenylsulfonyl)hydrazide
Synonyms	WM-8014 MOZ-IN-3WM 8014 MOZ-IN 3WM8014 MOZ-IN3
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	WM-8014 (Compound 36) has an IC50 of 55 nM, making it an inhibitor of MOZ. With an IC50 of 1.6 μM and 551 nM, respectively, WM-8014 suppresses proliferation and induces cell senescence. Additionally, WM-8014 decreased the MOZ gene Cdc6's mRNA encoding by 65.1%[1].
References	[1]. ARYL SULFONOHYDRAZIDES. WO2016198507 A1.

Solubility Data

Solubility (In Vitro)

DMSO : ≥ 250 mg/mL (~650.33 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6013 mL	13.0066 mL	26.0132 mL
	5 mM	0.5203 mL	2.6013 mL	5.2026 mL
	10 mM	0.2601 mL	1.3007 mL	2.6013 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.