COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor (antagonist) with IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd= 0.547 μM), thereby prolonging PARylation at DNA damage and trapping DNA repair factors.

Physicochemical Properties

Molecular Formula	C18H15NOS
Molecular Weight	293.382803201675
Exact Mass	293.09
Elemental Analysis	C, 73.69; H, 5.15; N, 4.77; O, 5.45; S, 10.93
CAS #	906439-72-3
PubChem CID	135443632
Appearance	Light yellow to yellow solid powder
LogP	4.9
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	3
Heavy Atom Count	21
Complexity	351
Defined Atom Stereocenter Count	0
SMILES	CC1=CC=C(C=C1)S/N=C/C2=C(C=CC3=CC=CC=C32)O
InChi Key	SFUAIBHPGDRCFL-XDHOZWIPSA-N
InChi Code	InChI=1S/C18H15NOS/c1-13-6-9-15(10-7-13)21-19-12-17-16-5-3-2-4-14(16)8-11-18(17)20/h2-12,20H,1H3/b19-12+
Chemical Name	1-[(E)-(4-methylphenyl)sulfanyliminomethyl]naphthalen-2-ol
Synonyms	COH-34; COH34; COH 34
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 Note: This product is not stable in solution, please use freshly prepared working solution for optimal results.
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

Targets	PARG ( IC50 = 0.37 nM )
ln Vitro	COH34 effectively eliminates cancer cells resistant to PARP inhibitors[1].
ln Vivo	COH34 shows antitumor activity and causes lethality in cancer cells with DNA repair defects in xenograft mouse cancer models[1].
References	[1]. Targeting dePARylation selectively suppresses DNA repair-defective and PARP inhibitor-resistant malignancies. Sci Adv. 2019 Apr 10;5(4):eaav4340.

Solubility Data

Solubility (In Vitro)

DMSO: ~16.7 mg/mL (~56.8 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.67 mg/mL (5.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (5.69 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 16.7 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	3.4085 mL	17.0427 mL	34.0855 mL
	5 mM	0.6817 mL	3.4085 mL	6.8171 mL
	10 mM	0.3409 mL	1.7043 mL	3.4085 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.