A PARG inhibitor
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PDD00017273

Item No. 19511

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(1,3-dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide
CAS Number
1945950-21-9
Molecular Formula
C23H26N6O4S2
Formula Weight
514.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
λmax
227 nm
SMILES
O=S(C1=CC=C(N(CC2=CC(C)=NN2C)C(N3CC4=CN=C(C)S4)=O)C(C3=O)=C1)(NC5(CC5)C)=O
InChi Code
InChI=1S/C23H26N6O4S2/c1-14-9-16(27(4)25-14)12-28-20-6-5-18(35(32,33)26-23(3)7-8-23)10-19(20)21(30)29(22(28)31)13-17-11-24-15(2)34-17/h5-6,9-11,26H,7-8,12-13H2,1-4H3
InChi Key
IFWUBRBMMNTBRZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

    $120

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    Product Description

    PDD00017273 is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor (IC50 = 26 nM in an enzyme assay).1 It maintains persistence of nuclear PAR chains in HeLa cells induced by the DNA damaging agent methylmethanesulfonate (MMS; IC50 = 37 nM). PDD00017273, in combination with MMS, increases nuclear phosphorylated H2AX (γH2AX) intensity, a marker of DNA double strand breaks, in MCF-7 cells in a concentration-dependent manner. It reduces clonogenic growth of ZR-75-1 and MDA-MB-436 cells but not HCC1937 cells (IC50s = 0.2, 0.8, and >10 μM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. James, D.I., Smith, K.M., Jordan, A.M., et al. First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib. ACS Chem Biol. 11(11), 3179-3190 (2016).