A PARP1 inhibitor
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TIQ-A

Item No. 16112

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
thieno[2,3-c]isoquinolin-5(4H)-one
CAS Number
420849-22-5
Molecular Formula
C11H7NOS
Formula Weight
201.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS (pH 7.2) (1:8): 0.1 mg/mlDMSO: 10 mg/mlEthanol: 0.5 mg/ml
λmax
230, 341, 355 nm
SMILES
O=C1NC2=C(C=CS2)C3=C1C=CC=C3
InChi Code
InChI=1S/C11H7NOS/c13-10-8-4-2-1-3-7(8)9-5-6-14-11(9)12-10/h1-6H,(H,12,13)
InChi Key
LQJVOLSLAFIXSV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $36

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    1 mg

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    5 mg

    $253

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    10 mg

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    Cayman Chemical
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    Product Description

    Poly(ADP-ribose) polymerase 1 (PARP1) is a critical DNA repair enzyme involved in DNA single-strand break repair via the base excision repair pathway. PARP1 is triggered by DNA damage and its excessive activation has been proposed as a causative factor in many pathological conditions including ischemia and reperfusion injury, asthma-related inflammation, and atherogenesis.1,2,3 TIQ-A is a PARP1 inhibitor (IC50 = 450 nM in cultured mouse cortical neurons).1 It displays neuroprotective effects in cultured mouse cortical neurons injured by oxygen-glucose deprivation (IC50 = 0.15 µM). TIQ-A has been used to inhibit eosinophilic infiltration into airways of OVA-challenged mice and to induce the regression of atherosclerotic plaques in high-fat fed apolipoprotein E(-/-) mice.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chiagurgi, A., Meli, E., Calvani, M., et al. Novel isoquinolinone-derived inhibitors of poly(ADP-ribose) polymerase-1: Pharmacological characterization and neuroprotective effects in an in vitro model of cerebral ischemia. J. Pharmacol. Exp. Ther. 305(5), 943-949 (2014).

    2. Oumouna, M., Datta, R., Oumouna-Benachour, K., et al. Poly(ADP-ribose) polymerase-1 inhibition prevents eosinophil recruitment by modulating Th2 cytokines in a murine model of allergic airway inflammation: A potential specific effect on IL-5. J. Immunol. 177(9), 6489-6496 (2006).

    3. Hans, C.P., Zerfaoui, M., Naura, A.S., et al. Thieno[2,3-c]isoquinolin-5-one, a potent poly(ADP-ribose) polymerase inhibitor, promotes atherosclerotic plaque regression in high-fat diet-fed apolipoprotein E-deficient mice: Effects on inflammatory markers and lipid content. J. Pharmacol. Exp. Ther. 329(1), 150-158 (2009).