Signaling Pathway

PARP

PARP

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PARP is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. PARP1, PARP2, VPARP (PARP4), Tankyrase-1 and -2 (PARP-5a or TNKS, and PARP-5b or TNKS2) have a confirmed PARP activity. Others include PARP3, PARP6, TIPARP (or "PARP7"), PARP8, PARP9, PARP10, PARP11, PARP12, PARP14, PARP15, and PARP16. PARP is found in the cell’s nucleus. The main role is to detect and signal single-strand DNA breaks (SSB) to the enzymatic machinery involved in the SSB repair.

PARP Inhibitors & Modulators (28)

Product Name Catalog No. Brief Description
A-966492

HY-10614

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

AG14361

HY-12032

AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM.

AZ6102

HY-12975

AZ6102 is a potent TNKS1/2 inhibitor (IC50=3/1 nM) that has 100-fold selectivity against other PARP family enzymes (IC50: 0.5-3 μM) and shows 5 nM Wnt pathway inhibition in DLD-1 cells.

AZD-2461

HY-13536

AZD2461 is a novel PARP inhibitor, which has the potential to avoid the olaparib resistence mediated by Pgp.

BGP-15

HY-100828

BGP-15 is a PARP inhibitor, that can protect against heart failure and atrial fibrillation in mice.

BMN-673

HY-16106

BMN 673 is a novel PARP1/2 inhibitor with IC50 of 0.58 nM(PARP1); does not inhibit PARG and is highly sensitive to PTEN mutation.

BMN-673 8R,9S

HY-16106A

BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673.

BSI-201

HY-12015

BSI-201 (Iniparib; NSC-746045) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC).

E7449

HY-12418

E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2; enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.

G007-LK

HY-12438

G007-LK displays high selectivity toward tankyrases 1 and 2 with biochemical IC50 values of 46 nM and 25 nM, respectively, and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice.

INO-1001

HY-12022

INO-1001 a novel potent PARP inhibitor with an IC50 of 3 nM.

JW 55

HY-13968

JW 55 is an inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2).

MK-4827

HY-10619

MK-4827(Niraparib) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.

MK-4827 hydrochloride

HY-10619A

MK-4827(Niraparib) Hcl is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.

MK-4827 tosylate

HY-10619B

MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.

MN-64

HY-19351

MN-64 is a inhibitor of tankyrases, showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition.

Nicotinamide

HY-B0150

Nicotinamide (Vitamin B3) is a water-soluble vitamin and is part of the vitamin B group.

NMS-P118

HY-18954

NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor.

NVP-TNKS656

HY-13990

NVP-TNKS656(TNKS-656) is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2.

Olaparib

HY-10162

Olaparib (AZD2281,  KU0059436) is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1and PARP-2, respectively.