PARP

PARP inhibitors block poly(ADP-ribose) polymerases (PARPs), enzymes that mark DNA damage and recruit repair proteins. PARP1 and PARP2 bind DNA single-strand breaks and attach poly(ADP-ribose) chains to themselves and to nearby chromatin proteins. Cells lacking breast cancer susceptibility proteins 1 or 2 (BRCA1, BRCA2), and therefore defective in homologous recombination, are highly sensitive to PARP inhibition. This synthetic lethal relationship, reported in 2005, has shaped much of the research on DNA repair inhibitors. Olaparib, niraparib, veliparib and talazoparib target the catalytic domains of PARP1 and PARP2, and 3-aminobenzamide is an early benzamide inhibitor. XAV 939 instead inhibits tankyrases 1 and 2 (TNKS1, TNKS2), which stabilizes axin in Wnt signaling studies.

Items 1-25 of 236

  • Olaparib
    Cat. No.
    A10111

    Olaparib (AZD2281)

    Synonyms: KU-0059436; AZD2281

    Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.

    5 mg
    $25.00
    10 mg
    $35.00
    All 10 sizes
  • XAV 939
    Cat. No.
    A10994

    XAV 939

    XAV 939 is a TNKS inhibitor (IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively).

    5 mg
    $40.00
    10 mg
    $50.00
    All 7 sizes
  • Rucaparib (AG-014699) phosphate
    Cat. No.
    A10045

    Rucaparib (AG-014699) phosphate

    Synonyms: PF-01367338; AG-014447 (as free base)

    AG-014699 (Rucaparib) is a PARP inhibitor that inhibits poly(ADP-ribose) polymerase (PARP) is a key enzyme in DNA repair.

    1 mg
    $25.00
    2 mg
    $40.00
    All 9 sizes
  • Talazoparib
    Cat. No.
    A11243

    Talazoparib (BMN673)

    Synonyms: BMN-673; LT-673

    BMN-673 is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity.

    2 mg
    $30.00
    5 mg
    $50.00
    All 9 sizes
  • PJ 34 hydrochloride
    Cat. No.
    A12665

    PJ 34 hydrochloride

    Synonyms: PJ34

    PJ 34 hydrochloride is a potent inhibitor of poly(ADP-ribose) polymerase (PARP) (EC50 = 20 nM).

    5 mg
    $30.00
    10 mg
    $40.00
    All 7 sizes
  • AG14361
    Cat. No.
    A10046

    AG14361

    AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.

    1 mg
    $40.00
    2 mg
    $60.00
    All 8 sizes
  • Iniparib
    Cat. No.
    A10164

    Iniparib (BSI-201)

    Synonyms: NSC-746045; IND-71677; BSI-201

    BSI-201 is a potent inhibitor of PARP-1 and has been shown to cross the blood-brain barrier.

    5 mg
    $40.00
    10 mg
    $55.00
    All 8 sizes
  • 3-Aminobenzamide
    Cat. No.
    A10475

    3-Aminobenzamide

    Synonyms: 3-AB

    3-Aminobenzamide is a novel PARP inhibitor, known to sensitize cells to radiation in vitro by inhibiting the repair of DNA damage.

    100 mg
    $20.00
    250 mg
    $30.00
    All 4 sizes
  • Rucaparib
    Cat. No.
    A14182

    Rucaparib

    Synonyms: AG-014699; PF-01367338

    Rucaparib is a potent inhibitor of purified full-length human PARP-1 and shows higher inhibition of cellular PARP in LoVo and SW620 cells.

    2 mg
    $35.00
    5 mg
    $55.00
    All 9 sizes
  • PJ34
    Cat. No.
    A15215

    PJ34

    PJ34 is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.

    5 mg
    $35.00
    10 mg
    $40.00
    All 5 sizes
  • G007-LK
    Cat. No.
    A15528

    G007-LK

    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,

    1 mg
    $40.00
    2 mg
    $55.00
    All 8 sizes
  • Niraparib tosylate
    Cat. No.
    A16618

    Niraparib tosylate

    Synonyms: MK-4827 tosylate

    Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively.

    2 mg
    $30.00
    5 mg
    $55.00
    All 8 sizes
  • Talazoparib tosylate
    Cat. No.
    A20238

    Talazoparib tosylate

    Synonyms: BMN 673ts

    Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.

    2 mg
    $30.00
    5 mg
    $50.00
    All 8 sizes
  • INO-1001
    Cat. No.
    A20680

    INO-1001

    Synonyms: IN01001

    INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor.

    2 mg
    $40.00
    5 mg
    $80.00
    All 5 sizes
  • A-966492
    Cat. No.
    A10019

    A-966492

    A-966492 displayed high potency against the poly(ADP-ribose) polymerase-1 (PARP-1) enzyme with a K(i) of 1 nM and an EC(50) of 1 nM in a whole cell assay.

    1 mg
    $20.00
    2 mg
    $25.00
    All 9 sizes
  • TC-E 5001
    Cat. No.
    A11454

    TC-E 5001

    TC-E 5001 is dual tankyrase (TNKS) inhibitor (Kd values are 79 and 28 nM for TNKS1 and TNKS2 respectively, IC50 = 33 nM for TNKS2) that is devoid of activity at PARP1 and PARP2 (IC50 >19 uM). Inhibits Wnt signaling and stabilizes Axin2 levels.

    5 mg
    $420.00
    10 mg
    $740.00
    All 5 sizes
  • AZD-2461
    Cat. No.
    A12393

    AZD-2461

    AZD2461 is a novel and potent PARP inhibitor with lower affinity to P-glycoprotein.

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes
  • UPF 1069
    Cat. No.
    A12750

    UPF 1069

    UPF 1069 is a selective poly(ADP-ribose) polymerase (PARP) 2 inhibitor (IC50 values are 0.3 and 8.0 μM for PARP-2 and PARP-1 respectively).

    5 mg
    $25.00
    10 mg
    $40.00
    All 6 sizes
  • JW 55
    Cat. No.
    A13731

    JW 55

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

    5 mg
    $20.00
    10 mg
    $30.00
    All 7 sizes
  • WIKI4
    Cat. No.
    A14283

    WIKI4

    WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2.

    5 mg
    $25.00
    10 mg
    $40.00
    All 7 sizes
  • ME0328
    Cat. No.
    A14309

    ME0328

    ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.

    5 mg
    $40.00
    10 mg
    $60.00
    All 6 sizes
  • TAK1/MAP4K2 inhibitor 1
    Cat. No.
    A14371

    TAK1/MAP4K2 inhibitor 1

    TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor targeting transforming growth factor β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), exhibiting IC₅₀ values of 41.1 nM and 18.2 nM, respectively.

    2 mg
    $170.00
    5 mg
    $215.00
    All 7 sizes
  • BMN-673 8R,9S
    Cat. No.
    A15024

    BMN-673 8R,9S

    Synonyms: (8R,9S)-BMN-673

    BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673. BMN 673 is a novel PARP inhibitor with IC50 of 0.58 nM.

    1 mg
    $240.00
    5 mg
    $320.00
    All 4 sizes

Items 1-25 of 236

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