parp-14

RBN-3143 is a potent inhibitor of NAD+-competitive catalytic PARP14 (IC50= 4 nM), which inhibits ADP-ribosylation mediated by PARP14 and stabilizes PARP14 in cell lines, demonstrating research potential for lung inflammation.

PARP14 inhibitor H10 is a selective inhibitor against PARP14 with IC50 of 490 nM

RBN012759 inhibits PARP14 protein with an IC50 value of 0.003 μM and is more than 300-fold selective over all PARP family members.[2]

GeA-69 (GeA69) is a selective and allosteric PARP14 macrodomain 2 (MD2) inhibitor (Kd: 0.86 μM in ITC assays).

OUL232 is a potent single ARTs PARP7, PARP10, PARP11, PARP12, PARP14 and PARP15 inhibitor for cancer and tumour research.

PARP14 inhibitor1 (compound Q22) is a selective inhibitor of PARP14 with an IC50 of 5.52 nM. It also exhibits anti-inflammatory properties and has a half-life of 182 minutes in mouse liver microsomes. This compound is applicable for atopic dermatitis research.

PARP14 inhibitor2 (Compound 3) is an orally active and highly selective PARP14 inhibitor with an IC50 value of less than 30 nM. It effectively inhibits the mono ADP-ribosyltransferase activity of PARP14 and modulates IFN-γ and IL-4 signaling, thereby reversing pro-tumor macrophage polarization and suppressing anti-tumor inflammatory responses. PARP14 inhibitor2 holds potential for research in PARP14-related conditions such as tumors, atopic dermatitis, and autoimmune diseases.

PARP10-IN-3 is a potent and selective mono-Adp-ribotransferase PARP10 inhibitor that inhibits human PARP10 (IC50:480 nM). PARP10-IN-3 also inhibited human PARP2 and human PARP15 with IC50 values of 1.7 μM.

PARP10-IN-2 is a potent inhibitor of PARP10, a mono-ADP-ribosyltransferase, with an IC50 value of 3.64 μM for human PARP10. It also inhibits PARP2 and PARP15, with IC50 values of 27 μM and 11 μM, respectively.

TIQ-A is a PARP1 inhibitor which 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 includi

ART-IN-1 (compound 7) is a selective inhibitor of PARP with IC50 values of 19 μM for PARP2, 22 μM for TNKS2, 2.4 μM for PARP10, >100 μM for PARP14, and 1.1 μM for PARP15 [1].

ARTD10/PARP10-IN-1 is a potent PARP inhibitor of the mono-ADP ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly ADP-ribose polymerase-1 (ARTD1/PARP1), with potential anticancer and antitumour activity for the study of prostate and breast cancers.

ARTD10/PARP10-IN-2 is a potent, non-selective inhibitor of mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1, exhibiting IC50 values of 2.0 μM and 9.7 μM, respectively.

OUL245, a 7-Hydroxy derivative, selectively inhibits PARP2 with an IC50 of 44 nM. Additionally, it exhibits inhibition against other PARP and TNKS enzymes, displaying IC50 values ranging from 2.9 to 8.8 μM.

YCH1899, an orally active PARP inhibitor, demonstrates potent inhibition of PARP1/2 with an IC50 of less than 0.001 nM. It shows marked antiproliferative efficacy against Olaparib-resistant (Capan-1/OP) and Talazoparib-resistant (Capan-1/TP) cells with IC50 values of 0.89 nM and 1.13 nM, respectively. Moreover, YCH1899 possesses favorable pharmacokinetic attributes in rats [1].

AG14361 is an effective inhibitor of PARP1 (Ki<5 nM).

Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with anti-endometrial cancer activity. It exhibits inhibitory concentration (IC50) values of 74 nM for PARP1, 109 nM for PARP2, and 1.4 μM for microtubules/tubulin. Tubulin/PARP-IN-1 induces apoptosis and autophagy, causing cell cycle arrest at the G2/M phase.