rp4

Xenipentone is a biochemical.

XRP44X (XRP 44X) is a potent inhibitor of Ras-Net (Elk-3) pathway.

48740 RP (RP 55779) is an antagonist of platelet-activating factor.

Pyrimethamine (Pirimecidan) is a competitive inhibitor of dihydrofolate reductase (DHFR), used as an antimalarial drug.

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8/2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

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.

Indican (Indoxyl-β-D-glucoside) is a natural protective compound that is used to protect the liver.

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]

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.

Casimersen (SRP-4045) is an antisense oligonucleotide in the phosphorodiamidate morpholino oligomer subclass. It binds to exon 45 of dystrophin pre-mRNA, skipping the exon to restore the open-reading frame, resulting in a functional but internally truncated dystrophin protein. Casimersen is used in Duchenne muscular dystrophy (DMD) research.

Golodirsen (SRP-4053) is a phosphorodiamidate morpholino oligomer (PMO) designed to selectively bind to exon 53 of dystrophin pre-mRNA, used in the investigation of Duchenne muscular dystrophy (DMD).

BMS-986020 (AM152) is a selective LPA1 antagonist.

BMS-986020 sodium (AM152 sodium) is a high-affinity LPA1 (Lysophosphatidic Acid Receptor 1) antagonist for investigating idiopathic pulmonary fibrosis, slowing the rate of decline in forced vital capacity (FVC) and pulmonary function. BMS-986020 inhibits bile acid and phospholipid transporters (BSEP, MRP4, MDR3), altering bile homeostasis.

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.

Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM/2.1 nM) is a selective PARP1/PARP2 inhibitor.

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

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].

Ceefourin 1 is a highly selective multidrug resistance protein 4 (MRP4) inhibitor.

PU 23 is an inhibitor of multidrug-resistant protein 4 (MRP4).

Girolline (RP 49532) inhibits protein biosynthesis and exhibits antitumor activity.