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RBN012759

  Cat. No.:  DC39102   Featured
Chemical Structure
2360851-29-0
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More than 5000 active chemicals with high quality for research!
Field of application
RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2360851-29-0
SMILES: O=C1NC(CS[C@H]2CC[C@H](O)CC2)=NC3=C1C(F)=CC(OCC4CC4)=C3
Formula: C19H23FN2O3S
M.Wt: 378.46
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants[1].
Target: PARP14:<3 nM (IC50) PARP4:10 μM (IC50) PARP5a:8 μM (IC50) PARP5b:10 μM (IC50) PARP6:4 μM (IC50) PARP7:4 μM (IC50) PARP8:20 μM (IC50) PARP10:1 μM (IC50) PARP11:1 μM (IC50) PARP12:5 μM (IC50) PARP15:3 μM (IC50) PARP16:6 μM (IC50)
In Vivo: RBN012759 (500 mg/kg BID; p.o.) is well-tolerated in mice with repeat dosing[1]. RBN012759 (100 mg/kg; p.o.) exhibits moderate orally bioavailability (30%) and short plasma half-life (0.4 h) due to moderate clearance (54 mL/min/kg) and low steady-state volume of distribution (1.4 L/kg) in mice[1].
In Vitro: RBN012759 (0.01-10 μM) decreases the MAR/PAR signal corresponding to PARP14 self MARylation and stabilizes PARP14 protein in a dose-dependent manner in human primary macrophages[1]. RBN012759 (0.1-10 μM) reduces IL-4 stimulated cytokine secretion in human primary macrophages[1].
References: [1]. Schenkel L, et, al. A potent and selective PARP14 inhibitor decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants. AACR Annual Meeting 2020
MSDS
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MSDS_20491_DC39102_2360851-29-0
COA
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Cat. No. Product name Field of application
DC73217 Thioparib Thioparib is a next-generation potent, orally bioavailable pan-PARP inhibitor with IC50 of 0.13/0.006 nM (PARP1/2), overcomes multiple PARPi resistance both in vitro and in vivo.
DC72591 OUL232 OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC50=7.8 nM), as well as the first PARP12 inhibitor ever reported.
DC70175 AEP07 AEP07 (AEP 07) is a selective small molecule inhibitor of PARP4 (vPARP) inhibitor with IC50 of 0.8 uM, >12-fold selective over other PARP family members.
DC45193 DR2313 DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo.
DC39102 RBN012759 RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.
DC11022 OUL35 OUL35 (NSC39047) is a potent and selective inhibitor of mono-ADP-ribosyltransferase PARP10/ARTD10 with IC50 of 330 nM, displays remarkable selectivity towards ARTD10 over other enzymes in the human protein family.
DC11504 GeA-69 GeA-69(GeA69) is a potent, selective, allosteric, cell-active PARP14 macrodomain 2 (MD2) inhibitor with Kd of 0.86 uM in ITC assays.
DC10056 AZ9482 AZ9482, a potent and selective PARP inhibitor featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine.
DC7046 A-966492 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
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