RBN012759

Names

[ Name ]:
RBN012759

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[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 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].

[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].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₂₃FN₂O₃S

[ Molecular Weight ]:
378.46

[ Storage condition ]:
-20°C

Related Compounds

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