1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. RBN012759

RBN012759 

目录号: HY-136979 纯度: 99.88%
产品使用指南

RBN012759 是一种有效的,选择性和具有口服活性的 PARP14 抑制剂,IC50 值 <3 nM,比对 monoPARPs 的选择性高 300 倍,比对 polyPARPs 的选择性高 1000 倍。RBN012759 可以降低肿瘤前巨噬细胞的功能并引起肿瘤外植体的炎症反应。

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RBN012759 Chemical Structure

RBN012759 Chemical Structure

CAS No. : 2360851-29-0

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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].

IC50 & Target[1]

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].

Molecular Weight

378.46

Formula

C₁₉H₂₃FN₂O₃S

CAS No.

2360851-29-0

SMILES

O=C1NC(CS[C@H]2CC[C@H](O)CC2)=NC3=C1C(F)=CC(OCC4CC4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

References
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Keywords:

RBN012759RBN 012759RBN-012759PARPpoly ADP ribose polymerasePARP14pro-tumormacrophageinflammatorycancerInhibitorinhibitorinhibit

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