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

RBN012759 

Cat. No.: HY-136979
Handling Instructions

RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 can decrease pro-tumor macrophage function and elicit inflammatory responses in tumor explants.

For research use only. We do not sell to patients.

RBN012759 Chemical Structure

RBN012759 Chemical Structure

CAS No. : 2360851-29-0

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5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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100 mg USD 3400 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 can decrease pro-tumor macrophage function and elicit inflammatory responses in tumor explants[1].

IC50 & Target[1]

PARP14

<3 nM (IC50)

PARP1

>100 μM (IC50)

PARP2

>100 μM (IC50)

PARP3

>100 μM (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)

PARP9

>100 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 is >300-fold selective over the monoPARPs and >1000-fold selective over the polyPARPs[1].
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[[email protected]]2CC[[email protected]](O)CC2)=NC3=C1C(F)=CC(OCC4CC4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

RBN012759RBN 012759RBN-012759PARPpoly ADP ribose polymerasePARP14pro-tumormacrophageinflammatorycancerInhibitorinhibitorinhibit

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