[CAS NO. 31083-55-3] PRT4165

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PRODUCTS SPECIFICATIONS [31083-55-3]

Catalog

SLK-S5315

Brand

Selleck

CAS

31083-55-3

DESCRIPTION [31083-55-3]

Overview

MDL	MFCD00435709
Molecular Weight	235.24
Molecular Formula	C15H9NO2
SMILES	O=C1C=2C(C(=O)C1=CC=3C=CC=NC3)=CC=CC2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	4.2510 mL	21.2549 mL	42.5098 mL
5 mM	0.8502 mL	4.2510 mL	8.5020 mL
10 mM	0.4251 mL	2.1255 mL	4.2510 mL
50 mM	-	-	-

Description

PRT4165 is a inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.

Targets

Bmi1/Ring1A ^[1]	BMI-1 ^[1] (Cell-free assay)
3.9 μM	3.9 μM

In vitro

PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation in vivo and in vitro. It inhibits the accumulation of all detectable ubiquitin at sites of DNA double-strand breaks (DSBs), the retention of several DNA damage response proteins in foci that form around DSBs, and the repair of the DSBs. PRT4165 inhibits both RNF2 and RING 1A, which are partially redundant paralogues that together account for the E3 ubiquitin ligase activity found in PRC1 complexes, but not RNF8 nor RNF168. U2OS cells treated with increasing concentrations of PRT4165 show increasing numbers of cells in G2/M.

References

[1] Alchanati I, et al. PLoS One. 2009, 4(12):e8104.
[2] Ismail IH, et al. J Biol Chem. 2013, 288(37):26944-54.
[3] Fenghua Bian, et al. Sci Rep. 2016, 6: 26061.

Synonyms

1H-Indene-1,3(2H)-dione, 2-(3-pyridinylmethylene)-

1,3-Indandione, 2-(3-pyridylmethylene)-

2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione

2-(3-Pyridylmethylene)-1,3-indandione

NSC 600157

PRT 4165

SML 1013

2-(Pyridin-3-ylmethylidene)indene-1,3-dione

2-[(Pyridin-3-yl)methylidene]-2,3-dihydro-1H-indene-1,3-dione

2-Pyridin-3-ylmethylene-indan-1,3-dione