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Merck
CN

SML2267

Sigma-Aldrich

GeA-69

≥98% (HPLC)

Synonym(s):

N-[2-(9H-Carbazol-1-yl)phenyl]-acetamide

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About This Item

Empirical Formula (Hill Notation):
C20H16N2O
CAS Number:
Molecular Weight:
300.35
UNSPSC Code:
12352200
NACRES:
NA.77
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Assay

≥98% (HPLC)

form

powder

color

off-white to brown

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

CC(NC1=CC=CC=C1C2=CC=CC3=C2NC4=CC=CC=C43)=O

InChI key

LDPDVNYCIOHPGF-UHFFFAOYSA-N

Biochem/physiol Actions

GeA-69 is a selective allosteric inhibitor of macrodomain 2 of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14), an anti-apoptotic pro-survival protein associated with inflammatory diseases and several types of cancer. GeA-69 exhibited a KD of 860 nM in ITC experiments. GeA-69 was shown to be an allosteric inhibitor of adenosine diphosphate ribose (ADPR) binding to PARP14 macrodomain 2 and to prevent recruitment of the PAPP14 macrodomain 2 to DNA damage sites.
Selective allosteric inhibitor of PARP14 macrodomain 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Marion Schuller et al.
ACS chemical biology, 12(11), 2866-2874 (2017-10-11)
Macrodomains are conserved protein interaction modules that can be found in all domains of life including in certain viruses. Macrodomains mediate recognition of sequence motifs harboring adenosine diphosphate ribose (ADPR) modifications, thereby regulating a variety of cellular processes. Due to

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