GeA-69
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MedKoo CAT#: 563775

CAS#: 2143475-98-1

Description: GeA-69 is a novel selective allosteric inhibitor targeting macrodomain 2 of poly-adenosine-diphosphate-ribose polymerase 14.


Chemical Structure

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GeA-69
CAS# 2143475-98-1

Theoretical Analysis

MedKoo Cat#: 563775
Name: GeA-69
CAS#: 2143475-98-1
Chemical Formula: C20H16N2O
Exact Mass: 300.13
Molecular Weight: 300.361
Elemental Analysis: C, 79.98; H, 5.37; N, 9.33; O, 5.33

Price and Availability

Size Price Availability Quantity
1g USD 3950
2g USD 7650
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Synonym: GeA-69; GeA69; GeA 69

IUPAC/Chemical Name: N-(2-(9H-carbazol-1-yl)phenyl)acetamide

InChi Key: LDPDVNYCIOHPGF-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H16N2O/c1-13(23)21-18-11-4-2-7-14(18)16-9-6-10-17-15-8-3-5-12-19(15)22-20(16)17/h2-12,22H,1H3,(H,21,23)

SMILES Code: CC(NC1=CC=CC=C1C2=CC=CC3=C2NC4=C3C=CC=C4)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM.
In vitro activity: The macrodomain recruitment was significantly decreased in cells pre-treated with 50 µM GeA-69 and completely prevented in cells exposed to 250 µM GeA-69. As expected, the negative control MnK2-68 did not interfere with PARP14 MD2 recruitment and further, GeA-69 did not affect the recruitment of an alternative macrodomain containing protein, YFP-ALC1. Although a high inhibitor concentration had to be applied to completely prevent PARP14 MD2 recruitment to DNA damage sites, these experiments proved that GeA-69 engages PARP14 MD2 in intact cells. Reference: ACS Chem Biol. 2017 Nov 17;12(11):2866-2874. https://pubmed.ncbi.nlm.nih.gov/28991428/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 92.5 307.96
Ethanol 10.0 33.29

Preparing Stock Solutions

The following data is based on the product molecular weight 300.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Schuller M, Riedel K, Gibbs-Seymour I, Uth K, Sieg C, Gehring AP, Ahel I, Bracher F, Kessler BM, Elkins JM, Knapp S. Discovery of a Selective Allosteric Inhibitor Targeting Macrodomain 2 of Polyadenosine-Diphosphate-Ribose Polymerase 14. ACS Chem Biol. 2017 Nov 17;12(11):2866-2874. doi: 10.1021/acschembio.7b00445. Epub 2017 Oct 19. PMID: 28991428; PMCID: PMC6089342.
In vitro protocol: 1. Schuller M, Riedel K, Gibbs-Seymour I, Uth K, Sieg C, Gehring AP, Ahel I, Bracher F, Kessler BM, Elkins JM, Knapp S. Discovery of a Selective Allosteric Inhibitor Targeting Macrodomain 2 of Polyadenosine-Diphosphate-Ribose Polymerase 14. ACS Chem Biol. 2017 Nov 17;12(11):2866-2874. doi: 10.1021/acschembio.7b00445. Epub 2017 Oct 19. PMID: 28991428; PMCID: PMC6089342.
In vivo protocol: TBD

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1: Schuller M, Riedel K, Gibbs-Seymour I, Uth K, Sieg C, Gehring AP, Ahel I, Bracher F, Kessler BM, Elkins JM, Knapp S. Discovery of a Selective Allosteric Inhibitor Targeting Macrodomain 2 of Polyadenosine-Diphosphate-Ribose Polymerase 14. ACS Chem Biol. 2017 Nov 17;12(11):2866-2874. doi: 10.1021/acschembio.7b00445. Epub 2017 Oct 19. PubMed PMID: 28991428; PubMed Central PMCID: PMC6089342.