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MedKoo Cat#: 563775 | Name: GeA-69
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Chemical Structure

GeA-69
GeA-69
CAS#2143475-98-1

Theoretical Analysis

MedKoo Cat#: 563775

Name: GeA-69

CAS#: 2143475-98-1

Chemical Formula: C20H16N2O

Exact Mass: 300.1263

Molecular Weight: 300.36

Elemental Analysis: C, 79.98; H, 5.37; N, 9.33; O, 5.33

Price and Availability

Size Price Availability Quantity
5mg USD 250.00 2 Weeks
10mg USD 400.00 2 Weeks
25mg USD 750.00 2 Weeks
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Related CAS #
No Data
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
Product Data
Instruction
View handling instruction
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
Solvent mg/mL mM
Solubility
DMSO 92.5 307.96
Ethanol 10.0 33.29
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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
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.