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Merck
CN

420201

JMJD2 Inhibitor, 5-carboxy-8HQ

The JMJD2 Inhibitor, 5-carboxy-8HQ, also referenced under CAS 5852-78-8, controls the biological activity of JMJD2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

JMJD2 Inhibitor, 5-carboxy-8HQ, JHDM Inhibitor I, Histone Lysine Demethylase Inhibitor II, 5-carboxy-8HQ, IOX1

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关于此项目

经验公式(希尔记法):
C10H7NO3
化学文摘社编号:
分子量:
189.17
UNSPSC Code:
12352200
MDL number:
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

orange

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C10H7NO3/c12-8-4-3-7(10(13)14)6-2-1-5-11-9(6)8/h1-5,12H,(H,13,14)

InChI key

JGRPKOGHYBAVMW-UHFFFAOYSA-N

General description

A cell-permeable, 5-carboxy-8-hydroxyquinoline that acts as a 2-oxoglutarate competitive inhibitor of JMJD (IC50 = 200 nM against JMJD2E in a FDH coupled assay). It demonstrates higher selectivity than 2.4-PDCA against other 2-OG oxygenases (IC50 = 2.4 µM, 1.7 µM, 20.5 µM, and 14.3 µM for JMJD2E, JMJD2A, FIH, and PHD2, respectively, in a MALDI-TOF MS assay). Additionally, it is shown to inhibit H3K9me3 demethylation (IC50 = 86.5 µM) in JMJD2A-transfected HeLa cells in a cellular demethylase assay, dose-dependently.




This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the IOX1 probe summary on the SGC website.

Packaging

Packaged under inert gas

Preparation Note

Following reconstiution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Hamada, S., et al. 2010. J. Med. Chem.53, 5629.
King, D.N.F., et al. 2010. PLoS One5, e15535.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Regulatory Review (Z)


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



历史批次信息供参考:

分析证书(COA)

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