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Merck
CN

SML4383

ALKBH1-IN-16

≥98% (HPLC)

Synonym(s):

DNA 6mA Demethylase ALKBH1 Inhibitor 16, N-Hydroxy-1-(5-((3-(trifluoromethoxy)benzyl)oxy)pyrimidin-2-yl)-1H-pyrazole-4-carboxamide

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About This Item

Empirical Formula (Hill Notation):
C16H12F3N5O4
Molecular Weight:
395.29
UNSPSC Code:
12352200
eCl@ss:
32160701
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

-10 to -25°C

Biochem/physiol Actions

ALKBH1-IN-16 is a cell-permeant hydroxamate analog that effectively competes with α-KG to suppress ALKBH1 (KD = 3.27 µM and IC50 = 1.696 µM), a DNA demethylase. By engaging ALKBH1, ALKBH1-IN-16 prevents its interaction with DNA, increasing N6-Methyladenine (6mA) levels in cellular DNA and mimicking the effects of ALKBH1 suppression on gene regulation and signaling. Furthermore, ALKBH1-IN-16 inhibits the growth of U251 brain cancer cells (IC50 = 12.92 µM) and, at higher doses, targets COX-2, HDAC2, and HDAC7 (IC50 = 1.45, 8.74, and 18.62 µM, respectively), showcasing its wider inhibitory impact on enzymes linked to inflammation and gene expression.


Pictograms

Exclamation mark

Signal Word

Warning

Hazard Codes

Precautionary Statements

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable



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