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FB23-2

Catalog No. T7138 CAS 2243736-45-8

FB23-2 is a potent and selective mRNA N6-methyladenosine (m6A) demethylase FTO inhibitor(IC50 : 2.6 μM).

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FB23-2, CAS 2243736-45-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 59.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 168.00
25 mg	In stock	$ 283.00
50 mg	In stock	$ 418.00
100 mg	In stock	$ 623.00
500 mg	In stock	$ 1,330.00
1 mL * 10 mM (in DMSO)	In stock	$ 107.00

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Purity: 98.91%

Purity: 98%

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Description	FB23-2 is a potent and selective mRNA N6-methyladenosine (m6A) demethylase FTO inhibitor(IC50 : 2.6 μM).
Targets&IC50	FTO:2.6 μM (IC50)
In vitro	FB23-2 directly bind to FTO and selectively inhibit FTO's m6A demethylase activity. Mimicking FTO depletion, FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro[1].
In vivo	FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice[1].
Cell Research	Quantitation of FB23 and FB23-2 in AML cells: NB4 and MONOMAC6 cells were treated with 10 μM FB23 or FB23-2 for 24 hr, respectively. Viable cells were distinguished with 0.1% trypan blue, counted and then harvested with PBS by several washings. Cells were diluted into 100 μl with 50% (v/v) water/methanol and followed by several shock freeze-thaw cycles. The supernatants were collected for analysis. The Ultimate 3000 system coupled with a TSQ Quantiva mass spectrometer was applied to determine the cellular concentration of compound FB23 and FB23-2. Analytes were separated on a XSELECT? HSS T3 column (100 mm × 3.0 mm, 2.5 μm). The mobile phases used for elution were (A) 0.1% (v/v) formic acid/water and (B) 0.1% (v/v) formic acid/acetonitrile. The mass spectrometer was operated in the negative MRM mode. Parent-to-product transitions were m/z 375.1→339.1, 375.1→298.1 for FB23, and m/z 390.3→318.0, 390.3→289.9 for FB23-2, respectively[1].
Animal Research	The NSGS mice were bred and subjected to the xeno-transplantation model. For the AML mouse model, 0.2 × 10^6 MONOMAC6 cells were directly transplanted into NSGS mice via tail vein. After 10 days, FB23-2 (2 mg/kg/day) and DMSO vehicle were intraperitoneally injected into the mice for a continuous 10 days. The mice were euthanized by CO2 inhalation if they exhibited classical AML symptoms including hunched posture, paralysis, and reduced body weight. Meanwhile, the PB, spleen, and liver samples were collected for further analysis[1].

Molecular Weight	392.24
Formula	C18H15Cl2N3O3
CAS No.	2243736-45-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 62.5 mg/mL (159.34 mM)

References and Literature

1. Huang Y , Su R , Sheng Y , et al. Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia[J]. Cancer Cell, 2019, 35(4):677-691.e10. 2. Inge V D W , Jamieson C . The Yin and Yang of RNA Methylation: An Imbalance of Erasers Enhances Sensitivity to FTO Demethylase Small-Molecule Targeting in Leukemia Stem Cells[J]. Cancer Cell, 2019, 35(4):540-541.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Apoptosis Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library Hematonosis Compound Library Anti-Obesity Compound Library

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Keywords

FB23-2 2243736-45-8 Apoptosis Others FB23 2 AML leukemia acute anti-proliferation Inhibitor FB232 m6A myeloid mRNA inhibit demethylase FB-23-2 inhibitor

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