FB23-2
FB23-2 is a potent FTO inhibitor. FB23-2 demonstrated the potent inhibitory impact in AML models. FB23-2 directly binds 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. Moreover, FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice. Collectively, our data suggest that FTO is a druggable target and that targeting FTO by small-molecule inhibitors holds potential to treat AML.
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Chemical Information
| Name | FB23-2 |
|---|---|
| Iupac Chemical Name | 2-((2,6-dichloro-4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-N-hydroxybenzamide |
| Synonyms | FB23-2; FB-23-2; FB 23-2; FB232; FB-232; FB 232; |
| Molecular Formula | C18H15Cl2N3O3 |
| Molecular Weight | 392.236 |
| Smile | O=C(NO)C1=CC=CC=C1NC2=C(Cl)C=C(C3=C(C)ON=C3C)C=C2Cl |
| InChiKey | ILHNIWOZZKIBNW-UHFFFAOYSA-N |
| InChi | InChI=1S/C18H15Cl2N3O3/c1-9-16(10(2)26-23-9)11-7-13(19)17(14(20)8-11)21-15-6-4-3-5-12(15)18(24)22-25/h3-8,21,25H,1-2H3,(H,22,24) |
| CAS Number | 2243736-45-8 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | 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 |
| Handling | |
| 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. |
| HS Code |
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| Mechanism | |
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| Clinical study |
1: Huang Y, Su R, Sheng Y, Dong L, Dong Z, Xu H, Ni T, Zhang ZS, Zhang T, Li C,
Han L, Zhu Z, Lian F, Wei J, Deng Q, Wang Y, Wunderlich M, Gao Z, Pan G, Zhong D,
Zhou H, Zhang N, Gan J, Jiang H, Mulloy JC, Qian Z, Chen J, Yang CG.
Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia.
Cancer Cell. 2019 Apr 15;35(4):677-691.e10. doi: 10.1016/j.ccell.2019.03.006.
PubMed PMID: 30991027.
2: Van Der Werf I, 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. Cancer Cell. 2019 Apr 15;35(4):540-541. doi:
10.1016/j.ccell.2019.03.011. PubMed PMID: 30991023.
Chemical Structure
