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STM2457

Catalog No. T9060 CAS 2499663-01-1

STM2457 is an inhibitor of the RNA methyltransferase METTL3 (IC50=16.9 nM) with selective and oral activity.STM2457 can be used in acute myeloid leukemia (AML) studies.

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STM2457, CAS 2499663-01-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 101.00
5 mg	In stock	$ 216.00
10 mg	In stock	$ 349.00
25 mg	In stock	$ 579.00
50 mg	In stock	$ 828.00
1 mL * 10 mM (in DMSO)	In stock	$ 237.00

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Purity: 99.06%

Purity: 98.90%

Purity: 97.77%

Purity: 97.44%

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Storage & Solubility Information

Description	STM2457 is an inhibitor of the RNA methyltransferase METTL3 (IC50=16.9 nM) with selective and oral activity.STM2457 can be used in acute myeloid leukemia (AML) studies.
In vitro	METHODS: Eight human acute myeloid leukemia cells AML were treated with STM2457 (0-100 μM) for 72 h. Cell proliferation was detected using CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay. RESULTS: STM2457-treated AML cell lines showed a significant reduction in growth after treatment in a concentration-dependent manner, with IC50s ranging from 0.6-10.3 μM. [1] METHODS: Human lung cancer cells A549 and H1975 were treated with STM2457 (1-5 μM) for 3-6 days and apoptosis was detected using Flow Cytometry. RESULTS: STM2457 induced apoptosis in A549 and H1975 cells. [2]
In vivo	METHODS: To assay anti-tumor activity in vivo, STM2457 (50 mg/kg) was administered intraperitoneally to NSG mice bearing xenografts derived from human AML patients once daily for twelve to fourteen days. RESULTS: Daily treatment with STM2457 resulted in impaired implantation and AML amplification in vivo and significantly prolonged mouse lifespan. [1] METHODS: To investigate the role of METTL3 in the pathogenesis of systemic lupus erythematosus (SLE), STM2457 (30 mg/kg) was administered intraperitoneally to a cGVHD lupus mouse model once every three days for ten weeks. RESULTS: METTL3 inhibition increased antibody production and exacerbated the lupus-like phenotype in cGVHD mice.METTL3 inhibition is involved in the pathogenesis of SLE by participating in the imbalance between CD4+ T cell activation and effector T cell differentiation. [3]

Molecular Weight	444.53
Formula	C25H28N6O2
CAS No.	2499663-01-1

Storage

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

Solubility Information

DMSO: 100 mM, Sonication is recommended.

References and Literature

1. Yankova E, et al. Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia. Nature. 2021 May;593(7860):597-601. 2. Xiao H, et al. Effects and translatomics characteristics of a small-molecule inhibitor of METTL3 against non-small cell lung cancer. J Pharm Anal. 2023 Jun;13(6):625-639. 3. Lu S, et al. m6A methyltransferase METTL3 programs CD4+ T-cell activation and effector T-cell differentiation in systemic lupus erythematosus. Mol Med. 2023 Apr 3;29(1):46.

Citations

1. Xu Q C, Tien Y C, Shi Y H, et al. METTL3 promotes intrahepatic cholangiocarcinoma progression by regulating IFIT2 expression in an m6A-YTHDF2-dependent manner. Oncogene. 2022: 1-12. 2. Zhao T, Zhao R, Yi X, et al. METTL3 promotes proliferation and myogenic differentiation through m6A RNA methylation/YTHDF1/2 signaling axis in myoblasts. Life Sciences. 2022: 120496. 3. Wang D, Wang D, Jin Q, et al.Suxiao Jiuxin Pill Alleviates Myocardial Ischemia/Reperfusion-Induced Autophagy via miR-193a-3p/ALKBH5 Pathway.Phytomedicine.2024: 155359.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Viral Compound Library Anti-Cancer Compound Library Hematonosis Compound Library Anti-Infection Compound Library Apoptosis Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

STM2457 2499663-01-1 Apoptosis Others leukaemia cancer autoimmune diseases inhibit myeloid STM 2457 Inhibitor STM-2457 inhibitor

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