1814881-70-3
Chemical Structure
LEM-14
- CAS No.: 1814881-70-3
- Formula:C25H26N4O4S
- Molecular Weight:478.56
IUPAC Name: (R)-2-((4-(1-oxoisochromane-3-carbonyl)piperazin-1-yl)methyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(1H)-one
InChIKey: ZJOXWRFJOUWUKX-GOSISDBHSA-N
SMILES: O=C1C(C2=C(CCCC2)S3)=C3NC(CN4CCN(C([C@H]5CC6=CC=CC=C6C(O5)=O)=O)CC4)=N1
Biological Activity: LEM-14 is a potent and selective NSD2 inhibitor with an IC50 of 132 µM. LEM-14 has very weak activitv against NSD1 and has no activity against NSD3. LEM-14 inhibits fibrotic gene expression in ND but not DIO BMDMs. LEM-14 combined with ionizing radiation (IR) enhances the apoptosis rate and reduces the colony-formation ability of CRC cells. LEM-14 exhibits enhanced anti-tumor efficacy in Balb/c nude mice bearing LoVo cell xenografts when combined with ionizing radiation. LEM-14 has the potential for the research of multiple myeloma and colorectal cancer[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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LEM-14 | 98.02% | LEM-14 is a potent and selective NSD2 inhibitor with an IC50 of 132 µM. LEM-14 has very weak activitv against NSD1 and has no activity against NSD3. LEM-14 inhibits fibrotic gene expression in ND but not DIO BMDMs. LEM-14 combined with ionizing radiation (IR) enhances the apoptosis rate and reduces the colony-formation ability of CRC cells. LEM-14 exhibits enhanced anti-tumor efficacy in Balb/c nude mice bearing LoVo cell xenografts when combined with ionizing radiation. LEM-14 has the potential for the research of multiple myeloma and colorectal cancer. | ||||||||||||||||||||
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References
- [1]. Shen Y, et al. Identification of LEM-14 inhibitor of the oncoprotein NSD2. Biochem Biophys Res Commun. 2019 Jan 1;508(1):102-108. [Content Brief]
- [2]. Mangum K, et al. The Histone Methyltransferase Whsc1 Regulates Tgfb-driven Macrophage to Myofibroblast Transition During Normal Wound Healing[J]. Journal of Vascular Surgery, 2023, 78(3): e19.
- [3]. Li X, et al. NSD2 methylates AROS to promote SIRT1 activation and regulates fatty acid metabolism-mediated cancer radiotherapy. Cell Rep. 2023 Oct 31;42(10):113126. [Content Brief]
