LEM-14

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].

Product Specifications

CAS Number

[1814881-70-3]

Product Name Alternative

AZD6140; AR-C 126532XX

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Apoptosis; Histone Methyltransferase

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/lem-14.html

Purity

98.02

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C1C(C2=C(CCCC2)S3)=C3NC(CN4CCN(C([C@H]5CC6=CC=CC=C6C(O5)=O)=O)CC4)=N1

Molecular Formula

C25H26N4O4S

Molecular Weight

478.56

Precautions

H302, H315, H319

References & Citations

[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.|[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.