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LEM-14

CAT: 0804-HY-114340-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-114340-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
NSD2/MMSET/WHSC1

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