12 Apr [MCE]: New Small Molecules from MCE for April 2021
MCE (MedChemExpress) provides a wide range of lifescience biochemicals, including more than 25,000 bioactive compounds, recombinant proteins, dye reagents, peptides and natural compounds for laboratory and scientific use.
| • KRAS G12C Degrader LC-2 CAS No. : 2502156-03-6 LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines. |
50 specific libraries for high throughput screening (HTS) and high content screening (HCS). Optimized for drug screening and new indication research. |
| • Vitamin D Receptor Antagonist TEI-9648 CAS No. : 173388-21-1 TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research. |
Cell Signaling Pathway
|
| • Insulin Secretion Stimulator GIP, human (TFA) GIP, human TFA, a peptide hormone consisting of 42 amino acids, is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP, human TFA acts as an incretin hormone released from intestinal K cells in response to nutrient ingestion. |
• Recent Publication Citing used MCE
Nature. 2021 Mar;591(7850):477-481. |
| • Opioid Receptor Antagonist UFP-101 TFA UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect. |
• HDAC Inhibitor AES-135 AES-135, a hydroxamic acid-based HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM. |
Compound Screening Libraries
Other New Products This Month
PTOTAC Linkers
PROTAC linker connects a ligand to the target protein and a ligand to the E3 ubiquitin ligase. MCE possesses thousands of PROTAC linkers for PROTAC systhesis, which are three main types: PEGs-, Alkyl-Chains- and Alkyl/ether- based linkers