PeptideDB

SHMT-IN-2

CAS: 2102681-49-0 F: C22H24F3N5O W: 431.45

SHMT-IN-2 is a stereo specific inhibitor of human SHMT1/2 with IC50 values of 13 nM and 66 nM for SHMT1 and SHMT2, respe
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Bioactivity SHMT-IN-2 is a stereo specific inhibitor of human SHMT1/2 with IC50 values of 13 nM and 66 nM for SHMT1 and SHMT2, respectively. SHMT-IN-2 can block the growth of many human cancer cells, and has sensitivity for B-cell lymphomas[1].
Target IC50: 2800 nM (SHMT1); IC50: 36 nM (SHMT2)
Invitro SHMT-IN-2 (compound 2) can inhibit cell growth with cellular IC50 values of 2800 nM and 36 nM for SHMT1 and SHMT2, respectively[1]. SHMT-IN-2 (30 μM) shows the growth sensitivity with the median IC50 was 4 μM to a panel of nearly 300 human cancer cell lines (with IC50 values of 1.72 μM and 1.73 μM for CCRF-CEM and HT,respectively), cell lines of B-cell lymphoma origin were enriched in the more sensitive half of cells[1].
Name SHMT-IN-2
CAS 2102681-49-0
Formula C22H24F3N5O
Molar Mass 431.45
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Reference [1]. regory S Ducker, et al. Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):11404-11409.