| Bioactivity | SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC50s of 5 and 13 nM, respectively, in an in vitro assay. | ||||||||||||
| Target | IC50: 5 nM (SHMT1), 13 nM (SHMT1) | ||||||||||||
| Invitro | SHIN1 (RZ-2994) inhibits human SHIN1 SHMT1/2 with IC50s of 5 and 13 nM, respectively in an in vitro assay. SHIN1 inhibits the growth of SHMT2 deletion HCT-116 cells with an IC50 of 10 nM. SHIN1 (RZ-2994) inhibits SHMT1/2 in HCT-116 cells. SHIN1 (RZ-2994) is particularly active against B-cell malignancies. SHIN1 blocks cell growth through a progressive depletion of purines, leading to loss of nucleotide triphosphates[1]. | ||||||||||||
| Name | SHIN1 | ||||||||||||
| CAS | 2146095-85-2 | ||||||||||||
| Formula | C24H24N4O2 | ||||||||||||
| Molar Mass | 400.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ducker GS, 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. |