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SCP1 inhibitor T-62 (T-62) is a specific, small molecule covalent inhibitor of small CTD phosphatase 1 (SCP1), reduces transcription factor REST protein level HEK293 cells.
NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.
K306 is a small molecule agonist that specifically targets SH2-containing 5' inositol phosphatase 1 (SHIP1), an enzyme involved in regulating cellular signaling pathways. SHIP1 is a lipid phosphatase that hydrolyzes the 5' phosphate of phosphatidylinositol-3,4,5-trisphosphate (PIP3), converting it to phosphatidylinositol-3,4-bisphosphate (PI(3,4)P2). This activity modulates the PI3K (phosphoinositide 3-kinase) signaling pathway, which is critical for cell survival, proliferation, and immune responses.
GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.
PROTAC SHP2 degrader-1 is a potent and effective SHP2 degrader. PROTAC SHP2 degrader-1 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins and is also neddylation- and proteasome-dependent.
NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 bind
SC-43, a sorafenib derivative, is an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) and reduces liver fibrosis. SC-43 reduces p-STAT3 and induces apoptosis with anti-tumor activity.
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.