Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM.
ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79?nM, 1580?nM and 1330?nM for human uPA, tPA, and plasmin, respectively.
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively.
SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A.
Thrombin is a trypsin-like allosteric serine protease. Thrombin enables site-specific cleavage of fusion proteins with an accessible Thrombin recognition sequence and can be used to digest GST-tagged proteins.
UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin.
LHVS is a potent, non-selective cysteine protease inhibitor. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion.
KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.
ARL67156 trisodium salt is an inhibitor of ecto-ATPase. ARL 67156 is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively.
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).
BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.
SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 ?M. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer??s disease.
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt.
S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
LMP7-IN-1 is an inhibitor of immunoproteasome (LMP7), may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer.
ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor, which inhibits the activation of binding protein procaspase-9 and procaspase-3.
LDN 0088050 is selectivity adipocyte fatty acid binding protein (AFABP, FABP4) inhibitor with Ki values of 0.29 and 1.3 μM for FABP4 and FABP3, respectively. LDN 0088050 binds to FABP4 with a Kd of 2.05 μM.
Imazamox (CL29926) is a systemic herbicide that inhibits the production of acetolactate synthase (ALS) in plants with high selectivity, high activity, safety and broadspectrum activity, which would then inhibit plant growth and ultimately lead to plant death.
