PI3Kγ is required for for T-cell and B-cell as well as mast cell migration and degranulation. As such, these kinases are attractive targets for potential anti-infmamatory drugs. TASP0415914 has shown excellent results in cell based assays. It is orally av

S6K-18 is a highly selective inhibitor of S6K1, with an IC50 of 52nM.

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

ML 086 is a potent, specific inhibitor of phosphatase PHOSPHO1 with IC50 of 139 nM, with no activity against TNAP (IC50>100 uM).

Chlorotoxin is a 36-amino acid peptide found in the venom of the deathstalker scorpion (Leiurus quinquestriatus).

LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

Voxilaprevir (GS-9857) is a potent HCV NS3/4A protease inhibitor that is used in combination with sofosbuvir and velpatasvir for treatment of HCV infection.

Disarib is a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain, demonstrates strong affinity to BCL2, but not to other antiapoptotic BCL2 family members(BCL-xL, BCL2A1 etc.).

Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively. Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies.

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α-Amyloid Precursor Protein Modulator is a cell-permeable benzolactam derived PKC activator (Ki = 11.9 nM for PKCα) that efficiently enhances non-amyloidogenic α-processing of amyloid precursor protein (APP) even at 100 nM in human fibroblast AG06848.

γ-Terpinene, a monoterpene, is an orally active antioxidant compound which can scavenge radicals directly. γ-Terpinene has potent antinociception activity.

A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.

NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist potentially for the treatment of solid tumors.

KDM5-C70 is the cell-permeable derivative of KDM5-C49, potent, selective and cell permeable KDM5 inhibitor with IC50 of 0.3, 0.3 and 0.58 uM for KDM5A, B and C, respectively.

AKI-603 is a novel small molecule Aurora A kinase inhibitor with IC50 of 12.3 nM, also inhibits Aurora B kinase activity to a less extent; disrupts normal spindle structure, and induces cell-cycle arrest; t; suppresses stem cell properties in breast cancer cells, and also suppresses the expression of self-renewal genes (β-catenin, c-Myc, Sox2, and Oct4); reduces xenograft tumor growth after intragastric administration.

β-Gentiobiose (Gentiobiose) is a naturally occurring oligosaccharin with a rapid turnover rate in ripening tomato fruit.

Maribavir(GW257406X; BW1263W94; 1263W94) inhibits HCMV replication is by inhibition of an HCMV encoded protein kinase enzyme called UL97 or pUL97.

U18666A, a cell permeable drug, is a cholesterol synthesis and transport inhibitor.

Sulopenem, also known as CP-70429, is a potent beta-lactamase inhibitor.Sulopenem showed potent antibacterial activity against gram-positive and gram-negative bacteria except Pseudomonas aeruginosa and Xanthomonas maltophilia. CP-70,429 was stable to various types of beta-lactamases except for the enzyme from X. maltophilia and was 16- to 128-fold more active than the other compounds against beta-lactamase-producing strains of Enterobacter cloacae and Citrobacter freundii.

Cytosporone B is the first naturally occurring agonist for nuclear orphan receptor Nur77. The molecule binds with high affinity (IC50=0.278 nM) to the ligand-binding domain of Nur77 and stimulates Nur77-dependent activities. Nur77 is also involved in glucose homeostasis, where it induces genes involved in gluconeogenesis. Csn-B physically binds to Nur77 and activates its transactivational activity and translocation to mitochondria to induce apoptosis. It inhibits cancer cell proliferation and tumor growth.

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