JAK-IN-30 (compound 31) is a water-soluble JAK inhibitor with IC50 values of 2, 15, 18 and 2 nM for JAK2, JAK1, JAK3 and TYK2, respectively. JAK-IN-30 has research potential for dry eye disease (DED)[1].
FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease[1][2].
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively[1].
C-82 is a second-generation specific CBP/β-catenin antagonist, which inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent[1].
HODHBt (HOOBt) inhibits STAT5-SUMO interaction by blocking SUMOylation of phosphorylated STAT5. HODHBt enhances the magnitude of IL-15 signaling and significantly increases the natural killer (NK) cell cytotoxicity phenotype and function and the generation of cytokine-induced memory-like (CIML) natural killer (NK) cells. HODHBt can be used for research of HIV-infection and cancer[1].
ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
Oct4 inducer-2 is an OCT4 inducer, which can maintain the formation of hiPSCs by promoting the expression of endogenous OCT4, which can be used in anti-aging research[1].
Super-TDU is a specific YAP antagonist targeting YAP-TEADs interaction. Super-TDU suppresses tumor growth in gastric cancer mouse model[1].
PRI-724 is a selective inhibitor of the CBP/β-catenin interaction.
OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.IC50 value: Target: Oct4 activatorin vitro: OAC1 enhances the formation of Oct4-GFP+ colonies and accelerates the dynamics of reprogramming. OAC1 enhanced reprogramming efficiency through a mechanism that is independent of endogenous Oct4 promoter demethylation. OAC1 enhanced reprogramming efficiency through a mechanism that is distinct from suppressing p53-p21 expression. Luciferase assay revealed that OAC1 had no effect on Topflash activity, although BIO activated the Topflash reporter potently. OAC1 functions through a mechanism that is independent of the Wnt signaling.
Peficitinib (ASP015K) hydrobromide is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss[1].
AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM.
PF-06700841 P-Tosylate is a dual JAK1 and TYK2 inhibitor with IC50s of 17 and 23 nM, respectively. Anti-inflammatory activity[1].
SGC-AAK1-1, a chemical probe, is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1[1].
CB-103 is a notch signaling pathway inhibitor extracted from patent US9296682B2. CB-103 is developed for the treatment of cancers[1].
ERK5-IN-3 (compound 33j) is a potent and selective ERK5 (extracellular signal-related kinase 5) inhibitor, with an IC50 of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC50 of 31 nM[1].
RL-0070933 is a potent smo cilial modulator with an EC50 value of 0.02 µM. RL-0070933 modulates the translocation and/or accumulation of smoothened to the primary cilia by hedgehog signaling pathway[1].
Demcizumab (OMP 21M18) is an anti-DLL4 monoclonal antibody. Demcizumab is a potent inhibitor of the Notch pathway. Demcizumab alone or in combination with chemotherapy is effective in various cancer models[1][2][3].
8-Chloro-cAMP is a cAMP analogue that induces growth arrest, and modulates cAMP-dependent PKA activity. 8-Chloro-cAMP has anticancer activity[1].
Trimethylamine N-oxide is a gut microbe-dependent metabolite of dietary choline and other trimethylamine-containing nutrients. Trimethylamine N-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine N-oxide also accelerates fibroblast-myofibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway[1][2][3].
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice[1][2].
Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway[1].
Erismodegib diphosphate (LDE225 diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively.
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
β-Neo-Endorphin is an endogenous opioid peptide. β-Neo-Endorphin is a hypothalamic “big” Leu-enkephalin of porcine origin. β-Neo-Endorphin shows activation of the Erk1/2, MMP-2 and MMP-9[1][2].
SLx-2119 is a selective inhibitor of ROCK2 with an IC50 of 105 nM.
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides[1][2].