TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases[1].
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].
Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits Autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1[1][2][3][4].
JAK1-IN-11 (compound 11) is a potent inhibitor of JAK，with IC50s of 0.02 nM (JAK1)，and 0.44 nM (JAK2)，respectively. JAK1-IN-11 has high selectivity against JAK1 over JAK2[1].
TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC50s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease[1].
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer[1].
CHIR 98024 (Compound L) is a glycogen synthase kinase 3 (GSK3) inhibitor with an EC50 of 0.2566 μM[1].
Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity[1][2].
Niclosamide-13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
CaMKP inhibitor sodium is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
ERK-IN-1 (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC (non-small celllung cancer), BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovanan cancer[1].
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities[1].
Casein kinase 1δ-IN-7 (compound 497) is a Casein kinase 1δ inhibitor. Casein kinase 1δ-IN-7 can be used in the study of neurodegenerative disorders such as Alzheimer's disease[1].
tCFA15 is a trimethyl cyclohexenonic long chain fatty alcohol containing 15 carbon atoms on the side chain, promotes the differentiation of neurons, and may regulates Notch signaling.
Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab potently inhibited RGMa mediated BMP signalling via the SMAD1/5/8 pathway, with an IC50 around 97 pM. Elezanumab promotes neuroregeneration and neuroprotection in neuronal injury and demyelination models binds N-terminal RGMa, blocks BMP signaling and lacks RGMc cross-reactivity. elezanumab has neuroregenerative and neuroprotective activities without impact on iron metabolism[1][2].
GNE-7883 is a pan-TEAD inhibitor with anti-cell proliferation activity. GNE-7883 overcomes resistance to KRAS G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation. GNE-7883 may be used in the study of YAP/TAZ-dependent cancers[1].
D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro.
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively[1]. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β[2].
JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with IC50 value of 5 nM.IC50 value: 5 nM [2]Target: WNTin vitro: CCT251545 is a potent and selective chemical probe for the human Mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases. CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with IC50 of 9 nM. CCT251545 is a small-molecule inhibitor of the WNT pathway discovered through cell-based screening. CCT251545 displays potent cell-based activity. CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1. [1] CCT251545 demonstrates weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0 ± 0 μM). CCT251545 potently inhibits reporter-based readouts of basal WNT pathway activity in LS174T and SW480 cells in the absence of WNT ligand or other stimulants (IC50 = 0.023 ± 0.011 μM and 0.190 ± 0.030 μM, respectively) and demonstrated potent inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC50 = 0.007 μM).[2]in vivo: CCT251545 as a potent and selective chemical probe suitable for cell-based exploration of the reported context-dependent roles of CDK8 and CDK19 and associated kinase module subunits in human disease and other biological settings. [1]
ERK1/2 inhibitor 8 is a potent ERK inhibitor with an IC50 of 0.48 nM for ERK2 (WO2021110168A1, WX007)[1].
ROCK-IN-8 (Example 4) is a ROCK inhibitor, with an IC50 value less than 100 nM. ROCK-IN-8 has anti-inflammatory activity. ROCK-IN-8 can be used for research of respiratory and gastro-intestinal diseases[1].
Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively.
PIMPC is a compound with antioxidant and metal-chelating properties. PIMPC is a novel inhibitor of glycogen synthase kinase 3 (GSK-3). PIMPC has potential anti-Alzheimer's disease effect[1].
GNF-6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling.1) GNF-6231 shows IC50s of greater than 10 μM on all CYP isoforms tested2) GNF-6231 have favorable potency and a PK profile across preclinical species upon oral administration.3) The reference for orally in MMTV-Wnt1 tumor bearing mice is dosed at 3 mg/kg.4) GNF-6231 showed very robust dose-related antitumor efficacy.
Cys-Kemptide is a cysteine-terminated substrate peptide that can used to measure protein kinase A (PKA) activity[1].
Physalin H is a natural product that can be isolated from Solanum nigrum. Physalin H is an inhibitor of Hedgehog (Hh) signaling and it disrupts GLI1-DNA-complex formation. Physalin H inhibits GLI1 transcription with an IC50 value of 0.7 μM. Physalin H shows cytotoxicity to PANC1 and DU145 cells with IC50 values of 5.7 and 6.8 μM, respectively[1].
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis[1].
Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway.