PKI (5-24),amide (IP20-amide) is a 20-residue peptide that corresponds to the active portion of the heat-stable inhibitor protein of cAMP-dependent protein kinase. PKI (5-24),amide is a potent cAMP-dependent protein kinase (PKA) (PKA) inhibitor with a Ki of 2.3 nM[1].
Zelasudil is a Rho-associated (ROCK) kinase inhibitor. Zelasudil has a ROCK2 binding affinity[1][2].
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research[1].
Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner[1].
THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer[1].
Novel antitumor agent, inducing PKR-mediated apoptosis and synergizing with IFN
Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.
Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.
Momelotinib-3,3,5,5-d6 (CYT387-3,3,5,5-d6) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
Tofacitinib is a JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration[1].
TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC. TX-1123 is a cyclo-oxygenase (COX) inhibitor with IC50 values of 1.16 μM and 15.7 μM for COX2 and COX1, respectively. TX-1123 has low mitochondrial toxicity. TX-1123 can be used in research of cancer[1][2].
LIMK-IN-1 (Compound 14) is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively. LIMK-IN-1 can be used for ocular hypertension and associated glaucoma research[1].
Tauroursodeoxycholate dihydrate (TUDCA dihydrate; UR 906 dihydrate; Taurolite dihydrate) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK[1][2].
γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local anesthetic that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease[1].
H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor[1].
Momelotinib-3,3,5,5-d4 (CYT387-3,3,5,5-d4) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
YAP-TEAD-IN-3 (compound 155) is a YAP/TAZ-TEAD inhibitor. YAP-TEAD-IN-3 inhibits Avi-humanTEAD4217-434 with an IC50 value of 9 nM. YAP-TEAD-IN-3 also inhibits NCI-H2052 with an GI50 of 0.048 μM (cell proliferation)，and an IC50 of 0.048 μM (YAP reporter gene expression)，respsectively[1].
ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM[1].
ERKtide is a biological active peptide. (ERKtide is a peptide substrate for ERK2. Extracellular regulated protein kinase 2 (ERK2) is a eukaryotic protein kinase whose activity is regulated by mitogenic stimuli.)
CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide is a macamide isolated from Maca (Lepidium meyenii Walp.) N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide induces mesenchymal stem cells osteogenic differentiation and consequent bone formation through activating the canonical Wnt/β‐catenin signaling pathway. N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide can be used for the research of osteoporosis[1].
Wnt pathway activator 2 is a potent Wnt activator extracted from patent WO2012024404A1, compound 2, has an IC50s of 13 nM[1].
Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
Momelotinib-2,2,6,6-d6 (CYT387-2,2,6,6-d6) is the deuterium labeled Momelotinib (HY-10961). Momelotinib has inhibitory activity for JAK1/JAK2[1][2].
Benzene hexabromide, a bromohydrocarbon, is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation.
Rovadicitinib hydrochloride is a JAK inhibitor with an IC50 value <20 nM. Rovadicitinib hydrochloride also exhibits anti-inflammatory activity[1][2].
KY-02327 is an orally active, small molecule inhibitor of the Dishevelled (Dvl)-CXXC5 interaction with IC50 of 3.1 uM, a metabolically stabilized KY-02061 analog; KY-02327 is more stable by 2.3-fold and 1.3-fold than KY-02061 in rat liver microsomes and in human hepatocytes, respectively; shows enhanced effect on induction of ALP activity of osteoblast cells compared with KY-02061; activates the Wnt/β-catenin pathway, promotes osteoblast differentiation, and rescues BMD, bone volume, and trabecular bone structures in variectomized (OVX) mouse model.
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1[1].