MLN120B is a specific, ATP competitive IKKβ inhibitor with an IC50 of 60 nM.
Galanin message associated peptide (1-41) amide is a peptide hormone[1].
H-Cyclopropyl-Gly-OH is a Glycine (HY-Y0966) derivative[1].
Nystose is a tetrasaccharide with two fructose molecules linked via beta (1→2) bonds to the fructosyl moiety of sucrose.
Dodecanoic acid ingenol ester is a natural compound.
Yadanziolide C is a quassinoid with antiproliferative and differentiation-inducing properties in promyelocytic HL-60 cells[1].
Simpinicline (OC-02), a highly selective nicotinic acetylcholine receptor (nAChR) agonist, shows potent antiviral activity against the SARS-CoV-2 variants in cell culture with an IC50 of 0.04 µM[1].
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controlling acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock treatment[1][2][3][4][5].
Dihydrosinapyl alcohol, a natural product, can be obtained from lignocellulose by hydrogenation and hydrogenolysis[1][2].
Dehydroglyasperin C, a isoflavone, is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C has antioxidant, neuroprotective, cancer chemopreventive, and anti-inflammatory activities[1][2][3].
Ethybenztropine (Ponalid) is a muscarinic receptor blocker. Ethybenztropine is an anticholinergic and antihistaminergic agent[1].
CW 008, a derivative of pyrazole-pyridine, is a CREB or PKA pathway agonist. CW 008 also is a stem cell differentiating agent. CW 008 stimulates osteoblast differentiation of human MSCs and increases bone formation in ovariectomized mice. CW008 promotes osteogenesis by activating cAMP/PKA/CREB signaling pathway and inhibiting leptin secretion[1][2][3].
TNIK inhibitor X is a potent inhibitor of Traf2- and Nck-interacting kinase (TNIK) (in vitro enzyme IC50=9 nM) with a reasonable selectivity over 30-folds against the majority of a panel of 50 kinases profiled; inhibits cell viability of PAMC82 and T47D cells harboring TNIK amplification with IC50 of 1.77 and 0.385 uM, respectively; shows no inhibitory activity against TNIK-non-amplified AZ-521 cells (IC50>30 uM); suppresses pAKT and induction of LC3 in TNIK-amplified PAMC82 cells, shows minimal effects on either Wnt signaling-mediated transcription.
AOH1996 is an orally active ligand of replisome component PCNA (Proliferating cell nuclear antigen), targeting to transcription-replication conflict (TRC). AOH1996 stabilizes the interaction of PCNA and RNA polymerase II, causing proteasome-dependent degradation of rpb1 and lethal DNA damages. AOH1996 also interferes the interaction of PCNA and its binding proteins, leading to DNA replication stress and inducing apoptosis. AOH1996 exerts synergistic effect with DNA damage agents, to inhibit tumor cells[1][2].
PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC50=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability[1].
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation[1][2].
N-[Bis(methylthio)methylene]glycine methyl ester is a Glycine (HY-Y0966) derivative[1].
AWL-II-38.3 is a potent ephrin-A receptor (EphA3) kinase inhibitor. AWL-II-38.3 does not exhibit significant cellular activity against Src-family kinases nor against b-raf[1][2][1][2].
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM)[1][2][3].
Tabimorelin (NN703) hemifumarate is an orally active growth hormone (GH) secretagogue. Tabimorelin hemifumarate is also a potent inhibitor of CYP3A4 activity[1].
Xylopine is an aporphine alkaloid with cytotoxic activity on cancer cells. Xylopine induces oxidative stress, causes G2/M cell cycle arrest and apoptosis in cancer cells[1].
AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
2′-Deoxy-6-O-methylinosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
PT-2385 is a selective HIF-2α antagonist with a Ki of less than 50 nM.
GLP-1R agonist 9 (Compound 96) is a GLP-1R agonist with EC50 values of 1.1 nM and 11 nM against CHO GLP-1R Clone H6 and CHO GLP-1R Clone C6, respectively[1].
Leachianone A, isolated from Radix Sophorae, has anti-malarial, anti-inflammatory, and cytotoxic potent[1]. Leachianone A induces apoptosis involved both extrinsic and intrinsic pathways[2].
2-(1-Methyl-1H-imidazol-4-yl)ethan-1-amine is a histamine (Him) metabolite.
SPC4061 an antisense nucleotide, is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases[1][2].
Dopamine serotonin antagonist-1 is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively.
1-Hexadecanol is a fatty alcohol, a lipophilic substrate.