Pacritinib is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
Dehydrojuncusol, a potent HCV inhibitor, targets HCV NS5A and is able to inhibit RNA replication of replicons harboring resistance mutations to anti-NS5A direct-acting antivirals. Dehydrojuncusol significantly inhibits HCV infection when added after virus inoculation of HCV genotype 2a (EC50=1.35 µM)[1].
MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
SIRT1-IN-2 (compound 3h) is a potent and selective SIRT1 (silent information regulator 1) inhibitor, with an IC50 of 1.6 μM[1].
N-Boc-dolaproine-methyl is the amino acid residue of the pentapeptide Dolastatin 10 (HY-15580). Dolastatin 10 inhibits tubulin polymerization and mitosis and has anticancer activity[1].
Aspercolorin, a secondary metabolite, is a cyclic peptide[1].
2-Amino-3,7-dihydro-5-iodo-7-β-D-ribofuranosyl-4H-pyrrolo[2,3-d]pyrimidin-4-one is a purine nucleoside analogue. 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].
2′-Deoxy-2′-fluoroguanosine, a nucleoside analog, is a potent inhibitor of influenza virus strains, with an EC90 of <0.35 μM for influenza virus A and B strains. 2′-Deoxy-2′-fluoroguanosine significantly inhibits replication of influenza virus in the upper respiratory tract, resulting in amelioration of fever and nasal inflammation[1][2].
Adipic acid-d10 is the deuterium labeled Adipic acid[1]. Adipic acid is found to be associated with HMG-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism[2].
Mipomersen (ISIS 301012 free base) is an antisense oligonucleotide inhibitor of apolipoprotein B (apoB). Mipomersen has anti-HCV effect and reduces the infectivity of the HCV. Mipomersen can be used for the research of homozygous familial hypercholesterolemia (HoFH)[1][2].
Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease[1].
Pseudolaric acid C2-O-β-D-glucoside is a natural product isolated from Pseudolarix kaempferi[1].
Berzosertib (VE-822) is an ATR inhibitor with a Ki value of less than 0.2 nM. It also inhibits ATM with a Ki of 34 nM.
EIPA is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
MFN2 agonist B-A l is a mall-molecule mimics of the peptide-peptide interface of MFN2, allosterically activates MFN2 and promotes mitochondrial fusion with EC50 of 3 nM; potently stimulates mitochondrial fusion in MFN2-deficient cells, competed for minipeptide binding at the MFN2 HR2 interaction site, correct mitochondrial damage induced by nonfunctioning MFN2 mutants by activating endogenous mitofusins by amelioration of mitochondrial dysmotility, fragmentation, depolarization, and clumping; normalizes axonal mitochondrial trafficking within sciatic nerves of MFN2 Thr105→Met105 mice.
Lithospermic acid ((+)-Lithospermic acid) is a plant-derived polycyclic phenolic carboxylic acid isolated from Salvia miltiorrhiza, and has the anti-oxidative and hepatoprotective activity on carbon tetrachloride (CCl4)-induced acute liver damage in vitro and in vivo[1].
Gluconate-1-13C sodium is the 13C labeled Gluconate sodi[1][2].
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].
ASR-488 activates the mRNA-binding protein CPEB1, induces apoptosis and inhibits bladder cancer growth[1].
Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer.IC50 value:Target:In vitro: Cinobufagin inhibited proliferation of cancer cells at doses of 0.1, 1, or 10 μM after 2–4 days of culture. Cytotoxicity of cinobufagin on the DU145 and LNCaP cells was dose-dependent. Cinobufagin increased [Ca2+]i and apoptosis in cancer cells after a 24-hr culture as well as caspase 3 activities in DU145 and PC3 cells and caspase 9 activities in LNCaP cells [1]. Cinobufagin suppresses cell proliferation and causees apoptosis in prostate cancer cells via a sequence of apoptotic modulators, including Bax, cytochrome c and caspases [2].In vivo:
Conagenin is an immunomodulator. Conagenin shows antitumor effects by activation of T cells and increasing antitumor effector cells[1].
Fmoc-Dap(Alloc)-OH is an alanine derivative[1].
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI)[1][2].
STAMBP-IN-1 is a small-molecule inhibitor of STAMBP deubiquitinase, and interrupts STAMBP-Ub-NALP7 interaction. STAMBP-IN-1 decreases protein level of its inflammasome substrate NALP7 and suppresses IL-1b release after Toll-like receptor (TLR) agonism. STAMBP-IN-1 inhibits the activity of STAMBP to cleave recombinant di-Ub with an IC50 value of 0.33 mM[1].
(Gln22,Asn23)-Amyloid β-Protein (1-40) is a peptide. (Gln22,Asn23)-Amyloid β-Protein (1-40) can be used for the research of Cerebral Amyloid Angiopathy Mutations[1].
Anti-inflammatory agent 30 (Compound 5) is an anti-inflammatory agent with hepatoprotective activity[1].
MF 5137 is a potent antibacterial agent.
3'-O-Methylguanosine is a methylated nucleoside analogs and a RNA chain terminator. 3'-O-methylguanosine can inhibit early virus-specific RNA synthesis[1].
4-Ethoxyphenol is an endogenous metabolite.
6'-O-β-Apiofuranosylsweroside is a secoiridoid glycoside that can be isolated from the leaves of Lonicera angustifolia Wall[1].