Tetrazine-SS-Biotin is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
A-1293102 is a potent and selective BCL-XL inhibitor that kills BCL-XL-dependent tumor cells[1].
Rocaglamide D (3'-Hydroxyrocaglamide) (compound 1) is a lignan that can be found in Aglaia odorata. Rocaglamide D shows cytotoxicity with IC50s of 0.32, 0.12, 0.25 µM for HeLa, SGC-7901, A549 cells, respectively[1].
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].
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).
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].
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].
Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.
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].
3-Pyridine-2,4,5,6-d4 -carboxylic acid, ethyl ester is the deuterium labeled 3-Pyridine-2,4,5,6-d4-carboxylic acid, ethyl ester[1].
BiP inducer X, a selective inducer of immunoglobulin heavy chain binding protein (BiP)/GRP78, is an effective ER (endoplasmic reticulum) stress inhibitor. BiP inducer X preferentially induces BiP with slight inductions of GRP94, calreticulin, and C/EBP homologous protein. BiP inducer X protects neurons from ER stress[1][2].
N2,N2-Dimethylamino-6-deamino adenosine 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].
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.
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells[1].
EIPA is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
L-Tyrosine Hydrazide is a tyrosine derivative[1].
PHI-27 (rat) is a 27 amino acid peptide.PHI-27 (rat) is used to find peptide hormones and other active peptides[1].
Ethylenethiourea is a degradation product of the ethylenebisthiocarbamate group of fungicides. Ethylenethiourea is tumorigenic and teratogenic. Ethylenethiourea is orally active[1][2].
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].
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:
Filipin III is the major component of Filipin, a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure[1].
S-110 is a dinucleotide consisting of 5-Aza-CdR followed by a deoxyguanosine which shows to be an effective DNA methylation inhibitor.