ANO1-IN-3 (Compound 3n) is a potent and selective ANO1 inhibitor with an IC50 of 1.23 μM. ANO1-IN-3 induces apoptosis[1].
1,1′-Disinomenine is an alkaloid that can be isolated from the stems of Sinomenium acutum. 1,1′-Disinomenine shows weak inhibition against A549 and Hela cells[1].
Lurbinectedin (PM01183) is a new DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
Thalidomide-O-C5-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Bempegaldesleukin (NKTR-214), a PEGylated interleukin-2 (IL-2), is an immunostimulatory IL-2 prodrug acting as a CD122-preferential IL-2 pathway agonist. Bempegaldesleukin can stimulate an antitumor immune response[1].
5'-O-DMT-N4-Ac-2'-F-dC is a modified nucleoside and can be used to synthesize DNA or RNA.
Adjudin is an extensively studied male contraceptive with a superior mitochondria-inhibitory effect. Adjudin is also a potent Cl- channel blocker.
6β-Hydroxytomentosin, a sesquiterpenoid, can be found in flowers of Inula japonica. 6β-Hydroxytomentosin exhibits weak cytotoxicities against A549, SK-OV-3, HepG-2 and HT-29 cell lines[1][2].
PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin[1].
IDH2R140Q-IN-1 (compound C6) is a potent inhibitor of IDH2R140Q, with an IC50 of 6.1 nM. IDH2R140Q-IN-1 can be used for the research of acute myeloid leukemia[1].
2-Chloro-9-[(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)]-9H-purine 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].
Poricoic acid B, isolated from Poria cocos, possesses anti-tumor activity[1].
Alizapride hydrochloride is a dopamine receptor antagonist with prokinetic and antiemetic effects which can also be used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.
Thielocin B1 is a protein-protein interaction inhibitor of PAC3 homodimer. Thielocin B1 was isolated as a novel phospholipase A2 inhibitor from the fermentation broth of Thielavia terricola RF-143.
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
HNHA is a potent histone deacetylase (HDAC) inhibitor. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer[1].
Mal-C6-α-Amanitin is a drug-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.
Aurora Kinases-IN-2 (compound 12Aj) is a potent Aurora kinases inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora Kinases-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora Kinases-IN-2 can be used for cancer research[1].
Citroside A is a megastigmane sesquiterpenoid with cytotoxic and anti-inflammatory activities. Citroside A displays potential effects against NO production with an IC50 of 34.25 μM. Citroside A exhibits pronounced cytotoxicity against SGC-7901 and HeLa cells with IC50 values of 27.52 μM and 29.51 μM, respectively[1].
MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.
Batimastat is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.
Ro 106-9920 is a potent inhibitor of NF-kappaB. Ro 106-9920 has the potential for the research of tumor and cancer diseases[1].
Hispolon, a polyphenol, can be isolated from Phellinus linteus. Hispolon possesses anticancer, antidiabetic, antioxidant, antiviral, hepatoprotective, anti-diabetic, and anti-inflammatory activities[1].
PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties[1].
Conatumumab (AMG 655) is a human monoclonal agonist antibody against human death receptor 5 (DR5, TRAILR2) (Kd: 1 nM for the long form of DR5, 0.8 nM for the short form of DR5). Conatumumab induces apoptosis via caspase activation. Conatumumab can be used in the research of cancers. [1][2][3].
Lidocaine-d10 (Lignocaine-d10) hydrochloride is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
A potent and selective HDAC3 inhibitor with IC50 of 0.26 uM, with no activity against HDAC1/4/6/8; induces dose-dependent selective increase of NF-κB acetylation in human colon cancer HCT116 cells, induces growth inhibition of cancer cells, and activates HIV gene expression in latent HIV-infected cells; shows promising activity for anticancer and antiviral benefits.
Carcinoembryonic antigen (CEA) is a tumor marker in lung cancer.
Toceranib is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively.