Amiprilose (SM1213; Therafectin) is a potent inhibitor against Hepatocellular carcinoma (HCC). Amiprilose induces lymphokine-induced macrophage activation directly to kill Listeria monocytogenes[1][2].
Akt1/Akt2-IN-2 (compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells[1].
7,8-Dihydro-8-oxo-7-propargyl-3’-deoxy-3’-fluoro-xylo-guanosine 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].
Hesperidin (HP) is a bioflavonoid that plays a role in plant defense and is abundant in citrus species, such as grapefruit, lemon and orange. Hesperidin is used effectively as a supplemental agent in complementary therapy protocols, since it possesses biological and pharmacological properties as an effective antioxidant, anti-inflammatory, anti-carcinogenic, and anti-hypertensive agent with lipid-lowering activity[1]IC50: hesperidin (IC50=116.68μmo/L))[4]in vitro: hesperidin and linarin are two of the main constituent of Valeriana's extract exhibiting a high affinity to KATP channel, which are related to the control of Ca++ concentration and release of GABA in synaptic nerve terminal, mainly on cells of SN[2]in vivo: Hesperidin was dissolved in 1% carboxymethyl cellulose (CMC) and administered orally at a dose of 50 mg/kg for 10 consecutive days. In the control group, rats were treated with the corn oil and 1% CMC vehicle.[1]
TCS 359, a 2-acylaminothiophene-3-carboxamide, is a potent inhibitor of FLT3 with IC50 of 42 nM. IC50 Value: 42 nM [1]Target: Flt3in vitro: TCS 359, a 2-acylaminothiophene-3-carboxamide, is a potent inhibitor of FLT3 with IC50 of 42 nM. TCS 359 inhibits MV4-11 proliferation with IC50 of 340 nM. TCS 359 is highly selective for FLT3 against a panel of kinases [1].
Tabituximab (OTSA101) is a humanized monoclonal antibody against frizzled class receptor 10 (FZD10)[1].
PROTAC Linker 34 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 34 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Obacunone, isolated from seeds of Marsh White grapefruit, exhibits anti-tumor activity by the induction of apoptosis[1].
Episilvestrol is a derivative of silvestrol, isolated from the fruits and twigs of Aglaia silvestris, and is a specific eIF4A-targeting translation inhibitor, with antitumor activity.
VX-661 is a second F508del CFTR corrector and help CFTR protein reach the cell surface.
Ibritumomab tiuxetan is an immunoconjugate composed of the murine IgG1κ anti-CD20 monoclonal antibody Ibritumomab that is covalently bound to the chelator Tiuxetan that permits the addition of the short-lived β-emitter radioisotope yttrium-90. Ibritumomab tiuxetan can be used for the research of non-Hodgkin's B-cell lymphomas[1][2].
β-catenin-IN-4 (Compound 39) is a β-catenin inhibitor with a Ki of 0.64 μM. β-catenin-IN-4 reduces the protein expression levels of cyclin D1 and c-Myc[1].
Larotrectinib (LOXO-101) sulfate is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
(R)-Nedisertib ((R)-M3814) is a less active R-enantiomer of Nedisertib, with an IC50 in the range of 7-30 nM for DNA-PK[1].
(E)-AG 99 ((E)-Tyrphostin 46; (E)-Tyrphostin AG 99) is a potent EGFR inhibitor[1].
Rezvilutamide (SHR3680) is an androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer[1][2].
(S)-Enzaplatovir ((S)-BTA-C585) is the S-enantiomer of Enzaplatovir. (S)-Enzaplatovir shows antiviral activities with an EC50 of 56 nM for respiratory syncytial viral (RSV) (patent WO2011094823A1 compound 77)[1].
DMT-2'-O-MOE-rA(Bz) phosphoramidite is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Glycine ethyl ester-13C (hydrochloride) is a 13C-labeled Mebendazole.
Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity[1][2].
Tin-protoporphyrin IX (SnPPIX) is a potent Heme oxygenase-1 (HO-1) inhibitor. Tin-protoporphyrin IX (SnPPIX) sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model[1].
Garivulimab (BGB-A333) is a humanized IgG1-variant monoclonal antibody that specifically targets and binds to PD-L1. Garivulimab selectively blocks the interaction of PD-L1 and PD-1. Garivulimab has antitumor activity[1].
Mitochondrial respiration-IN-2 is the fluorine derivative of Virginiamycin M1 (HY-N6686). Mitochondrial respiration-IN-2 can inhibit mitochondrial translation of glioblastoma stem cells[1].
7-Ethyl-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl)guanine 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].
Pertuzumab (PBS), a humanized monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.
ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research[1].
Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.
Bis-PEG8-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG8-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Niclosamide-13C6 is the 13C6 labeled Niclosamide. Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers[1][2][3][4].