Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis[1][2][3].
TLR7 agonist 13 is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
n-Octyl caffeate shows anti-cancer and apoptosis inducing activity in highly liver-metastatic murine colon 26-L5 carcinoma cell lines[1].
Mitoquidone (GR-30921), a pentacyclic pyrroloquinone, is a potent anticancer agent[1].
Veltuzumab (IMMU-106) is a humanized anti-CD20 monoclonal antibody. Veltuzumab has low EC50 value of 0.08-0.09 μg/mL in the Daudi cell line. Veltuzumab can be used for the research of cancer including non-Hodgkin lymphoma (NHL)[1].
ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
KTX-582 intermediate-1 is an intermediate in the synthesis of KTX-582 (HY-148274) and can be used for ADC preparation. KTX-582 is an IRAK4 degrader and inducer of apoptosis with DC50 of 4 nM and 5 nM for IRAK4 and Ikaros, respectively[1].
9-(β-D-Xylofuranosyl)guanine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
MP-A08 is a highly selective ATP competitive sphingosine kinase (SK) inhibitor that targets both SphK1 and SphK2 with Kivalues of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.In vitro:MP-A08 blocks pro-proliferative signalling pathways, induces mitochondrial-associated apoptosis in a SK-dependent manner, and reduces the growth of human lung adenocarcinoma tumours in a mouse xenograft model by both inducing tumour cell apoptosis and inhibiting tumour angiogenesis. MP-A08 inhibit SphK2, cause a decrease in EC barrier integrity in vitro in both cell type.[2]In vivo: MP-A08 suppresses the growth of human lung tumor xenografts in mice.
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity[1][2].
Garcinone E is a natural xanthone found in the rind of the mangosteen fruit. Garcinone E induces apoptosis and inhibits cancer cell migration. Garcinone E has anticancer effects on different human cancer cell lines, including colorectal, breast, and hepatocellular carcinomas[1].
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
Lanreotide acetate (BIM 23014 acetate) is a somatostatin analogue with antineoplastic activity. Lanreotide acetate can be used for carcinoid syndrome[1][2].
(-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM.
MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
Olanzapine D3 (LY170053 D3) is the deuterium labeled Olanzapine. Olanzapine is 5-HT2 and D1/D2 antagonist. Olanzapine is an antipsychotic agent with anticholinergic properties[1]. Olanzapine induces autophagy, mitochondrial damage and mitophagy in human SH-SY5Y neuronal cell line[2].
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a humanized monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKT activation[1].
HPK1-IN-19 is a hematopoietic progenitor kinase 1 (HPK1) inhibitor extracted from patent WO2020235902A1 compound 106[1].
Palbociclib hydrochloride is a highly selective CDK4/6 inhibitor with IC50s of 11 nM and 16 nM, respectively.
PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM[1].
KTX-582 intermediate-2 is an intermediate in the synthesis of KTX-582 (HY-148274) and can be used for ADC preparation. KTX-582 is an IRAK4 degrader and inducer of apoptosis with DC50 of 4 nM and 5 nM for IRAK4 and Ikaros, respectively[1].
NVP-CGM097 sulfate is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
Ugodotin is an antibody-drug conjugate. Ugodotin can binds IGF-1R with antitumor activity[1].
Fluorescent Brightener 28 is a visible light emitting diode (LED)-light sensitive photoinitiator for free radical photopolymerizations[1].
UCK2 Inhibitor-1 (Compound 20874830-2) is a non-competitive UCK2 inhibitor with an IC50 of 4.7 µM[1].
N2-iso-Butyroyl-5’-O-(4,4’-dimethoxytrityl)-3’-O-methylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
Hepln-13 is a potent and orally active Hepsin inhibitor with an IC50 of 0.33 µM. Hepln-13 can be used for the research of metastatic prostate cancer[1].
Antiproliferative agent-22 (compound 2) is an anticancer agent. Antiproliferative agent-22 shoes anti-proliferative activities against MCF-7, MDA-MB-231 and MDA-MB-468 cells with IC50 values of 6.2 μM, 3.3 μM and 3.3 μM, respectively[1].
AC-4-130 is a novel, potent STAT5 SH2 domain inhibitor, binds to and efficiently blocks STAT5 activation and subsequent transcriptional activity, shows high selectivity for STAT5 over STAT1 and STAT3; disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription; substantially impairs the proliferation and clonogenic growth of human AML cell lines and primary FLT3-ITD+ AML patient cells in vitro and in vivo; synergistically increases the cytotoxicity of the JAK1/2 inhibitor Ruxolitinib and the p300/pCAF inhibitor Garcinol in vivo.