Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties[1].Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
NR2F6 modulator-1 is a potent nuclear receptor subfamily 2, group F, member 6 (NR2F6) modulator. NR2F6 modulator-1 can be used for researching immune modulation and modulation of cancer stem cell activity[1].
SYC-435 (SYC435) is a potent inhibitor of mutant IDH1, binds at the isocitrate pocket of mutated IDH1 with Ki values of 190 nM against IDH1 R132H and 120 nM against IDH1 R132C; SYC-435 is cell active and capable of significantly reducing D-2-HG production in an HT1080 fibrosarcoma cell line expressing IDH1 R132C (IC50=2.4 uM).
Triptorelin acetate is a Gonadotropin-releasing hormone (GnRH) receptor agonist[1].
Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
2,3,5-Tri-O-benzyl-D-ribono-1,4-lactone 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].
Cardionogen 1 (CDNG1/vuc230) is a Wnt signaling pathway inhibitor that slows down Myc-induced liver tumorigenesis. Cardionogen 1 treatment of zebrafish embryos before gastrulation inhibits cardiomyocyte formation, whereas treatment during or after gastrulation induces cardiomyocyte formation. Cardionogen 1 has potential in research into cancer and cardiovascular disease[1][2].
MHY-1685, a novel mammalian target of rapamycin (mTOR) inhibitor, provides opportunities to improve hCSC-based myocardial regeneration.
MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively[1]. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity[2].
ABT-737 is a selective and BH3 mimetic Bcl-xL, Bcl-2 and Bcl-w inhibitor with EC50s of 78.7 nM, 30.3 nM and 197.8 nM, respectively.
Nenocorilant (Relacorilant) is a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research[1][2][3].
Emicoron is a new promising G4 ligand and bind G-rich oncogene promoters. Emicoron possesses a marked antitumoral activity? alone or in combination with chemotherapeutics in vivo. Emicoron can be used for cancer research[1].
Sanguinarine (Sanguinarin) gluconate, a benzophenanthridine alkaloid, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB[1].
Ubamatamab (REGN4018) is a human bispecific antibody targeted against Mucin 16 (MUC16) and CD3. Ubamatamab demonstrates potent antitumor activity[1].
GGFG-Eribulin (Compound GGFG) is a Drug-Linker Conjugates for ADC. GGFG-Eribulin consists of the ADC Cytotoxin Exatecan (HY-13442) and a linker. GGFG-Eribulin can be used for synthesis of ADCs[1].
PTC-209 hydrobromide is a specific BMI-1 inhibitor with IC50 of 0.5 μM in both GEMS reporter and ELISA assays.
Pyridoclax is a potential Mcl-1 inhibitor.
(±)-BAY-1251152 is a racemic mixture of BAY-1251152. BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.
DHODH-IN-23 (Compound A) is an orally active DHODH inhibitor that can be used for the research of cancer[1].
4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) .IC50 value: 1.7 nM (Ki)Target: σ1in vitro: 4-IBP is a σ1 receptor agonist, decreases the migration of human cancer cells, including glioblastoma cells. 4-IBP is used to investigate whether targeting theσ1 receptor could modify in vitro the migration rates of human cancer cells and increase the sensitivity of metastasizing human A549 NSCLC cells and infiltrating human glioblastoma cells to cytotoxic insults of either proapoptotic or proautophagic drugs.[1]in vivo: 4-IBP increases the antitumor effects of temozolomide and irinotecan in immunodeficient mice that were orthotopically grafted with invasive cancer cells.[1]
Perifosine is an oral Akt inhibitor. All cells are sensitive to the antiproliferative properties of Perifosine with an IC50 of ~0.6-8.9 μM.
BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases[1].
SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.
3’-Deoxy-5-trifluoromethyluridine 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].
Tamtuvetmab (AT-005) is a caninised blontuvetmab against CD52. Tamtuvetmab increases progression-free survival (PFS), exhibits in vivo efficacy in dogs with naïve T-cell lymphoma (LSA). Tamtuvetmab has been approved by veterinary[1][2].
IMP-1710 (IMP1710) is a potent, selective, covalent UCHL1 inhibitor with IC50 of 38 nM.IMP-1710 demonstrated exquisite selectivity in a cross-screening against 20 DUBs.IMP-1710 can profile activity of endogenous UCHL1 with excellent selectivity in cell types including endothelial cells (EA.hy926) and adenocarcinoma human alveolar basal epithelial cells (A549).IMP-1710 demonstrated >50% fibroblast–myofibroblast transition (FMT) inhibition (IC50=740 nM) in idiopathic pulmonary fibrosis (IPF), as well as αSMA inhibition.IMP-1710 is a powerful and selective probe to explore UCHL1 activity with potential application to substrate identification, mode of action studies, and cellular target profiling.
Agroclavine is a natural, clavine type of ergot alkaloid. Agroclavine is a D1 dopamine receptor and α1-adrenoceptor agonist. Agroclavine also has anticancer and antimicrobial activities[1][2].
2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.
VISTA-IN-2 (Compound 1) is an inhibitor of V-domain Ig suppressor of T-cell activation (VISTA). VISTA-IN-2 induces VISTA degradation in cells through an autophagic mechanism. VISTA-IN-2 rescues VISTA-mediated immunosuppression, and enhances antitumor activity of immune cells. VISTA-IN-2 also activates the antitumor immunity and inhibits tumor growth in a CT26 mouse model[1].
Isoliensinine is a bisbenzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera, with anti-oxidant and anti-inflammatory and anti-cancer activities. Isoliensinine induces apoptosis in triple-negative human breast cancer cells[1][2].