E3 ligase Ligand-Linker Conjugates 6 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM[1]. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist[2]. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively[3].
2’-Deoxy-2’-fluoro-6-S-Methyl-6-thio-ara-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].
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer[1].
Tigapotide (PCK-3145) is an anti-tumour peptide that reduces the development of skeletal metastases associated with prostate cancer. Tigapotide induces apoptosis and reduces tumour parathyroid hormone-related peptide (PTHrP) levels[1].
m-PEG12-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. m-PEG12-amine is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
EPZ011989 hydrochloride is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor, with a Ki value of <3 nM. EPZ011989 shows anti-tumor activity. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups[1].
FGFR4-IN-11 (Compound 30) is a potent, selective, covalent FGFR4 inhibitor with an IC50 of 2.1 nM. FGFR4-IN-11 significantly inhibits the FGF19/FGFR4 signaling pathway and shows antitumor activity[1].
Aminooxy-PEG3-azide is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Aminooxy-C2-PEG3-azide is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].
NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
Efizonerimod alfa is a potent monoclonal antibody OX40 activator. Efizonerimod alfa can be used for cancer research[1].
PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.
α-Cytidine 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].
Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations[1][2][3][4].
PI3K/mTOR Inhibitor-14 (compound Y-2) is a potent PI3K and mTOR dual inhibitor with IC50s of 171.4 nM and 10.1 nM, respectively. PI3K/mTOR Inhibitor-14 has antitumor activities[1].
MELK-IN-1 is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK) with an IC50 and a Ki of 3 nM and 0.39 nM, respectively.
Pyridinium bisretinoid A2E (A2E)is an initiator of blue-light-induced apoptosis. Photoactivation of Pyridinium bisretinoid A2E mediates autophagy and the production of reactive oxygen species[1][2].
Gypenoside L is a saponin that can be found in Gynostemma pentaphyllum. Gypenoside L increases the SA-β-galactosidase activity, promotes the production of senescence-associated secretory cytokines. Gypenoside L also can activate p38 and ERK MAPK pathways and NF-κB pathway to induce senescence. Gypenoside L exhibits anti-tumor and anti-inflammatory activities[1][2].
Lixudebart is a humanized immunoglobulin G1-kappa, anti-CLDN1 monoclonal antibody[1].
TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
Picankibart is a mouse-derived IgG1κ antibody targeting IL23A[1].
PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.
3,5-Di-O-benzoyl-2-deoxy-2-fluoro-5-trifluoromethyl-arabinouridine 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].
T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
NPD8733 (NPD-8733) is a small-molecule ligand of valosin-containing protein (VCP)/p97, binds to the D1 domain of VCP/p97; suppresses the enhanced migration of NIH3T3 cells co-cultured with MCF7 cells using a wound healing co-culture assay.
C-di-IMP (Cyclic-di-IMP) is a STING agonist. C-di-IMP can be used for the research of tumor[1].
MK 2206 is an orally active allosteric Akt inhibitor with IC50s of 5, 12 and 65 nM for Akt1, Akt2 and Akt3, respectively.
Hosenkoside G, a baccharane glycoside isolated from the seeds of Impatiens Balsamina L., possesses anti-tumor activity[1][2].
Proanthocyanidins are a class of polyphenols with antibacterial, antifungal and antiviral activities, which can be used in the treatment of chronic venous insufficiency, capillary fragility, sunburn and retinopathy.
NVP-QAV-572 is a PI3K inhibitor extracted from patent US7998990B2, Compound Example 8, has an IC50 of 10 nM.