Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
STING agonist C11 is a novel cell-permeable STING agonist that activates IFN-dependent signaling processes and induces IFN secretion from human cells; induces transcription and translation of interferon-dependent antiviral genes, induces canonical IRF3 phosphorylation and ISG transcription in a manner that requires STING but not MAVS or TRIF; potently blocks replication of multiple emerging Alphavirus types including Chikungunya, Ross River, Mayaro, and O'nyong'nyong viruses.
HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma[1].
Lucideric acid A is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells[1].
γ-Lumicolchicine is an inactive analogue of Colchicine (HY-16569)[1]
NRP1 antagonist 2 (Compound 1) is an NRP1 antagonist[1].
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts[1].
CCG-273463 is a potent, selective and covalent GRK5 inhibitor with an IC50 value of 9 nM. CCG-273463 can be used in the research of heart failure, hypertrophic cardiomyopathy, and cancer[1].
Belrestotug (EOS-448) is an antagonistic anti-TIGIT (VSIG9, VSTM3) human immunoglobulin G1 kappa (hIgG1 kappa) antibody. Belrestotug shows antineoplastic activity[1].
MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells[1].
Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q.
RIPK2 inhibitor 1 is a novel potent, selective RIPK2 inhibitor with IC50 of 5-10 nM; potently inhibits the proliferation of cancer cells by > 70% and also inhibits NF-κB activity.
CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity[1].
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent.
FR901465 is a potent anti-cancer and anti-tumor agent. FR901465 can be used for cancer research[1].
Kadsuphilin A can be extracted from Kadsura coccinea (Lem.) and has weak antiproliferative activity[1].
Nicotinic acid riboside is a NAD+ precursor in human cells. Nicotinic acid riboside is an authentic intermediate of human NAD+ metabolism[1][2].
FINO2 is a potent ferroptosis inducer. FINO2 inhibits GPX4 activity. FINO2 is a stable oxidant that oxidizes ferrous iron and stable at varying pH levels. FINO2 causes widespread lipid peroxidation[1].
Socazolimab (ZKAB001) is an anti-PD-L1 monoclonal antibody. Socazolimab has lasting safety and efficacy in the treatment of recurrent or metastatic cervical cancer. Socazolimab also has potential applications in small cell lung cancer, esophageal squamous cell carcinoma (ESCC), advanced urothelial carcinoma and osteosarcoma[1][2][3][4][5].
5'-O-(4,4'-Dimethoxytrityl)-2'-O-methyl-2-thiouridine 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].
Tamoxifen is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.
MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively[1].
Lanreotide (BIM 23014) is a somatostatin analogue with antineoplastic activity. Lanreotide can be used for the research of carcinoid syndrome[1][2].
Aloin(Aloin-A; Barbaloin-A) is a natural antitumor anthraquinone glycoside with iron chelating and non-atherogenic activities.IC50 value:Target:in vitro: Aloin significantly inhibited HUVECs proliferation, migration and tube formation in vitro. suppressed activation of VEGF receptor (VEGFR) 2 and STAT3 phosphorylation in endothelial cells. In addition, the constitutively activated STAT3 protein, and the expression of STAT3-regulated antiapoptotic (Bcl-xL), proliferative (c-Myc), and angiogenic (VEGF) proteins were also down-regulated in response to AL in human SW620 cancer cells [1]. aloin exerted inhibition of cell proliferation, adhesion and invasion abilities of B16-F10 melanoma cells under non-cytotoxic concentrations. Furthermore, aloin induced melanoma cell differentiation through the enhancement of melanogenesis and transglutaminase activity [2].in vivo: Aloin substantially reduced tumor volumes and weight in vivo mouse xenografts, without obviously toxicity [1]. Aloin (10, 30 mg/kg bw) or vehicle was given by gavage to mice after each alcohol administration. Alcohol elevated the serum transaminases alanine aminotransferase, aspartate aminotransferase, total cholesterol and triglyceride levels which were significantly attenuated by the co-administration of aloin (p < 0.05) [3].
NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8+ T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model[1].
TCH-165 is a specific small molecule modulator of proteasome assembly, regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation; enhances the degradation of both α-syn and tau, does not induce the degradation of GAPDH, enhances the degradation of intrinsically disordered proteins in cell culture; display a decrease in assembled 26S and an increase in 20S proteasome in treated cells.
PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
Antiproliferative agent-15 is an anticancer agent. Antiproliferative agent-15 shows antiproliferative activity against human colon (HCT116 and HCT15) and brain (LN-229 and GBM-10) cancer cell lines[1].