Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels.
N4-Benzoyl-5'-O-DMT-2'-O-propargyl adenosine 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].
CHIR-99021 is a GSK-3α/β inhibitor with an IC50 of 10 and 6.7 nM，showing 500-fold selectivity over its closest homologs CDC2 and ERK2, as well as other protein kinases.
TSPO ligand-3 is a ligand of AUTAC2. AUTAC2 contains an p-fluorobenzylguanine (FBnG) and an synthetic ligand of FKBP (SLF) moiety, which can cause significant silencing of FKBP12 in HeLa cells[1].
3’-N-Acetyl-3’-amino-3’-deoxyuridine 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].
CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC50 of 3 nM and a Ki of 1.16 nM.
CNDAC is a major metabolite of oral drug sapacitabine, and a nucleoside analog.
LTV-1 is a highly potent, cell-permeable and reversible inhibitor of lymphoid tyrosine phosphatase (LYP) (IC50 = 508 nM). IC50 value: 508 nMTarget: LYPin vitro: LTV-1 inhibits LYP in a dose-dependent manner at low- and sub-micromolar concentrations in T cells. LTV-1 enhances TCR signaling in intact cells. Exhibits competitive to mixed mode of inhibition (Ki = 384 nM). LTV-1 inhibits the mutant, disease associated LYP-Trp620 activity. LTV-1 blocks the action of the mutant LYP protein in human T cells.
ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC50 value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.
RORγt inhibitor 2 (Compound 119) is a potent RORγt inhibitor with an IC50 of 9.2 nM. RORγt inhibitor 2 can be used for the research of cancer, inflammation or autoimmune diseases mediated by RORγt[1].
BT1718 is a bicyclic anticancer peptide targeting MT1-MMP. BT1718 uses MT1-MMP to target tumors and promote delivery of the cytotoxic payload Mertansine (HY-19792). BT1718 is a bicycle toxin conjugate with a KD value of 3 nM. MT1-MMP is overexpressed in a variety of advanced solid tumors, including triple-negative breast cancer (TNBC), non-small cell lung cancer[1][2].
Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
Bavituximab (Anti-Human Phosphatidylserine Recombinant Antibody) is a phosphatidylserine (PS)-targeting monoclonal antibody, suppresses tumor growth by targeting tumor vasculature and reactivating antitumor immunity. Bavituximab plus Paclitaxel (HY-B0015) and Carboplatin (HY-17393), have enhanced inhibition on non-small-cell lung cancer[1].
BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.
WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
PROTAC RAF degrader 1 (compound 512) is a PROTAC RAF degrader. PROTAC RAF degrader 1 induces targeted degradation of BRAF mutants (DC50: 5.4 nM, 4.64 nM, 15.5 nM, 2.11 nM, 63.9 nM for BRAF V600E, V600K, G464V, G469A, K601E respectively). PROTAC RAF degrader 1 has anti-tumor activity. PROTAC RAF degrader 1 can be used for research of disorders that result from aggregation or accumulation of RAF, or the constitutive activation of RAF[1].
S6K1-IN-DG2 (Compound 66) is a p70S6K inhibitor (IC50: < 100 nM)[1].
VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.
Rodorubicin (Cytorhodin S) is a tetraglycosidic anthracycline with preclinical antitumor activity[1].
Tafasitamab is an Fc-modified, humanized monoclonal antibody that binds to the human B-cell surface antigenCD19[1][2].
Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity[1]. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation[2].
RU-301 is a pan-TAM receptor inhibitor, exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively[1].
Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.
N3-PEG3-CH2CH2-Boc is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. N3-PEG3-CH2CH2-Boc is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[2].
Sibrotuzumab (BIBH 1) is a humanized IgG1 monoclonal antibody targets fibroblast activation protein (FAP). Sibrotuzumab can be used for the research of colorectal cancer and non-small cell lung cancer (NSCLC)[1].
Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.
TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
SV40 T-Ag-derived NLS peptide is a nuclear localization signal DNA tagged to this peptide efficiently translocates into the cell nucleus[1].
Orientin is a naturally occurring bioactive flavonoid that possesses diverse biological properties, including anti-inflammation, anti-oxidative, anti-tumor, and cardio protection. Orientin is a promising neuroprotective agent suitable for therapy for neuropathic pain[1][2].