SPA70 is a potent and selective hPXR antagonist (IC50=0.51 uM) that interacts with the ligand-binding domain (LBD) of hPXR, inhibits hPXR in human hepatocytes and mouse models and enhances the chemosensitivity of cancer cells; displays highly selectivity over 10 other nuclear receptors (FXR, LXR, RXR, PPAR, etc.); antagonizes hPXR target genes induced by various hPXR agonists, blocks hPXR-mediated drug metabolism in vivo.
CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.
2'-OMe-G(ibu) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity[1].
BMS-986020 is an LPA1 antagonist.target: LPA1BMS-986020 is in Phase 2 clinical development for treating idiopathic pulmonary fibrosis. BMS-986020 selectively inhibits the LPA receptor, which is involved in binding of the signaling molecule lysophosphatidic acid, which in turn is involved in a host of diverse biological functions, such as cell proliferation, platelet aggregation, smooth muscle contraction and others.
ICMT-IN-52 (compound 44) is an inhibitor of ICMT (IC50=0.052 μM)[1].
B-Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
Amatuximab (MORab-009) is a chimeric, humanized IgG1/k MAb that targets the cell surface mesothelin (MSLN). Mesothelin is a glycosylphosphatidyl inositol (GPI)-anchored membrane glycoprotein, which is present in a restricted set of normal adult tissues such as the mesothelium[1][2].
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes[1].
Seco-DUBA is a duocarmycin (DUBA) prodrug containing two hydroxyl groups, which can each be used for coupling to an antibody via a linker. Seco-DUBA can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
Rovadicitinib hydrochloride is a JAK inhibitor with an IC50 value <20 nM. Rovadicitinib hydrochloride also exhibits anti-inflammatory activity[1][2].
Anti-melanoma agent 1 (Compound 5m) is an anti-melanoma agent and induces cell apoptosis[1].
Lanatoside E is a cyclic triterpene saponin with antitumor activity[1].
Thalidomide-O-C7-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Pomalidomide-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1[1][2].
2-Methoxyestradiol is an angiogenesis inhibitor and apoptosis inducer with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules.
SAR405838 is a highly potent and selective MDM2 inhibitor, binds to MDM2 with Ki= 0.88 nM and has high specificity over other proteins.IC50 value: 0.88 nM (Ki) [1]Target: MDM2in vitro: SAR405838 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells.[1] SAR405838 effectively induces apoptosis in the RS4;11 cell line. SAR405838 potently inhibits cell growth and induces dose-dependent apoptosis in the ABTR1 and ABTR2 sublines, albeit with modestly reduced potency compared with that in the control RS4;11 cell line.[2]in vivo: At well-tolerated dose schedules, SAR405838 achieves either durable tumor regression or complete tumor growth inhibition in mouse xenograft models of SJSA-1 osteosarcoma, RS4;11 acute leukemia, LNCaP prostate cancer and HCT-116 colon cancer. Remarkably, a single oral dose of SAR405838 is sufficient to achieve complete tumor regression in the SJSA-1 model. In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,). [1]
5’-Deoxy-5’-iodo-2’-O-methyl-5-methyluridine 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].
Viomycin is a potent antibiotic against Mycobacteria. Viomycin rapidly inhibits polypeptide chain elongation when added to purified endogenous Escherichia coli polysomes actively engaged in polypeptide synthesis[1][2].
6-Hydroxy-DOPA is a selective and effective allosteric inhibitor of the RAD52 ssDNA binding domain. 6-Hydroxy-DOPA can be used for the research of cancer[1].
PROTAC Linker 14 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 14 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Mirin is a small-molecule inhibitor of MRN (Mre11, Rad50, and Nbs1) complex.Target: in vitro: Mirin was shown to block Mre11 exonuclease activity and MRN-dependent ATM activation, and to inhibit the ionizing radiation-induced G2/M checkpoint and homologous recombination in mammalian cells. Mirin inhibition of ATM activation is independent of Mre11 nuclease inhibition since the M(HN)RN and M(HL/DV)RN mutant complexes are inhibited equivalently to the wild-type enzyme despite the fact that they are nuclease-deficient. The effects of Mirin have been ascribed to its effects on Mre11 nuclease activity, but as we show here, Mirin is inhibitory of MRN function independent of the nuclease activity of the complex. [2] Addition of the Mre11 inhibitor Mirin to egg extracts and mammalian cells reduces RCC1 association with mitotic chromosomes. HeLa cells expressing Histone H2B-EYFP were treated with Mirin (25 or 50 μM), and mitotic progression was immediately monitored using live cell imaging. Although Mirin-treated cells were able to congress chromosomes to the metaphase plate with similar kinetics as untreated cells, a significant fraction of Mirin-treated cells paused for extended periods of time in a metaphase-like stage without anaphase onset . [1]
PBRM1-BD2-IN-4 (compound 15) is a potent PBRM1 Bromodomain inhibitor with Kd values of 5.5 μM and 11.1 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.2 μM for PBRM1-BD2. PBRM1-BD2-IN-4 can be used to research anticancer[1].
(-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.
Anticancer agent 74 is a moderate anticancer agent. Anticancer agent 74 has lower selectivity and cytotoxicity than doxorubicin to normal cell[1].
Pivekimab is a human monoclonal IgG1 antibody targeting interleukin 3 (IL-3). Pivekimab is a CD123-targeting antibody-drug conjugate. Pivekimab can be used in research of blastic plasmacytoid dendritic cell neoplasm (BPDCN)[1].
GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2/13/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes.
2’-Deoxy-2’-fluoro-N3-(2S)-(2-amino-3-carbonyl] propyl-beta-D-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].