Ostarine(MK-2866; GTX-024) is a modulator of human androgen receptor.IC50 value:Target: androgen receptorOstarine (MK-2866) is an androgen receptor modulator (SARM) with an ED50 of 0.44 mg/day. Ostarine (MK-2866) has anabolic activity. Lack of PSA increases in men and hair growth in women further corroborated selective anabolic effects of Ostarine (MK-2866). Ostarine (MK-2866) also resulted in a dose-dependent decrease in LDL and HDL cholesterol levels, with the average LDL/HDL ratio for all doses remaining in the low cardiovascular risk catergory.
4-(Benzo[d]oxazol-2-yl)aniline is a potent antitumor agent. 4-(Benzo[d]oxazol-2-yl)aniline has inhibitory activity against mammary carcinoma cell lines[1].
Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC50 of 2.1 nM for CDK6[1].
VERU-111 (ABI-231) is a potent and orally bioavailable α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer[1][2][3].
Sprengerinin is a potential angiogenesis inhibitor. Sprengerinin exerts anti-tumorigenic effects in vitro[1].
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities[1][2].
Betifisolimab (MSB-2311) is a humanized monoclonal antibody directed against the immunosuppressive ligand PD-L1. Betifisolimab has the potential for advanced solid tumors and hematological malignancies research[1].
Peplomycin (Bleomycin PEP; Pepleomycin) is an antibiotic analogue of Bleomycin (HY-108345), with high antitumor effect and less pulmonary toxicity. Peplomycin induce apoptosis in oral squamous carcinoma cell line SSCKN cells and pulmonary fibrosis in rats[1][2][3][4].
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3[1].
MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation[1].
MC-VA-PABC-MMAE is a drug-linker conjugate for ADC. MC-VA-PABC-MMAE contains the ADCs linker (peptide MC-VA-PABC) and a potent tubulin polymerization inhibitor MMAE (HY-15162)[1][2].
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma[1].
Tigatuzumab (CS-1008) is a humanized IgG1 monoclonal antibody targets death receptor 5 (DR5). Tigatuzumab induces cell Apoptosis of cancer cells and inhibits tumor growth in vivo. Tigatuzumab can be used for the research of cancer[1].
Boserolimab (MK-5890) is a chimeric humanized IgG1κ antibody targeting the mouse signaling regulatory protein CD27.
Garsorasib is a potent inhibitor of KRAS G12C with an IC50 of 10 nM. Garsorasib has the potential for the research of various cancer such as pancreatic cancer, endometrial cancer, colorectal cancer, or lung cancer (non-small cell lung cancer) (extracted from patent WO2020233592A1, compound 2)[1].
PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction[1].
KTX-582 intermediate-3 is an intermediate in the synthesis of KTX-582 (HY-148274) and can be used for ADC preparation. KTX-582 is an IRAK4 degrader and inducer of apoptosis with DC50 of 4 nM and 5 nM for IRAK4 and Ikaros, respectively[1].
S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
AGI-24512 is a methionine adenosyltransferase 2A (MATA2 ) inhibitors useful for treatment of cancer. AGI-24512 blocks growth of MTAP-deleted cancer cells in vitro.
SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively[1]. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration[2].
PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit[1].
Polyphyllin VI, an active saponin mainly isolated from traditional medicinal plant Paris polyphylla, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis[1][2].
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM)[1][2].
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer[1].
Antitumor agent-119 (compound 13K) is a 2-benzoxazolyl hydrazone derivative with anticancer activities. Antitumor agent-119 inhibits the cell growth of Butkitt, CCRF-CEM, HeLa, and HT-29 with IC50 values of 30 nM, 140 nM, 100 nM, and 40 nM, respectively[1].
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.
PROTAC CDK9 Degrader-1 is a selective CDK9 degrader.
Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect[1].
Thalidomide-O-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].