5'-Deoxy-5'-iodoguanosine 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].
Cortistatin-29 (human) is a somatostatin neuropeptide with potential for studying diseases such as cancer, inflammation, autoimmunity, fibrosis, and pain[1][2].
Propargyl-PEG5-Br is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Pinosylvin is a pre-infectious stilbenoid toxin isolated from the heartwood of Pinus spp, has anti-bacterial activities[1]. Pinosylvin is a resveratrol analogue, can induce cell apoptosis and autophapy in leukemia cells[2].
1-Monopalmitin, a bitter melon extract, inhibits the P-glycoprotein (P-gp) activity in intestinal Caco-2 cells[1].
OTS514 is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM.
Vorolanib (CM082; X-82) is an orally active, multikinase VEGFR/PDGFR inhibitor. Vorolanib minimizes toxicity, disrupts tumor angiogenesis and tumor cell proliferation, and induces of tumor cell death[1].
SOS1 agonist-1 (compound 79) is an agonist for the Son of sevenless homologue SOS1. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP to GTP on RAS and regulates RAS activation. SOS1 agonists increase nucleotide exchange on RAS, enhance cellular RAS-GTP levels, and trigger biphasic signaling changes in ERK1/2 phosphorylation. Play an anti-cancer role[1].
Enpp-1-IN-13 (Compound 1a) is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP) inhibitor with IC50 values of 1.29 μM and 20.2 μM against ENPP1 and ENPP3, respectively. Enpp-1-IN-13 shows anticancer activity[1].
Val-Cit-PABC-Ahx-May is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Thalidomide-NH-C10-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
Dorsomorphin is a potent and selective AMPK inhibitor, that is competitive with ATP, with Ki=109±16 nM in the absence of AMP.
Boc-NH-PEG2-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4 (IRAK4). PROTAC IRAK4 ligand-1 can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966)[1].
KY386 is a potent, selective inhibitor of DHX33 helicase, with the IC50 of 19 nM. KY386 inhibits U251-MG cells (DHX33-overexpressing cancer cell strain) with IC50 of 20 nM.and shows potent anti-cancer activity and moderate metabolic stability[1].
1αH,5αH-Guaia-6-ene-4β,10β-diol is a sesquiterpenoid derivative identified from Alisma orientale. 1αH,5αH-Guaia-6-ene-4β,10β-diol has anti-cancer activities[1].
YW2065 has excellent anti-colorectal cancer effects in vitro and in vivo. YW2065 achieves its inhibitory activity for Wnt signaling by stabilizing Axin-1, a scaffolding protein that regulates proteasome degradation of β-catenin. Simultaneously, YW2065 also led to the activation of the tumor suppressor AMPK, providing an additional anticancer mechanism. In addition, YW2065 showed favorable pharmacokinetic properties without obvious toxicity.
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on PROTAC. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins[1].
2'-O-Me-C(Bz) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
Aminooxy-PEG5-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.IC50 Value: Target: DPYDin vitro: Gimeracil had radiosensitizing effects by partially inhibiting homologous recombination (HR) in the repair of DNA double strand breaks. Tail moments in neutral comet assay increased in gimeracil-treated cells. Gimeracil restrained the formation of foci of Rad51 and replication protein A (RPA), whereas it increased the number of foci of Nbs1, Mre11, Rad50, and FancD2. Gimeracil did not sensitize DPYD-depleted cells [1]. Gimeracil inhibited DNA DSB repair. It did not sensitize cells deficient in HR but sensitized those deficient in NHEJ. In SCneo assay, Gimeracil reduced the frequency of neo-positive clones. Additionally, it sensitized the cells in S-phase more than in G0/G1 [2].in vivo:
2’,3’,5’-Tri-O-acetyl 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].
AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively[1].
A novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells; enhances p53 transcriptional activity and restores wt-like DNA binding ability to mut p53R280K; inhibits the growth of wt/mut p53-expressing tumors in xenograft mice models, without apparent toxicity.
(-)-Cleistenolide is a α,β-unsaturated δ-lactone isolated from Cleistochlamys kirkii Oliver. (-)-Cleistenolide has antibacterial and antitumor activity[1].
YEQLRNSRA is a MycC peptide[1].
SOS1-IN-5 is a potent inhibitor of SOS1. SOS1-IN-5 is a pyrimidobicyclic derivative. SOS1-IN-5 blocks the activation of KRAS by interfering with RAS-SOS1 interaction, and achieves the purpose of broad-spectrum inhibition of KRAS activity. SOS1-IN-5 has the potential for the research of cancer diseases (extracted from patent WO2021203768A1, compound 4)[1].
Betulin diacetate, a natural diterpene, is an anti-AID agent and also possesses anti-cancer activity[1][2].
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia[1].
BML-190(IMMA) is a potent and selective CB2 receptor ligand (Ki values are 435 nM and > 2 μM for CB2 and CB1 respectively). IC50 Value: 435 nM(Ki CB2)Target:CB2 receptorin vitro: BML-190 increases the accumulation of cAMP, via forskolin-stimulated mechanism in HEK-293 cells. Alternate studies suggest that BML-190 reduces the toxicity of culture supernatants to SH-SY5Y human neutroblastoma cells. Various research suggests that BML-190 is an essential tool in studying the proliferation of neuroblastoma. BML-190 diminishes LPS-induced NO and IL-6 production in a concentration-dependent manner. BML-190 also inhibits LPS-induced PGE2 production and COX-2 induction. in vivo: