3,5-Bis-O-(2,4-dichlorobenzyl)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
KRAS inhibitor-4 (compound F12) is a potent KRAS inhibitor and developed as anticancer agents[1].
Ac-SVVVRT-NH2 is a PGC-1α modulator that modulates the activity of the human PGC-1α promoter (114%). Ac-SVVVRT-NH2 increases PGC-1α mRNA (125%) and accumulation of intracellular lipids (128%) in subcutaneous human adipocytes. Ac-SVVVRT-NH2 can be used in the research of diseases which is modulated by PGC-1α[1].
Coppersensor-1 (CS1) is a boron dipyrromethene (BODIPY)-based fluorescent sensor for selective and sensitive detection of copper(I) ions (Cu+) in biological samples, including live cells[1].
4,5-Diaminofluorescein is a fluorescent detector for nitric oxide (NO) in cells and tissues[1].
3’-O-(2-Methoxyethyl)cytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Bis-PEG5-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activities of EZH2 have been shown by a number of studies in various different cancer types. EZH2-IN-11 has the potential for the research of cancer diseases (extracted from patent WO2019204490A1, compound 17)[1].
(S)-MALT1-IN-5 is a potent inhibitor of MALT1 protease. (S)-MALT1-IN-5 inhibits the activity of MALT1 is expected to be able to correct the enhancement of MALT1 activity due to abnormality of T cell receptor signal or B cell receptor signal, and cancer or inflammatory disease caused by MALT1 activity is expected. (S)-MALT1-IN-5 has the potential for the research of MALT1-related diseases (extracted from patent WO2020111087A1, compound 1)[1].
Hemiasterlin derivative-1 is a hemiasterlin derivative. Hemiasterlin derivative-1 can be used for the synthesis of the Antibody-drug conjugate (ADC)[1].
Cytoglobosin D, a cytochalasan derivative, displays cytotoxic activity toward the A-549 cell line (IC50=2.55 μM)[1].
Promestriene-d3 is the deuterium labeled Promestriene. Promestriene is a synthetic diethyl-ether of estradiol and a locally effective estrogen. Promestriene has an efficient action on vaginal atrophy while it is minimally absorbed[1][2].
Imidazole ketone erastin (IKE) s a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system Xc- and an activator of ferroptosis.
PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader[1].
Ditiocarb (Diethyldithiocarbamic acid) is an accelerator of the rate of copper cementation. Ditiocarb (Diethyldithiocarbamic acid) reduces the incidence of HIV infection, and also enhances adjuvant immunotherapy of high risk breast cancer[1][2][3].
Lacnotuzumab (MCS110) is a neutralizing humanized IgG1/κ monoclonal antibody targeting CSF-1 that prevents CSF-1 from activating the CSF-1R. Lacnotuzumab can be used for the research of pigmented villonodular synovitis[1][2].
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1][2].
2',3'-Didehydro-2',3'-dideoxyuridine 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].
p97-IN-1 is a potent p97 inhibitor with an IC50 <30 nM (WO2015109285A1, compound FF07)[1].
Ospemifene is a selective estrogen for the prevention of postmenopausal osteoporosis with IC50 values of 827nM and 1633nM for ERα and ERβ, respectively. target: ERα and ERβIC50:827 and 1633 nm for ERα and -β, respectively[1] IN vitro: The estrogen-dependent MCF-7 human breast cancer cells were used as a model for studies on the effects of Ospemifene on breast cancer cells. The addition of the compound at concentrations of 0.1 nm to 10 μm did not cause a significant increase in MCF-7 cell growth in vitro when studied by measuring ATP or 3-[4,5-dimethylthiazol-2-yl]2,5-diphenyltetrazolium bromide levels, cell numbers, and rate of [3H]thymidine incorporation during a 7-day culture period. On the other hand, the compound did not inhibit the growth stimulation caused by 1 nm estradiol, except at a concentration 10 mm by only 30%. Similar results were obtained with ZR 75–1 cells, another estrogen-dependent human breast cancer cell line. The cytotoxicity of FC1271a at high concentrations was therefore markedly lower than that for TAM, TOR, or RAL.[1]In ER+ MCF-7 cells, TOR VI and FC-1271a exhibited anti-estrogenic activity. The anti-estrogenic effects of these compounds were less potent as anti-estrogens when compared with TOR and RAL.[2]"In vivo: In the DMBA rat mammary carcinoma model, Ospemifene showed a clear antitumor effect that seemed to be caused primarily by a decrease in the appearance of new tumors but also by a retardation of tumor progression without stimulating the growth of human breast cancer cells.[1]Tumor growth was shown to be inhibited at these doses, indicating anti-estrogenic activity at all doses including 50 and 100 mg/kg Ospemifene. By the end of treatment, MCF-7 tumors in Ospemifene treated mice were statistically smaller compared with control tumors.[2]
Valspodar is a P-glycoprotein (P-gp) inhibitor widely used as overcoming multidrug resistance modulator.
Ingenol is a PKC activator, with a Ki of 30 μM, with antitumor activity.
Tyrosinase-IN-5 (compound 16c) is a potent inhibitor of tyrosinase with an IC50 of 0.02 μM. Tyrosinase-IN-5 efficiently suppresses the melanogenesis without significant toxicity on cells[1].
CG-806 is a pan FLT3/BTK Multi-Kinase inhibitor.
Biotinyl-NH-PEG3-C3-amido-C3-COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
UNC-1062 is a potent and selective Mer kinase inhibitor with IC50 of 1.1 nM, Ki of 0.33 nM; shows improved selectivity and activity against Mer relative to other TAM family RTKs (78-fold selectivity over Axl and 36-fold over Tyro3); inhibits Mer auto-phosphorylation in human pre-B leukemia 697 cells with IC50 of 6.4 nM, also inhibits colony formation in soft agar in tumor cells.
CCK2R ligand CRL is a ligand-linker conjugate; which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker[1].
SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity[1].