Fmoc-3VVD-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
K858 Racemic is an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM.
IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma[1].
RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors[1].
PEG4 linker is an ADC linker for the drug ADCT-502 (anti-Her2 Ab). ADCT-502 can be used to treat breast cancer[1].
4-Hydroxy-1-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)-2(1H)-pyridinone 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].
Momelotinib-d8 (CYT387-d8) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally acitve and ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively, shows much less activity against JAK3[1][2].
Benzyl-PEG8-Ots is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Fmoc-L-Asn(beta-D-GlcNAc(Ac)3)-OH (Fmoc-Asn(Ac3AcNH-beta-Glc)-OH) can be used in the synthesis of silicon-fluoride acceptor (SiFA) derivatized octreotate derivatives. SiFA-octreotate analogues, as tumor imaging agents, are useful tool for the research of positron emission tomography (PET)[1].
L-albizziin, as a sulfhydryl group reagent, is a glutamase inhibitor. L-albizziin can be used for the research of cancer[1].
Fosciclopirox suppresses growth of urothelial cancer by targeting the γ-secretase complex. Fosciclopirox selectively delivers the active metabolite, Ciclopirox (CPX), to the entire urinary tract[1][2]. Ciclopirox has anticancer activity in a number of solid and hematologic malignancies.
m-PEG4-azide (13-Azido-2,5,8,11-tetraoxatridecane) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription with IC50 of 5 μM.
Troxacitabine is nucleoside analog with potent anticancer activity.
Minimolide F is a sesquiterpene lactone. Minimolide F has inhibitory activity against human nasopharyngeal cancer cells. Minimolide F can be used for the research of cancer[1].
Emibetuzumab (LY2875358) is a humanized bivalent MET antibody (IgG4 type). Emibetuzumab shows high neutralization and internalization activities, resulting in inhibition of both HGF-dependent and HGF-independent MET pathway activation and tumor growth. Emibetuzumab can be used in study of cancer[1].
Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.
Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity[1].
Denileukin diftitox (DAB 389IL-2) is a diphtheria toxin (DT)-related interleukin 2 (IL-2) fusion protein toxin that depletes cells expressing the high-affinity form of the IL-2 receptor (IL-2R), CD25. Denileukin diftitox binds to cells expressing IL-2R and inhibits protein synthesis through internalization of the diphtheria toxin fragment[1][2][3].
Cloxacillin is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins[1][2][3].
HUHS015 is a potent PCA-1/ALKBH3 inhibitor both in vitro and in vivo. The bioavailability (BA) of HUHS015 was 7.2% in rats after oral administration. Continuously administering HUHS015 significantly suppressed the growth of DU145 cells, which are human hormone-independent prostate cancer cells, in a mouse xenograft model without untoward effects. [1]
Wnt/β-catenin agonist 4 (Derivative 83) is an agonist of Wnt that activates Wnt/β-catenin signal transmission[1].
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC)[1].
Hydroxy-PEG2-C2-PFP ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs.
FGFR-IN-4 is a potent inhibitor of FGFR. Fibroblast growth factor receptor (FGFR) is a tyrosine kinase receptor that binds to fibroblast growth factor ligands. FGFR-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2022033532A1, compound 20)[1].
Alexidine, a bis-biguanide, exhibits antifungal and antibiofilm activity against a diverse range of fungal pathogens. Alexidine is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis[1].
c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer. IC50 value:Target: c-MetMore details please refer to Patent WO 2012015677 A1.
N-Acetylputrescine (NAP) is an endogenous metabolite widely present in animals and plants. N-Acetylputrescine can be used as a biomarker for lung squamous cell carcinoma (SCCL) and Parkinson's disease (PD) for disease diagnosis[1][2][3].
MC-Val-Cit-PAB-vinblastine has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-vinblastine is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
NC-043 (15-Oxospiramilactone) is a diterpenoid derivative inhibitor of Wnt/β-catenin signaling that interferes with the β-catenin/TCF4 association; decreases the mRNA and/or protein expression of Wnt target genes Axin2, Cyclin D1 and Survivin in SW480 cells, inhibits anchorage-independent growth and xenograft tumorigenesis in vitro and in vivo; inhibits canonical Wnt signaling downstream of β-catenin stability, causes G2/M arrest and inhibits colon cancer cell growth.