FR 901537 is a potent and competitive aromatase inhibitor. FR 901537, a novel naphthol derivative, has the potential for breast cancer research[1].
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader[1].
Fumarate hydratase-IN-1, an enzyme of the TCA cycle. Inhibition of fumarate hydratase-IN-1 can contribute to tumorigenicity in some cells. The use of a photoaffinity labeling strategy identified fumarate hydratase as the principal pharmacological target.[1]In vitro: The activity of this enzyme was measured using a well-established assay that monitored the conversion of fumarate into L-malate and subsequent oxidation of L-malate to oxaloacetate by malate dehydrogenase. Initial controls established that neither the carboxylic acid 3 nor ester 2 inhibited malate dehydrogenase Using this two-enzyme protocol we found that carboxylic acid 3 inhibited fumarate hydratase in a dose-dependent fashion in vitro. Besides, inhibition of fumarate hydratase can contribute to tumorigenicity in some cells.[1]
(2,4,6-Trichloro-3-hydroxy-5-methoxyphenyl)methyl β-D-glucopyranoside (Compound 1) is a chlorophenyl glycoside that can be isolated from Lilium regale. Lilium regale is used for research of lung ailments[1].
GSK2110183 is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.
MC-AlkyMC-Alkyl-Hydrazine is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI can be used as a probe for FAP-targeted tumour imaging. NOTA-FAPI has good tumour detection efficacy and excellent imaging quality[1].
(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas[1][2].
BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity[1][2].
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines[1].
IDO-IN-18 (Compound 00815) is an IDO inhibitor. IDO-IN-18 can be used for research of immunosuppression associated infectious or cancer diseases[1].
MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.
Fascaplysin is an antimicrobial and cytotoxic red pigment, that can come from the marine sponge (Fascaplysinopsis sp.). Fascaplysin has been synthesized in seven steps from indole (65% yield). Fascaplysin can induces apoptosis and autophagy in human leukemia HL-60 cells. Fascaplysin shows anti-tumor activity[1][2].
NBD-Arg-Pro-Lys-Pro-Leu-Ala-Nva-Trp-Lys-(DMC)-NH2 is an substrate for hydrolysis of the matrix metalloproteinase stromelysin (MMP-3) and can be easily detected at Abs/Em=350/465 nm[1].
Infigratinib phosphate (BGJ-398 phosphate) is a potent inhibitor of the FGFR family with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
Taltobulin intermediate-2 is an intermediate in the synthesis of Taltobulin (HY-15584). Taltobulin is a common toxin component in ADC preparation (ADC Cytotoxin), and it is also a powerful tubulin (Microtubule/Tubulin) inhibitor. Taltobulin disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis[1].
E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway[1].
Raloxifene-d10-1 is the deuterium labeled Raloxifene[1]. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[2].
FDW028 a potent and highly selective FUT8 inhibitor. FUT8 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the chaperone-mediated autophagy (CMA) pathway. FDW028 can be used for metastatic colorectal cancer (mCRC) research[1].
CBP/p300-IN-14 is a potent inhibitor of CBP/EP300 (lysine acetyltransferase) with an IC50 of 3.3 nM (extracted from patent WO2021213521A1, compound 27)[1].
DpC is an anti-tumor agent. DpC inhibits cancer cell proliferation (IC50: 0.007-0.096 渭M). DpC synergizes with multiple anti-cancer therapeutics[1].
Potassium tert-butyl malonate is an intermediate in the synthesis of malonate monoester potassium salt[1].
GADGVGKSAL is a mutant KRAS G12D 10mer peptide. GADGVGKSAL can be used as an immunogenic neoantigen for cancer immunotherapy research[1].
HBV-IN-23 (Compound 5k) is an inhibitor of HBV DNA replication with an IC50 of 0.58 µM. HBV-IN-23 inhibits HBV DNA replication in both drug sensitive and resistant HBV strains. HBV-IN-23 shows anti-hepatocellular carcinoma cell (HCC) activities. HBV-IN-23 induces HepG2 cells apoptosis[1].
(S,R,S)-AHPC-C3-NH2 (dihydrochloride) is the dihydrochloride form of (S,R,S)-AHPC-C3-NH2 (HY-130711). (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader[1].
Furomollugin is a natural product with antioxidant and antibacterial activities, can be isolated from Rubia cordifolia. Furomollugin lacks potent anti-tyrosinase activity, but also exhibits significant anticancer property[1].
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC)[1].
AZD3147 is a potent, orally active, selective dual inhibitor of mTORC1 and mTORC2 with an IC50 value of 1.5 nM. AZD3147 also has a selective effect on PI3K[1].
Corixetan is a highly efficient thorium chelator. Corixetan can efficiently complex Th-227 with sufficient in vivo stability[1].