ATX inhibitor 9 is a potent inhibitor of ATX. ATX inhibitor 9 is a thickened heteroaryl derivatives compound. Autotaxin (ATX), also known as ENPP2, is a secreted enzyme that is highly expressed mainly in cancer cells, bronchial epithelial cells and alveolar macrophages in the lung. ATX inhibitor 9 has the potential for the research of cancer or fibrous degenerative disease (extracted from patent WO2021078227A1, compound 3)[1].
Biotin-PEG5-amine is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Naxitamab (Hu3F8) is a humanized monoclonal antibody targeting the disialoganglioside GD2. Naxitamab can be used in research of neuroblastoma, osteosarcoma and other GD2-positive cancers[1].
C3 Peptide P16, is a 16 amino acid synthetic peptide derived from human C3d, a fragment generated in trypsin-cleaved C3. C3 Peptide P16 enhances in vitro phosphorylation of pp105 and pp100, a cellular component presenting in the human B lymphoma cells[1][2].
Axl-IN-12 (Example 2) is a potent AXL inhibitor. Axl-IN-12 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals[1].
Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential anti-tumour activity[1].
Marsdenoside A (compound 7) is a Marsdenoside isolated from Alocasia genus. Marsdenoside A has a weak growth inhibitory effect on two tumor cell lines, MGC-803 and HT-29, with IC50 >50 μg/mL.
L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM.
L-Ribulose, an isomer of L-ribose, is an important precursor for other rare sugars and L-nucleoside analogue synthesis[1].
Dovitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
Y-33075 is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.
pan-KRAS-IN-3 (Example 84) is a pan-KRAS inhibitor. pan-KRAS-IN-3 can be used for research of cancers[1].
JHDM-IN-1 (Compound 1) is a Jumonji C domain-containing HDMs (JHDM) inhibitor with IC50s of 3.4, 4.3, 5.9, 10 and 43 μM against JMJD2C, JMJD2A, JMJD2E, PHF8 and JMJD3, respectively[1].
Melengestrol acetate is a progesterone derivative, acts as an orally active corticosteroid hormone to promote endometrial proliferation, pregnancy maintenance, and delay of menstrual activity[1]. Melengestrol Acetate is used as a contraceptive agent for growth promoting effects and suppression of estrus in animals. Melengestrol acetate inhibits both the androgen-dependent and -independent prostatic tumors in vivo and can be used for cancer research[2].
FASN inhibitor 1 is a fatty acid synthase (FASN) inhibitor extracted from patent US20170119786A1, compound 242A.
EF-5 (EF5; 2-Nitroimidazole) is a hypoxia labeling agent used to identify hypoxia in cells.
ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity[1].
Fmoc-Lys(Pal-Glu-OtBu)-OH is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Lys(Pal-Glu-OtBu)-OH is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
AST5902 is the active metabolite of Firmonertinib (HY-112870) (EGFR inhibitor). AST5902 has antineoplastic activity[1][2].
PSB-1901 is a potent A2B adenosine receptor (A2BAR) antagonist with Kis of 0.0835 nM and 0.131 nM for human and mouse A2BARs respectively. PSB-1901 can be used for the research of cancer[1].
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
UNC 669 is a potent antagonist of L3MBTL1(IC50=4.2 uM) and L3MBTL3(IC50=3.1 uM).IC50 value: 4.2 uM/3.1 uM (L3MBTL1/L3MBTL3) [1]Target: L3MBTL1/L3MBTL3
m-PEG3-aldehyde is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Golgicide A is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF), GBF1[1].
HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo[1].
Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development[1][2].
Pip-alkyne-Ph-COOCH3 is an alkyl chain-based PROTAC linker can be used in the synthesis of PROTAC ARD-266[1].
2-Deoxy-D-glucose-13C is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
hCAIX/XII-IN-3 (compound 6q) is a potent and selective hCAIX and hCAXIIinhibitor with Ki values of >10000, >10000, 66.2, 4.4 nM for hCAI, hCAII, hCAIX and hCAXII, respectively[1].
5'''-O-Feruloyl complanatoside B is isolated from Astragali Semen, the seeds of Astragalus Complanatus. Semen Astragali Complanati (SAC) include fatty acids, amino acids, polysaccharides, flavonoids, triterpene glycosides and trace elements; have been reported to involve in chronic diseases such as cardiovascular diseases, diabetes mellitus and cancers[1][2].