Enpp-1-IN-4 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). Enpp-1-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2019177971A1, compound 1)[1].
The first selective, cell-permeable inhibitor of GAG sulfotransferases with IC50 of 2.0-2.5 uM ; displays 8- to 18-fold greater specificity for GAG sulfotransferases compared to cytosolic sulfotransferases; decreases chondroitin sulfate-E (CS-E) and overall sulfation levels on cell-surface and secreted chondroitin sulfate proteoglycans (CSPGs), and reverses CSPG-mediated inhibition of axonal growth.
These compounds show selective inhibition on tumor related subtypes HCA IX and XII, and are also considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.
H-DL-Phe-OtBu.HCl is a phenylalanine derivative[1].
H-D-Ala-OBzl.TosOH is an alanine derivative[1].
(S)-Methyl 2-amino-3-(3-hydroxyphenyl)propanoate hydrochloride is a phenylalanine derivative[1].
Lurasidone is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
DNA-PK-IN-2 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-2 has the potential for the research of cancer diseases (extracted from patent WO2021136462A1, compound 1)[1].
Vitisin B (Compound 5) is iaolated from from Vitis thunbergii var. taiwaniana. Vitisin B has anti-inflammatory effects against lipopolysaccharide(LPS)-induced arthritis[1].
N-(tert-Butoxycarbonyl)-S-butylhomocysteine is a cysteine derivative[1].
2’-β-C-Ethynyladenosine 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].
PF-04217903 methanesulfonate is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).IC50 value: 4.8 nM [1]Target: c-Metin vitro: Being more selective than staurosporine or PF-02341066, PF-04217903 displays >1000-fold selectivity for c-Met over a panel of 208 kinases, although more susceptible to oncogenic mutations of c-Met that attenuate potency than PF-02341066. In addition to WT c-Met, PF-04217903 displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC50 of 3.1 nM, 6.4 nM, and 6.7 nM, respectively, but has no inhibitory activity against c-Met-Y1230C with IC50 of >10 μM [1]. PF-04217903 in combination with sunitinib significantly inhibits endothelial cells, but not the tumor cells B16F1, Tib6, EL4, and LLC [2] PF-04217903 significantly inhibits the clonogenic growth of LXFA 526L and LXFA 1647L with IC50 values of 16 nM, and 13 nM, respectively, yielding an additive effect when in combination with cetuximab [3]. in vivo: Although unable to inhibit tumor growth in the sunitinib-sensitive B16F1 and Tib6 tumor models, the combination of PF-04217903 and sunitinib significantly inhibits tumor growth in sunitinib-resistant EL4, and LLC tumor models compared with sunitinib or PF-04217903 alone by significantly blocking vascular expansion, indicating a functional role for HGF/c-Met axis in the sunitinib-resistant tumors [2].
3’-beta-C-Methyl-N6-methyladenosine is an adenosine analogue. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. The popular products in this series are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Lauric acid-d5 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Curcapicycloside (Pilosidine), a norlignan glucoside, exhibits antibacterial activity against Escherichia coli[1].
PI3K-IN-35 (Compound 6l) is a highly selective PI3K inhibitor with IC50 values of 13.98, 7.22 and 10.94 μM for PI3K-α、PI3K-β and PI3K-δ, respectively. PI3K-IN-35 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-35 can be used in leukemia research[1].
DIZ-3 is a selective multimeric G4 ligand based on a G4-ligand-dimerizing strategy. DIZ-3 intercalates into the G4-G4 interface, stabilizing the higher-order structure. DIZ-3 induces cell cycle arrest and apoptosis, and thus inhibits cell proliferation in alternative lengthening of telomere (ALT) cancer cells[1].
OJV-VI is found in ophiopogonis[1].
PQDVKFP is a synthetic peptide, recognizing antigenic domains within the hepatitis C virus (HCV) core protein[1].
MALT1-IN-3 (compound 122) is a potent MALT1 protease inhibitor, with an IC50 of 0.06 μM. MALT1-IN-3 has IC50 of 0.14 and 0.13 μM for human IL6/IL10 in OCI-LY3 cells, respectively[1].
Jesaconitine is a toxic alkaloid. Jesaconitine can be derived from Aconitum. Jesaconitine is one of the major metabolites that can be detected in the blood of the right atrium after aconitum poisoning. Various types of arrhythimia are characteristic in aconitine intoxication[1].
ARM1 (4BSA) is a potent aminopeptidase and epoxide hydrolase inhibitor. ARM1 shows aminopeptidase inhibitory activity with an IC50 7.61 µM and epoxide hydrolase inhibitory activity with an IC50 12.4 µM[1].
N-(4-Azido-2-nitrophenyl)-N''-biotinylnorspemidine (Compound 4) is a biotin derivative[1].
Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor[1].
GA3-AM is a cell permeable analog of the plant hormone gibberellic acid that acts as a chemical dimerizer or chemical inducer of dimerization[1].
(S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsive agent. (S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19. (S)-Mephenytoin can be used for the analysis of cytochrome P450 metabolism[1][2].
A novel potent gonadotrophin releasing hormone (GnRH) antagonist.
SP-420 is a desferrithiocin analogue with iron-clearing efficiency with ICE value of 26.7; more potent than desferrithiocin.
Fmoc-PEG4-Ala-Ala-Asn-PAB is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
3-Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-Dehydrotrametenolic acid induces apoptosis and has anticancer activity[1][2].