Enzyme Inhibitors

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D0817 (−)-Deguelin >98% (HPLC), powder Inhibitor of activated Akt. Does not affect MAPK, ERK1/2, or JNK. Anticancer, chemoprotective agent.
C9911 (S)-(+)-Camptothecin ≥90% (HPLC), powder (S)-(+)-Camptothecin binds irreversibly to the DNA-topoisomerase I complex, inhibiting the reassociation of DNA after cleavage by topoisomerase I and traps the enzyme in a covalent linkage with DNA. The enzyme complex is ubiquinated and destroyed by the 26S proteasome, thus depleting cellular topoisomerase I. Blocks the cell cycle in S-phase at low does and induces apoptosis in a large number of normal and tumor cell lines by cell cycle-dependent and cell cycle-independent processes.
377627 2-Imino-1-imidazolidineacetic acid 98% Creatine analog that protects tissues from ischemic damage; decreases the rate of ATP production via creatine kinase and reduces the proliferation of tumor cell lines that are characterized by high levels of creatine kinase expression.
P6273 2-Propylpentanoic acid 2-Propylpentanoic acid is a short-chain fatty acid and potentially inhibits histone deacetylase action. It is known to promote tumor cell toxicity and increase susceptibility to radiation. 2-Propylpentanoic acid elevates the levels of γ-aminobutyric acid in the brain. Reduced central nervous system action is observed in overdosage of 2-propylpentanoic acid. It enhance the inhibitory action of γ-aminobutyric acid (GABA) by blocking voltage-dependent sodium channel.
Anticonvulsant that also has efficacy as a mood stabilizer in bipolar disorder
D9568 3,3′-Diindolylmethane ≥98% (HPLC) Acid-catalyzed reaction product of a phytochemical naturally found in Brassicaceae, indole-3-carbinol. It functions as an antitumor agent. This derivative can both directly stimulate apoptosis at relatively high concentrations and sensitize TRAIL-induced apoptosis in human cancer cells. DIM induces a G1 cell cycle arrest in human breast cancer MCF-7 cells by a mechanism that includes increased expression of p21. DIM is a strong mitochondrial H+-ATPase inhibitor. The function of DIM and its derivatives as a new plant growth promoter has been studied in an eco-friendly system.
H0165 7-Ethyl-10-hydroxycamptothecin ≥98% (HPLC), powder Active metabolite of irinotecan. Inhibitor of topoisomerase I.. Gene expression analysis of colon cancer cell lines treated with SN-38 showed differential effects: the majority of affected genes were down-regulated (including, most strongly, genes related to receptor and kinase activity, signal transduction, apoptosis, RNA processing, protein metabolism and transport, cell cycle and transcription. Some of the up-regulated genes were involved in apoptosis, transcription, development and differentiation.
A9657 DL-Aminoglutethimide DL-Aminoglutethimide is a derivative of the sedative glutethimide. Originally introduced as an anticonvulsant, it was found to cause adrenal insufficiency. Blocks adrenal steroidogenesis by inhibiting the enzymatic conversion of cholesterol to pregnenolone. It also blocks the peripheral conversion (aromatization) of androgenic precursors to estrogens. The D-isomer is 30 times more potent at inhibiting aromatase activity, whereas the L-isomer is more potent at inhibiting cholesterol side-chain cleavage (steroidogenesis).
A8851 Apicidin ≥98% (HPLC), from microbial Apicidin is a potent inhibitor of histone deacetylase (HDAC). It particularlyinhibits histone deacetylase 1 and 3 (HDAC1 and HDAC3). Apicidin exhibits anti-protozoal activity against apicomplexan metabolite produced by parasites. It also possesses anti-proliferative activity against several cancer cell lines. Apicidin shows anti-cancer activity against human acute promyelocytic leukemia cell.
B178 Butein solid Butein exhibit several pharmacological activities, such as anti-oxidant and anti-inflammatory activity. It stimulates apoptotic cell death of human cervical cancer cells. It has therapeutic potentials for chronic diseases, including liver tuberculosis, obesity, diabetes and hypertension. Butein can repress migration and invasion of bladder, breast and pancreatic cancer cells.
Inhibits EGFR and Src tyrosine kinase activities; inhibits cAMP-dependent PDE-IV. Induces apoptosis in B16 melanoma cells and HL-60 human leukemia cells.
E1383 Etoposide synthetic, 98.0-105.0%, powder Etoposide is an antitumor agent that complexes with topoisomerase II and DNA to enhance double-strand and single-strand cleavage of DNA and reversibly inhibit religation. Blocks the cell cycle in in S-phase and G2-phase of the cell cycle; induces apoptosis in normal and tumor cell lines; inhibits synthesis of the oncoprotein Mdm2 and induces apoptosis in tumor lines that overexpress Mdm2.
Etoposide is used in treating advanced testicular cancer, Kaposi′s sarcoma, non-small cell lung cancer (NSCLC), SCLC (small cell lung cancer) and lymphoma.
F2552 Formestane solid Aromatase inhibitor used as an anti-cancer agent against estrogen-dependent tumors.
F4425 Fostriecin sodium salt from Streptomyces pulveraceus ≥98% (HPLC) Fostriecin is a natural inhibitor of serine/ threonine phosphatases. It is a phosphate monoester produced by fermentation beer of Streptomyces pulveraceus. Fostriecin is a strong inhibitor of protein phosphatases type 2A and 4 (PP2A and PP4) and a weak inhibitor of protein phosphatases type 1 and 5 (PP1 and PP5). It exhibits anti-tumor activity against several tumor cells in vitro and L1210 and P388 leukemias in vivo. The anti-tumor activity of fostriecin is due to its ability to interfere with the reversible phosphorylation of proteins that are involved in the progression of the cell cycle. It also exhibits cytotoxic effects. Fostriecin can inhibit the DNA, RNA and protein synthesis.
H5257 Hispidin solid, ≥98% (HPLC) Hispidin exhibits robust antioxidant, anticancer and antidiabetic properties. It has the ability to guard against peroxynitrite-mediated cytotoxicity, DNA damage and the development of hydroxyl radicals.
Potent inhibitor of protein kinase Cβ, cytotoxic for cancer cells.
I7378 Indomethacin 98.5-100.5% (in accordance with BP) Cyclooxygenase (COX) inhibitor that is relatively selective for COX-1.
M2147 Mevinolin from Aspergillus sp. ≥98% (HPLC) Lovastatin is a cholesterol lowering drug and competitive inhibitor of HMG-CoA reductase, a rate limiting enzyme in cholesterol synthesis. Blocks the production of mevalonate, a critical compound in the production of cholesterol and isoprenoids. This product is a substrate of Pgp and CYP3A. It increases cellular resistance to anticancer agents such as doxorubicin and induces apoptosis in myeloma cells. The roles of Pgp and CYP3A, possible connection between drug resistance, regulation of the mevalonate pathway, and iosprenylation of signaling proteins in these observations remain to be resolved. The product induces apoptosis in numerous cancer cell lines perhaps, in part, by inhibiting the isoprenylation of Rho family GTPases. It causes cell cycle arrest in G1 and G2/M phases.
O3139 Oxamflatin ≥98% (HPLC), solid Histone deacetylase inhibitor; anti-cancer agent.
R7772 Roscovitine ≥98% (TLC) Roscovitine is a potent, selective inhibitor of cyclin-dependent kinases.
Roscovitine is a purine derived inhibitor. It stimulates apoptosis in cancer cells. It has inhibitory action on mitogen activated protein kinase (MAPK) and M-phase promoting factor (MPF) kinase activity. Roscovitine is known to arrest meiosis and thus, prevent embryonic development.
S1438   Sulindac sulfone ≥94% (HPLC), (solid or powder) Metabolite of sulindac that inhibits cell growth by inducing apoptosis independently of cyclooxygenase inhibition. Inhibits the development and induces regression of premalignant adenomatous polyps.
Sulindac sulfone is non-steroidal anti-inflammatory drug and an analgesic that has antiproliferative and apoptotic effects. It inhibits the expression and activity of cyclooxygenase-2 in human colon cancer cells1,2 and reduces tumor burden in adenomatous polyposis patients.3
S8139 Sulindac ≥98.0% Nonsteroidal anti-inflammatory; preferential inhibitor of COX-1.
Sulindac is non-steroidal anti-inflammatory drug and an analgesic that has antiproliferative and apoptotic effects. It inhibits the expression and activity of cyclooxygenase-2 in human colon cancer cells25,26 and reduces tumor burden in adenomatous polyposis patients.27
T8552 Trichostatin A ≥98% (HPLC), from Streptomyces sp. Inhibits histone deacetylase at nanomolar concentrations; resultant histone hyperacetylation leads to chromatin relaxation and modulation of gene expression. May be involved in cell cycle progression of several cell types, inducing cell growth arrest at both G and G/M phases; may induce apoptosis. Enhances the efficacy of anticancer agents that target DNA.
T9777 Trypsin-chymotrypsin inhibitor from Glycine max (soybean) lyophilized powder  
T2067 Tyrphostin AG 879 99% (HPLC) Inhibits the tyrosine kinase activity of the nerve growth factor receptor (TrkA; pp140trk) and heregulin receptor erbB-2 (HER-2).
Tyrphostin AG 879 is known to block RAF-1 and Her-2 expression and exhibit anticancer functions in breast cancer cells3. Furthermore, AG879 is known to block ETK1-PAK1 interactions and the growth of RAS-induced sarcomas in nude mice4.
P4543 Valproic acid sodium salt 98% Anti-convulsant that also has efficacy as a mood stabilizer in bipolar disorder.
Valproic acid is an anticonvulsant and mood-stabilizing drug. It is used to treat epilepsy and bipolar disorder. Valproic acid helps to repress the Warburg effect and the development of tumor in neuroblastoma.
X3628 XK469 ≥98% (HPLC), solid XK469 is a topoisomerase IIβ inhibitor; apoptosis inducer.