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Enzyme Inhibitors

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Image	Description	Biochem/physiol Actions	CAS Number	Product #
	(−)-Deguelin >98% (HPLC), solid	Inhibitor of activated Akt. Does not affect MAPK, ERK1/2, or JNK. Anticancer, chemoprotective agent.	522-17-8	D0817
	(−)-Depudecin >95% (HPLC), from microbial	Inhibitor of histone deacetylase (HDAC) both in vivo and in vitro. Alters the spindle shaped morphology of v-Ha-ras-transformed NIH3T3 cells to a flattened shape and induces an intricate actin stress fiber network in these cells and in MG63 osteosarcoma cells. Also exhibits anti-angiogenic activity.	139508-73-9	D5816
	(S)-(+)-Camptothecin ~95% (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.	7689-03-4	C9911
	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.	35404-50-3	377627
	2-Propylpentanoic acid	Anticonvulsant that also has efficacy as a mood stabilizer in bipolar disorder	99-66-1	P6273
	DL-Aminoglutethimide	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).	125-84-8	A9657
	Apicidin ≥95%, from microbial, solid	Potent (nM) cell permeable inhibitor of histone deacetylase. Also, exhibits antiprotozoal and potential antimalarial properties. Apicidin has antiproliferative activity on HeLa cells accompanied by cell arrest at the G1 phase. In addition, it induces selective changes in the expression of p21 and gelsolin.	183506-66-3	A8851
	Butein solid	Inhibits EGFR and Src tyrosine kinase activities; inhibits cAMP-dependent PDE-IV. Induces apoptosis in B16 melanoma cells and HL-60 human leukemia cells.	487-52-5	B178
	Etoposide synthetic, ≥98%, powder	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.	33419-42-0	E1383
	Formestane solid	Aromatase inhibitor used as an anti-cancer agent against estrogen-dependent tumors.	566-48-3	F2552
	Fostriecin sodium salt from Streptomyces pulveraceus ≥98% (HPLC)	Fostriecin was discovered as an anti-tumor antibiotic isolated from the fermentation beer of Streptomyces pulveraceus (subspecies fostreus). Fostriecin has antitumor activity against a wide spectrum of tumor cells in vitro and excellent activity against P388 and L1210 leukemias in vivo. The antitumor activity of fostriecin originates from its ability to interfere with the reversible phosphorylation of proteins that are critical for progression through the cell cycle.	87860-39-7	F4425
	Hispidin solid, ≥98% (HPLC)	Potent inhibitor of protein kinase C_β, cytotoxic for cancer cells.	555-55-5	H5257
	Indomethacin ≥99% (TLC)	Cyclooxygenase (COX) inhibitor that is relatively selective for COX-1.	53-86-1	I7378
	Mevinolin from Aspergillus sp. ≥98% (HPLC)	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.	75330-75-5	M2147
	Oxamflatin ≥98% (HPLC), solid	Histone deacetylase inhibitor; anti-cancer agent.	151720-43-3	O3139
	Roscovitine ≥98% (TLC)	Potent, selective inhibitor of cyclin-dependent kinases.	186692-46-6	R7772
	Sulindac sulfone 99% (TLC), solid	Metabolite of sulindac that inhibits cell growth by inducing apoptosis independently of cyclooxygenase inhibition. Inhibits the development and induces regression of premalignant adenomatous polyps.	59864-04-9	S1438
	Sulindac ≥98.0%	Nonsteroidal anti-inflammatory; preferential inhibitor of COX-1.	38194-50-2	S8139
	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.	58880-19-6	T8552
	Trypsin-chymotrypsin inhibitor from Glycine max (soybean) lyophilized powder		37330-34-0	T9777
	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).	148741-30-4	T2067
	Urinary Trypsin Inhibitor Fragment ≥95% (HPLC)	Blocks the metastasis of human ovarian cell line (HRA) without affecting their proliferation.	164859-77-2	U4751
	Valproic acid sodium salt ≥98%	Anti-convulsant that also has efficacy as a mood stabilizer in bipolar disorder.	1069-66-5	P4543
	XK469 ≥98% (HPLC), solid	Topoisomerase IIβ inhibitor; apoptosis inducer.		X3628

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