Cancer Research

Mechanisms of Action

Angiogenesis Inhibitors
Name Biological activity Product No.
Angiostatin K1-3 A proteolytic fragment of plasminogen that is a specific inhibitor of endothelial cell growth and angiogenesis. A1477
DL-α-Difluoromethyl-ornithine Irreversible inhibitor of ornithine decarboxylase (ODC); chemoprotective agent that blocks angiogenesis. D193
Endostatin Potent inhibitor of angiogenesis and tumor growth; inhibits endothelial cell proliferation. E8154
Fumagillin Inhibitor of endothelial cell proliferation and angiogenesis. F6771
Genistein Antiangiogenic agent, down-regulates the transcription of genes involved in controlling angiogenesis. G6649
Minocycline Inhibits endothelial cell proliferation and angiogenesis. M9511
Staurosporine Blocks angiogenesis by inhibiting the upregulation of VEGF expression in tumor cells. S4400
(±)-Thalidomide Selectively inhibits biosynthesis of tumor necrosis factor α (TNF-α); inhibits angiogenesis. T144

DNA Intercalators / Cross-linkers
Name Biological activity Product No.
Bleomycin Inhibits DNA synthesis and causes cleavage at specific base sequences. Induces apoptosis in a variety of cells; inhibits tumor angiogenesis. B5507
Carboplatin Forms cytotoxic adducts with DNA; induces apoptosis. C2538
Carmustine DNA alkylating/crosslinking agent effective against glioma and other solid tumors. C0400
Chlorambucil Alkylates DNA; induces apoptosis of leukemia cells by a p53-dependent mechanism. C0253
Cyclophosphamide Cytotoxic nitrogen mustard that crosslinks DNA and causes strand breakage. C0768
cis-Diammineplatinum(II) dichloride (Cisplatin) Forms cytotoxic adducts with the DNA dinucleotide d(pGpG); induces apoptosis. P4394
Melphalan Forms DNA intrastrand crosslinks by alkylation of 5'-(GGC) sequences. M2011
Mitoxantrone DNA intercalating agent that inhibits DNA synthesis M6545
Oxaliplatin Cytotoxicity follows the formation of adducts with DNA. O9512

DNA Synthesis Inhibitors
Name Biological activity Product No.
(±)-Amethopterin (Methotrexate) Folic acid antagonist; blocks thymidine biosynthesis by inhibiting dihydrofolate reductase. A7019
3-Amino-1,2,4-benzotriazine 1,4-dioxide Hypoxia-activated antineoplastic agent. A9938
Aminopterin Folic acid antagonist; blocks thymidine biosynthesis by inhibiting dihydrofolate reductase. More potent, but more toxic, than methotrexate. A1784
Cytosine β-D-arabinofuranoside Selective inhibitor of DNA synthesis. C1768
5-Fluoro-5'-deoxyuridine Inhibits proliferation of tumors, cell lines or fibroblasts transformed by H-Ras or Trk oncogenes. F8791
5-Fluorouracil Inhibits thymidylate synthetase and depletes dTTP; it forms nucleotides that can be incorporated into RNA and DNA and induces p53-dependent apoptosis. F6627
Ganciclovir In suicide gene therapy of solid tumors, the gene for Herpes simplex virus thymidine kinase is delivered to tumor cells and expressed, which in turn activates ganciclovir cytotoxicity. G2536
Hydroxyurea Inactivates ribonucleoside reductase and blocks the synthesis of deoxynucleotides, thus inhibiting DNA synthesis and inducing cell death. H8627
Mitomycin C Inhibits DNA synthesis, nuclear division, and proliferation of cancer cells. M0503

DNA-RNA Transcription Regulators
Name Biological activity Product No.
Actinomycin D Inhibits cell proliferation by complexing to DNA and blocking the production of mRNA by RNA polymerase; induces apoptosis. A1410
Daunorubicin Complexes to DNA and blocks production of mRNA by RNA polymerase. D8809
Doxorubicin Binds to DNA and inhibits reverse transcriptase and RNA polymerase. D1515
Homoharringtonine Binds to the 80S ribosome in eukaryotic cells and inhibits protein synthesis by interfering with chain elongation. H0635
Idarubicin Anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin. I1656

Enzyme Inhibitors
Name Biological activity Product No.
S(+)-Camptothecin Binds irreversibly to the DNA-topoisomerase I complex leading to the irreversible cleavage of DNA and the destruction of cellular topoisomerase I by the ubiquitin-proteasome pathway. Induces apoptosis in many normal and tumor cell lines. C9911
Curcumin Potent inhibitor of protein kinase C, EGFR tyrosine kinase and IκB kinase. Induces apoptosis in cancer cells. C7727
(-)-Deguelin Inhibitor of activated Akt. Does not affect MAPK, ERK1/2 or JNK. D0817
5,6-Dichlorobenz-imidazole 1-β-D-ribofuranoside Inhibitor of RNA synthesis, causes premature termination of transcription. D1916
Etoposide Binds to the DNA-topoisomerase II complex to enhance cleavage and inhibit religation; inhibits synthesis of the oncoprotein Mdm2 and induces apoptosis in tumor lines that overexpress Mdm2. E1383
Formestane Aromatase inhibitor F2552
Fostriecin Interferes with the reversible phosphorylation of proteins that are critical for progression through the cell cycle. F4425
Hispidin Potent inhibitor of protein kinase Cβ. H5257
2-Imino-1-imidazoli-dineacetic acid (Cyclocreatine) Creatine analog; decreases the rate of ATP production via creatine kinase and reduces the proliferation of tumor cell lines characterized by high levels of creatine kinase expression. 37,762-7
Mevinolin Inhibits mevalonic acid production and induces apoptosis in numerous cancer cell lines, perhaps, in part, by inhibiting the isoprenylation of Rho-family GTPases. M2147
Trichostatin A Histone deacetylase inhibitor that enhances the cytotoxic efficacy of anticancer drugs that target DNA. T8552
Tyrphostin AG 34 Tyrosine protein kinase inhibitor in human colon cancer cell lines. T6318
Tyrphostin AG 879 Inhibits the tyrosine kinase activity of the nerve growth factor receptor (TrkA; pp140trk) and heregulin receptor erbB-2. T2067

Gene Regulation
Name Biological activity Product No.
5-Aza-2'-deoxycytidine Causes DNA demethylation or hemi-demethylation, creating openings that allow transcription factors to bind to DNA and reactivate tumor suppressor genes. A3656
5-Azacytidine A2385
Cholecalciferol (Vitamin D3) Antiproliferative action on breast, prostate, and colon cancer cells C9756
4-Hydroxytamoxifen Metabolite of tamoxifen that is a potent selective estrogen response modifier (SERM); the trans (Z) isomer has efficacy against estrogen-sensitive cancers. The cis (E) isomer is an estrogen agonist. H6278
Melatonin Enhances apoptotic death of cancer cells; inhibits proliferation/metastasis of breast cancer cells by inhibiting estrogen receptor action. M5250
Mifepristone Progesterone receptor antagonist; stimulates prolactin secretion. Pgp inhibitor. M8046
Raloxifene Selective estrogen response modifier (SERM), may have efficacy against estrogen-sensitive cancers. R1402
all trans-Retinal (Vitamin A aldehyde) Ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR) that act as transcription factors to regulate the growth and differentiation of normal and malignant cells. R2500
Retinoic acid, all trans (Vitamin A acid) R2625
9-cis-Retinoic Acid R4643
13-cis-Retinoic acid R3255
Retinol (Vitamin A) R7632
Tamoxifen Selective estrogen response modifier (SERM), used therapeutically and prophylactically against estrogen-sensitive tumors. T5648
Troglitazone Anti-tumor agent; PPAR-γ agonist; induces apoptosis via a p53 pathway. T2573

Microtubule Inhibitors
Name Biological activity Product No.
Colchicine Antimitotic agent that disrupts microtubules by binding to tubulin and preventing its polymerization; induces apoptosis in several normal and tumor cell lines. C9754
Dolastatin 15 Reported to interact with tubulin and induce apoptosis. D5566
Nocodazole Antimitotic agent that binds to β-tubulin and disrupts mitotic spindle function; induces apoptosis in several normal and tumor cell lines. M1404
Paclitaxel Binds to β-tubulin and promotes the formation of highly stable microtubules that resist depolymerization, preventing cell division. T7191
Podophyllotoxin Inhibits microtubule assembly. P4405
Rhizoxin Binds to β-tubulin in most eucaryotic cells including animals, plants and fungi. It completely prevents formation of an intrachain cross-link in β-tubulin by N,N'-ethylenebis(iodoacetamide). R8149
Vinblastine Antimitotic agent. Inhibits microtubule assembly by binding tubulin and inducing self-association; depolymerizes pre-existing microtubules. Induces apoptosis in several tumor cell lines. V1377
Vincristine V8879
Vindesine V8254
Vinorelbine (Navelbine) Potent anti-mitotic, anti-tumor agent. Low neurotoxicity is related to its higher affinity for mitotic microtubules than for axonal microtubules. V2264

Other Antitumor Agents
Name Biological activity Product No.
17-(Allylamino)-17-demethoxygeldanamycin Inhibits the activity of oncogenic proteins such as N-ras, Ki-ras, c-Akt, and p185erB2. Induces apoptosis. A8476
4-Amino-1,8-naphthalimide Sensitizes cells to radiation-induced cell damage and enhances the cytotoxicity of 1-methyl-3-nitro-1-nitrosoguanidine. A0966
Apigenin Inhibits cell proliferation by arresting the cell cycle at the G2/M phase. Inhibition of growth through cell cycle arrest and induction of apoptosis appear to be related to induction of p53. Inhibitory effects on tumor promotion may also be due to inhibition of kinase activity and the resulting suppression of oncogene expression. It has also been reported to inhibit topoisomerase I catalyzed DNA religation and enhance gap junctional intercellular communication. A3145
Brefeldin A Disrupts the structure and function of the Golgi apparatus. An activator of the sphingomyelin cycle. B7651
Cimetidine H2 histamine receptor antagonist; I1 imidazoline receptor agonist; anti-ulcer agent. Blocks cancer metastasis by inhibiting the expression of E-selectin on the surface of endothelial cells, thus blocking tumor cell adhesion. C4522
Dichloromethylene-diphosphonic acid Analog of pyrophosphate ion that inhibits the osteoclastic activity leading to bone resorption and osteoporosis. Found also to inhibit collagenase and matrix metalloproteinase 1. D4434
Leuprolide (Leuprorelin) Luteinizing hormone releasing hormone (LH-RH) agonist. L0399
Luteinizing Hormone-Releasing Hormone Hypothalamic peptide that stimulates release of gonadotrophins from anterior pituitary, thus regulating reproductive functions. L7134
Pifithrin-α Reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1 and mdm2 expression. Enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin, etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. P4359
Rapamycin Inhibition of the molecular target of rapamycin (mTOR) mediates the antiproliferative and anticancer activity of rapamycin by blocking the PI3K/Akt pathway. R0395
Sex hormone-binding globulin Regulates the availability of sex steroid hormones and limits their access to target cells. Inhibits estradiol-induced proliferation of breast cancer cells. S1437
Thapsigargin Cytotoxin that induces apoptosis by disrupting intracellular free Ca2+ levels. T9033
Urinary trypsin inhibitor fragment (Bikunin) Blocks the metastasis of human ovarian cell line (HRA) without affecting their proliferation. U4751

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