Perillyl alcohol, or POH, is a naturally occurring monocyclic terpenes derived from the mevalonate pathway in plants. Perillyl alcohol can be found in the essential oils of various botanicals, such as lavender, lemongrass, sage, and peppermint. It has a number of manufacturing, household, and medical applications. For example, perillyl alcohol may be used as an ingredient in cleaning products and cosmetics, and it has shown promise for inhalation therapy of patients with brain cancer.

GSK321 is a potent and selective IDH1 mutant inhibitor. GSK321 potently inhibited intracellular 2-HG production in HT-1080 cells, with a half-maximal effective concentration (EC50) of 85 nM by LC/MS/MS analysis. The inhibition of mutant IDH1 by GSK321 overcomes the pathognomonic differentiation block of AML cells and induces myeloid differentiation of IDH1 mutant cells at the level of leukemic blasts and more stem-like cells.

5'-deoxyadenosine, also known as 5'dAdo or 5'-dAdo, is a substrate of bacterial methylthioadenosine/S-adenosylhomocysteine (MTA/SAH) nucleosidase and a product inhibitor produced by radical SAM enzymes. 5′-dADO may be useful to study the specificity and distribution of radical S-adenosyl-L-methionine enzymes.

MTDIA, also known as MT-DADMe-ImmA, and Methylthio-DADMe-Immucillin A, is a MTAP inhibitor. Human 5'-methylthioadenosine phosphorylase (MTAP) is solely responsible for 5'-methylthioadenosine (MTA) metabolism to permit S-adenosylmethionine salvage. Transition-state (TS) analogues of MTAP are in development as anticancer candidates. TS analogues of MTAP incorporate a cationic nitrogen and a protonated 9-deazaadenine leaving group, which are mimics of the ribocation transition state. MT-ImmA and MT-DADMe-ImmA are two examples of these TS analogues.

Aloisine A is a potent and selective CDK/GSK-3 inhibitor. Aloisine A inhibits cell proliferation by arresting cells in both G1 and G2. IC50 data of Aloisine A: Cdc2 (CDK1)/cyclin B (IC50 = 150nM), Cdk2/cyclin A (IC50 = 120nM), Cdk2/cyclin E (IC50 = 400nM), Cdk5/p25 (IC50 = 200nM), Cdk5/p35 (IC50 = 160nM), and GSK-3α (IC50 = 500nM). Aloisine A also inhibits GSK-3β (IC50 = 650nM) and JNK (c-Jun N-terminal kinase) (IC50~3-10μM). Aloisine A blocks the cell cycle in both G1 and G2 phase.

GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1). GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns. GSK-LSD1 inhibits LSD1 with an IC50 of 16 nM and is > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). GSK-LSD1 induces gene expression changes in cancer cell lines (average EC50 < 5 nM) and inhibits cancer cell line growth (average EC50 < 5 nM). Lysine specific demethylase 1 (LSD1) is a histone demethylase found in various transcriptional co-repressor complexes. LSD1 is involved in ES cell differentiation, hematopoiesis, and has been described as having a role in Acute Myeloid Leukemia (AML). (http://www.thesgc.org/chemical-probes/GSK-LSD1)

Bromopyruvic acid is a hexokinase II inhibitor and an effective antitumor agent. The characteristics of 3-bromopyruvate in vitro and in vivo have been reported in the scientific literature since the 1940s. Because it is a highly reactive alkylating agent and it is inherently unstable, it had been described as a metabolic poison. Research at Johns Hopkins has suggested that 3-bromopyruvate could be used to selectively kill cancer cells, while leaving normal cells intact. Recently, the FDA accepted an IND application for the use of 3-bromopyruvate for a Phase I clinical trial in liver cancer. IMPORTANT NOTE: this product we are offering is a pure chemical solid powder, which is for research use only, not for human or therapeutic use. Buyer must be a professional and understands how to use and handle the chemical properly.

AlPcS4 , also known as aluminum phthalocyanine tetrasulfonate Chloroaluminum tetrasulfophthalocyanine; or AlS4Pc, AlPcS4(a), is a potent photosensitizer, and is potentially useful in cancer sonodynamic therapy and cancer photodynamic therapy. Aluminum phthalocyanine disulfonate is a mixture of regional isomers, in which sulfonate group can be in 3- or 4- position in phenyl ring. Aluminum phthalocyanine disulfonate is also a Coloring Agent; Dermatologic Agent; Fluorescent Dye; Indicators and Reagent; Luminescent Agent; Photosensitizing Agent; Radiation-Sensitizing Agent.

Aluminum phthalocyanine disulfonate sodium, also known as AlPcS2 disodium or AlS2Pc or AlPcS(2a), is a potent photosensitizer, and is potentially useful in cancer sonodynamic therapy and cancer photodynamic therapy. Aluminum phthalocyanine disulfonate is a mixture of regional isomers, in which sulfonate group can be in 3- or 4- position in phenyl ring. Aluminum phthalocyanine disulfonate is also a Coloring Agent; Dermatologic Agent; Fluorescent Dye; Indicators and Reagent; Luminescent Agent; Photosensitizing Agent; Radiation-Sensitizing Agent.

MC-70 is a potent P-gp inhibitor (EC50 = 0.69 μM). Multidrug resistance (MDR) is the major cause of the failure of cancer therapy since this phenomenon generates cancer cells that are unresponsive to chemotherapeutic agents. P-glycoprotein (P-gp) is a well-known membrane transporter expressed in a number of strategic biological barriers, where it exerts a protective effect of paramount importance.

Temozolomide Acid, also known as TMZA, is a metabolite of temozolomide (TMZ) with demonstrable anticancer activity in vitro. Temozolomide, (TMZ) (brand names Temodar and Temodal and Temcad) is an oral chemotherapy drug. It is an alkylating agent used as a treatment of some brain cancers; as a second-line treatment for astrocytoma and a first-line treatment for glioblastoma multiforme.

Nigericin is an antibiotic derived from Streptomyces hygroscopicus. Its isolation was described in the 1950s, and in 1968 the structure could be elucidated by X-ray crystallography. The structure and properties of nigericin are similar to the antibiotic monensin. Commercially it is obtained as a byproduct, or contaminant, at the fermentation of Geldanamycin. It is also called Polyetherin A, Azalomycin M, Helixin C, Antibiotic K178, Antibiotic X-464. Nigericin acts as an H+, K+, Pb2+ ionophore. Most commonly it is an antiporter of H+ and K+. In the past nigericin was used as an antibiotic active against gram positive bacteria. It inhibits the Golgi functions in Eukaryotic cells. Nigericin exhibits anticancer and anti-HIV activity.

MC1742 is a novel and selective HDAC inhibitor with potential anticancer activity. Musculoskeletal sarcomas are aggressive malignancies of bone and soft tissues often affecting children and adolescents. Histone deacetylase inhibitors (HDACi) have been proposed to counteract cancer stem cells (CSCs) in solid neoplasms. When tested in human osteosarcoma, rhabdomyosarcoma, and Ewing's sarcoma stem cells, the new HDACi MC1742 increased acetyl-H3 and acetyl-tubulin levels and inhibited CSC growth by apoptosis induction. At nontoxic doses, 1 promoted osteogenic differentiation. (copied from J Med Chem. 2015 Apr 30. [Epub ahead of print].

Doxorubicin-SMCC, also known as ADR-SMCC, dox-SMCC, is a derivative of doxorubicin with a SMCC linker (Succinimidyl-4-( N -maleimidomethyl)cyclohexane-1-carboxylate). Maleimide in doxrubicin-SMCC can react with sulfhydryl groups at pH 6.5-7.5 to form a stable thioether bond. Doxorubicin-SMCC can be used to synthesize doxorubicin bioconjugates with proteins, enzymes; antobodies, antigens, and other biopolymers. Doxorubicin-SMCC is often used for drug delivery research.

Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets gene bodies containing clusters of sequences with a propensity for G-quadruplex formation. As a result, pyridostatin modulated the expression of these genes, including the proto-oncogene SRC.

9-hydroxyellipticine, also known as IGIG 929 and LS133324, is a potent cytotoxic and antitumor agent. Structurally, 9-hydroxyellipticine is a 9-hydroxy derivative of ellipticine. The hydroxy group in 9-hydroxyellipticines increases the apparent affinity for DNA, stabilisation of toposiomerase II-DNA cleavable complex, oxidation to reactive quinone-imine intermediates, phosphorylation of p53 suppressor proteins and cytotoxicity relative to the parent ellipticines.

Gemcitabine monophosphate disodium salt, also called GemMP, is a monophosphate derivative of Gemcitabine. Gemcitabine (Gem) is a deoxycytidine analog that is effective against pancreatic cancer and other malignancies following conversion to the 5'-O-mono-, di- and tri-phosphate forms. GemMP decreased tumor cell growth at concentrations ranging from 1 to 50 nM. GemMP is a potent cytotoxic agent that serves to induce apoptosis in association with increased Fas expression in cultured thyroid cancer cell lines. (Anticancer Res. 2000 Sep-Oct;20(5A):2915-22).

ATN-163 is a five amino acid peptide. ATN-163 is a scramble peptide of ATN-161. ATN-161 (Ac-PHSCN-NH2), a five-amino acid peptide with documented anti-angiogenic activity.

Thiocolchicine is a potent tubulin polymerization and microtubule assembly inhibitor, a axonal cytoskeleton modulator and apoptosis inducer. Structurally, thiocolchicine is a colchicine analog in which the C-10 methoxy is replaced with a thiomethyl moiety. Thiocolchicine was shown to bind with high affinity to the colchicine site on tubulin (Ka = 1.07 +/- 0.14 x 10(6) M-1). Thiocolchicine-dimers were shown to be potent topoisomerase I inhibitors.

Purpurogallin is a red, crystalline compound, and the aglycon of several glycosides from nutgalls and oak barks. It can inhibit hydroxyestradiol methylation by catechol-O-methyltransferase. It potently and specifically inhibits PLK, TLR1/TLR2 activation pathway. Purpurogallin showed antiplatelet and antithrombotic activities; anti?inflammatory effects; antitumor activity, anti-oxidation activities; hepatoprotecting effects; antibacterial activity toward gram-positive bacteria.

Methylthioadenosine, also known as MTA and 5'- Methylthioadenosine, is a naturally occurring sulfur-containing nucleoside present in all mammalian tissues. In vitro experiments showed that MTA treatment inhibited melanoma cell proliferation and viability in a dose dependent manner, where BRAF mutant melanoma cell lines appear to be more sensitive. Importantly, MTA was effective inhibiting in vivo tumor growth. The molecular analysis of tumor samples and in vitro experiments indicated that MTA induces cytostatic rather than pro-apoptotic effects inhibiting the phosphorylation of Akt and S6 ribosomal protein and inducing the down-regulation of cyclin D1. ( BMC Cancer . 2010 Jun 8;10:265.)

NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h.

NU6140 is a cyclin-dependent kinase 2 (cdk2) inhibitor; induces cell-cycle arrest at the G2-M phase.

PD0407824, also known as PD407824 is a potent selective, small molecular CHK1 inhibitor with potential anticancer activity.

CAY10505 is a phosphatidylinositol 3-kinase-γ inhibitor , was found to significantly improve acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats. CAY10505 , may improve hypertension-associated vascular endothelial dysfunction. Inhibition of PI3Kγ might be a useful approach in the therapeutics of vascular endothelium dysfunction.

KU59403 is a potent and selective ATM (Ataxia telangiectasia mutated) inhibitor with with potential anticancer activity. KU59403 was not cytotoxic to human cancer cell lines (SW620, LoVo, HCT116, and MDA-MB-231) per se but significantly increased the cytotoxicity of topoisomerase I and II poisons: camptothecin, etoposide, and doxorubicin. KU59403 significantly enhanced the antitumor activity of topoisomerase poisons in mice bearing human colon cancer xenografts (SW620 and HCT116) at doses that were nontoxic alone and well-tolerated in combination

PD180970 is a novel Bcr-Abl inhbiitor. PD180970 inhibited in vivo tyrosine phosphorylation of p210Bcr-Abl (IC50 = 170 nM) and the p210BcrAbl substrates Gab2 and CrkL (IC50 = 80 nM) in human K562 chronic myelogenous leukemic cells. In vitro, PD180970 potently inhibited autophosphorylation of p210Bcr-Abl (IC50 = 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death. PD180970 is among the most potent inhibitors of the p210Bcr-Abl tyrosine kinase, which is present in almost all cases of human chronic myelogenous leukemia. PD180970 is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia.

PD166326 is one of the most potent members of the pyridopyrimidine class of protein tyrosine kinase inhibitors. In mice with the CML-like disease, PD166326 rapidly inhibited Bcr/Abl kinase activity after a single oral dose and demonstrated marked antileukemic activity in vivo. In vivo, PD166326 was also superior to imatinib mesylate in inhibiting the constitutive tyrosine phosphorylation of numerous leukemia-cell proteins, including the src family member Lyn. PD166326 also prolonged the survival of mice with imatinib mesylate-resistant CML induced by the Bcr/Abl mutants P210/H396P and P210/M351T.

YC-137 is a BCL-2 inhibitor, which selectively induces apoptosis of Bcl-2-overexpressing cells and disrupts its interaction with Bid BH3, thereby blocking the anti-apoptotic activity of Bcl-2.

OM137 is an inhibitor of Aurora kinases. which is growth inhibitory to cultured cells when applied at high concentration and potentiates the growth inhibitory effects of subnanomolar concentrations of paclitaxel.