Small Molecules
Showing 97–108 of 108 results
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Triciribine
Triciribine is a synthetic cell-permeable and reversible tricyclic nucleoside that selectively inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3 but does not inhibit Akt kinase activity or upstream Akt activators, PI3-Kinase or PDK1. It has shown to inhitib cell growth and induce apoptosis in cancer cells with aberrant Akt activity both in vitro and in vivo.
1 mg
Cat. No.: 32-M26
$109.00
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Troglitazone
Troglitazone is a potent antiproliferative and apoptosis inducer and is a selective PPARγ agonist. There was no activation of PPARα and PPARδ observed at concentrations up to 10 µM. Troglitazone binds to the PPARγ ligand-binding domain (LBD) but fails to induce interaction of the PPARγ LBD with the transcriptional coactivators SRC-1, TIF2, AIB1, p300, or TRAP220. PPARγ is mainly expressed in adipose tissue, one of the target tissues for insulin, but has subsequently been found to be expressed in vascular smooth muscle cells, endothelial cells, macrophages, and some cancer cells. Troglitazone also induces cell cycle arrest and apoptosis in several cancer cell lines with an EC50 of 10 µM
5mg
Cat. No.: 05-E10
$59.00
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Tyrphostin AG 490
Tyrphostin AG 490 is a specific and potent JAK-2 protein tyrosine kinase inhibitor. It has been shown to inhibit EGF receptor autophosphorylation, DNA synthesis and cell growth. It induces apoptosis with no deleterious effect on normal hematopoiesis. Tyrphostin AG 490 has been shown to inhibit the growth of leukemic cells in vitro and in vivo. This compound is a valuable tool for studying the cellular role of JAK kinases in signal transduction.
10 mg
Cat. No.: 22-B79
$59.00
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U0126
U0126 is a highly selective inhibitor of both MEK1 (IC50 of 72nM) and MEK2 (IC50 of 58 nM). U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-related kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways. The effects of U0126 on the growth of eight human breast cancer cell lines have shown that U0126 selectively represses anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. Upon treatment with U0126, cells deprived of anchorage entered apoptosis.
5 mg
Cat. No.: 84-P22
$99.00
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Valproic Acid
Valproic Acid is a small molecule histone deacetylase (HDAC) inhibitor that that exhibits anticancer, anti-inflammatory and neuroprotective effects . It has been shown to inhibit multiple pathways including the ERK, PKC and Wnt/β-Catenin pathways. Valproic Acid has been shown to regulate the differentiation and proliferation of various cell types, including mesenchymal and hematopoietic stem cells, primary neurons, neuroblastomas and neural progenitor cells. Valproic acid, when used in combination with cytokines differentiate cells into a uniform and homogeneous cell population of hepatic progenitor cells, followed by maturation into functional hepatocytes.
5 g
Cat. No.: 25-B43
$49.00
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Vandetanib
Vandetanib is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor. It has been shown to inhibit VEGFR-dependent tumor angiogenesis and EGFR– and RET-dependent tumor cell proliferation and survival. Vandetanib has also been shown to inhibt fms-like tyrosine kinase 4 (VEGFR3, IC50 = 110 nM) and epidermal growth factor receptor (EGFR/HER1, IC50 = 500 nM) but shows selectivity relating to a range of other tyrosine and serine-threonine kinases.
50 mg
Cat. No.: 29-E58
$99.00
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Wortmannin
Wortmannin is a potent and specific phosphatidylinositol 3-kinase (P13K) inhibitor. Inhibitor of the P13K/Akt signal transduction cascade enhances the apoptotic effects of radiation or serum withdrawal and blocks the antiapoptotic effect of cytokines. Wortmannin has been shown to block many of the short-term metabolic effects induced by insulin receptor activation by the inhibition of P13K.
1 mg
Cat. No.: 49-U91
$49.00
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WP1066
WP1066 is a Janus kinase (Jak) 2 inhibitor. It works by degrading the Jak2 protein, thus blocking its downstream signal transducer and activator of transcription (STAT) and phosphoinositide-3-kinase pathways to result in the activation of the caspase pathway. The Jak/STAT pathway is one of a handful of pleiotropic cascades used to transduce a multitude of signals for development and homeostasis in animals. In mammals, it is the principal signaling mechanism for a wide array of cytokines and growth factors. WP1066 also acts as an immune adjuvant by inducing proliferation of effector T cells and upregulating CD86 and CD80.
10mg
Cat. No.: 76-J32
$115.00
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XAV939
XAV939 is a cell permeable, small molecule inhibitor of the Wnt/β– catenin pathway. It inhibits tankyrase 1 (IC₅₀= 11nM)and tankyrase 2 (IC₅₀=4nM), stabilizes axin and stimulates β-catenin degradation. Small molecule XAV939 has also been shown to inhibit proliferation of the µ-catenin-dependent colon carcinoma cell line DLD-1.
5 mg
Cat. No.: 52-A47
$99.00
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Y27632
Y27632 (dihydrochloride) is a highly potent ATP-competitive inhibitor of Rho– associated coiled-coil forming protein serine/threonine kinase (ROCK). It has been shown to prevent dissociation-induced apoptosis in human embryonic stem cells (hES cells). Y27632 enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency.
Sale!2 mg
Cat. No.: 53-B85
Original price was: $109.00.$89.00Current price is: $89.00.
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ZM447439
ZM447439 is a selective ATP-competitive inhibitor of Aurora B kinase. The Aurora kinases have important roles in regulating mitosis and cytokinesis, with Aurora B involved in centromere function as part of the Chromosomal Passenger Complex, with survivin, INCENP, and borealin. ZM447439 selectively inhibits proliferating cells rather than non-dividing cells, suggesting its potential in cancer therapy.
5mg
Cat. No.: 94-U12
$99.00
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ZSTK474
ZSTK474 is a cell permeable and reversible P13K inhibitor with an IC₅₀ at 6nm. It was identified as part of a screening library, selected for its ability to block tumor cell growth. ZSTK474 has shown strong antitumor activities against human cancer xenographs when administered orally to mice without a significant toxic effect.
50 mg
Cat. No.: 86-M73
$99.00
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Showing 97–108 of 108 results