Cancer
Showing 49–71 of 71 results
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Ponatinib
Ponatinib, also known as AP24534, is considered to be a pan-BCR-ABL inhibitor. It was specifically designed to bind BCR-ABL with very high potency and to inhibit the entire spectrum of mutants conferring resistance against other tyrosine kinase inhibitors (TKIs), such as VEGFR2, FGFR1, PDGFRα, mutant FLT3 phosporylation and LYN among others, including the T315I mutant that is resistant to all current therapies. It has been shown to suppress BCR-ALB(T315I)-driven tumor growth in mice.
10mg
Cat. No.: 37-N29
$119.00
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PRE-084
PRE-084 is a high affinity sigma receptor agonist, selective for the σ1 subtype. It is a potent ligand of the σ receptor without much affinity for the PCP receptors.
10mg
Cat. No.: 06-R16
$82.00
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Rapamycin
Rapamycin is a macrocyclic triene antibiotic that binds to the cytosolic protein FK-binding protein 12 (FKBP12) and inhibits mTOR pathway by directly binding to the mTOR Complex1 (mTORC1). It is a potent immunosuppressant and has shown anticancer activity. Rapamycin It has a variety of uses both in vitro and in vivo and has been used to prevent organ rejection after transplantation.
Sale!5 mg
Cat. No.: 33-U72
Original price was: $129.00.$65.00Current price is: $65.00.
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Roscovitine
Roscovitine, also known as Seliciclib or CYC202, is a potent and reversible inhibitor of select cyclin-dependent kinases (CDKs), CDK1, CDK2, and CDK5. It has less sensitivity towards related kinases including ERK1,2. This molecule competes for the binding site of ATP in the catalytic cleft. Treatment of cultured cells with roscovitine can cause cell cycle arrest or apoptosis.
1mg
Cat. No.: 34-K14
$29.00
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SAHA (Vorinostat)
SAHA (Vorinostat) is a histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme and blocks substrate access. It inhibits class I and class II HDACs at around 50nM. SAHA has been shown to cause growth arrest and death of some transformed cells both in vitro and in vivo, with little or no toxic effects on normal cells.
100 mg
Cat. No.: 31-V28
$99.00
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Saracatinib (AZD0530)
Saracatinib is a highly selective, orally available Src/Abl kinase inhibitor. It is highly selective for Src and Abl kinases against a large range of tyrosine and serine-threonine kinases (VEGFR, FGFR, c-Kit etc,) Saracatinib exerts its activity through ATP competitive and reversible inhibition of the target enzyme. Saracatinib has been shown to inhibit tumor growth in a manner independent of dose and inhibits phosphorylation of focal adhesion kinase (FAK) and paxillin in a dose-dependent manner in a Calu-6 Xenograft model.
10 mg
Cat. No.: 12-B11
$99.00
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Selumetinib
Selumetinib, also known as AZD6244, is a potent inhibitor of MAPK/ERK kinase 1/2. It is not competitive with ATP and inactivates the ERK1/2 phosphorylation. This is important because these kinases lie downstream to BFAF and RAGS genes. The effect of mutation in these genes is controlled by inhibiting the kinases downstream.
5mg
Cat. No.: 07-V75
$89.00
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Sodium Butyrate
Sodium Butyrate is a short fatty acid chain that has an effect on the molecular, tissue and cellular levels. Sodium Butyrate has been shown to induce cell growth arrest, differentiation and apoptosis in cancer cells. It inhibits histone deacetylase (HDAC) and decreases Ca²⁺ release from intracellular stores. Sodium butyrate has been used to direct the differentiation of mouse embryonic stem cells into hepatocytes when used in combination with Activin A.
5 g
Cat. No.: 71-B16
$29.00
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Sorafenib
Sorafenib, also known as Nexavar, is a small molecule inhibitor of several tyrosine protein kinases, VEGFR 2 & 3 as well as PDGFR, and RAF/MEK/ERK cascade inhibitor. It also inhibits c-Kit, the ligand for Stem cell factor. It does not significantly inhibit MEK-1 or ERK-1 activity. It interacts in combination with the proteasome inhibitor bortezomib to induce apoptosis in a broad spectrum of neoplastic cell lines.
NOTE: The small molecule Sorafenib sold by Reagents Direct is NOT Nexavar®, and is NOT for human use.
5mg
Cat. No.: 13-D24
$99.00
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SU6656
SU6656 is a potent, cell-permeable, reversible, and ATP-competitive Src family kinase inhibitor. Src kinases are known to function in signal transduction pathways. It inhibits Src as well as other closely related kinases including Fyn, Yes, and Lyn. It can act as a weak inhibitor of Lck and PDGF receptor kinase.
5mg
Cat. No.: 42-K78
$99.00
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TG101348
TG101348 is an ATP competitive Janus -associated kinase 2 (JAK2) inhibitor. It has has also been shown to inhibit Flt3 and Ret. It is not known to suppress any other kinases. It blocks the JAK2-driven STAT5 phosphorylation, cell proliferation and cell survival in JAK2V617F-expressing cell lines.
5mg
Cat. No.: 48-F21
$150.00
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Tozasertib
Tozasertib is a potent inhibitor of all aurora kinases, including isotypes A, B and C. It has been shown to inhibit cell cycle progression, induce apoptosis and block tumor growth in varieties of in vivo xenograft models. Tozasertib has been shown to cause accumulation of cells with 4N DNA content and potently inhibit the proliferation of a wide variety of tumor cell types with IC50 values ranging from 15 to 113 nM. Tozasertib had no effect on the viability of noncycling primary human cells at concentrations as high as 10uM.
25 mg
Cat. No.: 11-W09
$59.00
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Trichostatin A (TSA)
Trichostatin A is a selective and potent inhibitor of histone deacetylase (HDAC). It selectively inhibits the removal of acetyl groups from the amino-terminal lysine residues of core histones, resulting in chromatin relaxation and modulation of gene expression. Trichostatin A has been shown to inhibit both the G1- and G2– phases of the mammalian cell cycle and has been used to induce apoptosis in cancer cells with low toxicity to non-cancer cells.
1 mg
Cat. No.: 62-K44
$79.00
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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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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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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 49–71 of 71 results