Cancer
Showing 1–24 of 71 results
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17-AAG
17-AAG is a synthetic derivative of geldanamycin and acts as an anti-tumor agent. 17-AAG binds specifically to heat shock protein Hsp90. Hsp90 is a protein chaperone that binds to client proteins. Client proteins include important cancer– relevant targets such as mutated p53, Her2, Bcr-Abl, Raf-1, Akt and others. 17-AAG disrupts the Hsp-900 client protein complexes and leads to the degredation of the client proteins.
1 mg
Cat. No.: 10-G06
$99.00
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Abiraterone
Abiraterone is a potent steroidal inhibitor of cytochrome P450 CYP17 with an IC50 at 4 nM. Abiraterone has been shown to selectively inhibit the target enzyme, resulting in inhibition of testosterone production in both the adrenals and the testes.
2 mg
Cat. No.: 35-D62
$109.00
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AT13387
AT13387 is a synthetic, small-molecule inhibitor of heat shock protein 90 (Hsp90). It selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. Hsp90, a chaperone protein upregulated in a variety of tumor cells, regulates the folding, stability and degradation of many oncogenic signaling proteins.
5mg
Cat. No.: 81-D36
$280.00
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AT9283
AT9283 is a multi-targeted kinase inhibitor of both Aurora kinases (A & B) as well as Janus kinase (Jak) 2. It also targets serine/threonine protein kinases associated with myeloid cell proliferation. AT9283 inhibited growth and survival of multiple solid tumor cell lines.
2mg
Cat. No.: 64-Q25
$100.00
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AZD1480
AZD1480 is a potent JAK2 inhibitor that can suppress growth, survival, as well as FGFR3 and STAT3 signaling and downstream targets. AZD1480 is a potent, competitive small-molecule inhibitor of JAK1/2 kinase, and is capable of inhibiting STAT3 phosphorylation and tumor growth in a STAT3-dependent manner. This may lead to induction of tumor cell apoptosis and a decrease in cellular proliferation. JAK2, often upregulated or mutated in a variety of cancer cells, mediates STAT3 activation and plays a key role in tumor cell proliferation and survival.
5mg
Cat. No.: 09-B31
$100.00
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Bafilomycin A1
Bafilomycin A1 is a macrolide antibiotic that selectively inhibits vacuolar-type (v-type) H+ ATPase. The compound can inhibit E1E2 ATPases from sarcoplasmic reticulum, E. coli, and ox brain versus F1F0 ATPases found in bacteria and mitochondria. It blocks pH regulation in brain cells. Additionally, Bafilomycin A1 prevents lysosomal cholesterol trafficking in macrophages and can be used to distinguish different types of ATPases.
1 MG
Cat. No.: 24-R68
$135.00
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BAY 11-7082
Bay 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation. The transcription factor NF-κB plays a key role in regulating over 150 target genes that include the expression of inflammatory cytokines, chemokines, immunoreceptors, and cell adhesion molecules. Bay 11-7082 selective and irreversibly inhibits NF-κB activation by blocking TNF-α-induced phosphorylation of IκB-α without affecting IκB-α phosphorylation. BAY 11-7082 has also demonstrated stimulation of the stress-activated protein kinases, p38 and JNK-1.
10 mg
Cat. No.: 82-X11
$75.00
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BEZ235 (NPV-BEZ235)
NPV-BEZ235 is a dual inhibitor of phosphatidylinositol 3-kinase (P13K)and the downstream mammalian target of rapamycin (mTOR) by binding to the ATP-binding cleft of these enzymes. It specifically blocks the dysfunctional activation of the P13K pathway and induce G(1) arrest. NPV-BEZ235 has been shown to inhibit VEGF induced cell proliferation and survival in vitro and VEGF induced angiogenesis in vivo. It has also been shown to inhibit the growth of human cancer in animal models.
5 mg
Cat. No.: 59-P86
$99.00
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BI2536
BI2536 is a small molecule inhibitor of Polo Like Kinase 1 (PLK1). PLK1 is a serine/threonine protein kinase and is a key regulator of multiple processes essential to mitosis and cell division. Inhibition of PLK1 by BI2536 results in mitotic arrest, disruption of cytokinesis and apoptosis in tumor cell populations. BI2536 has been shown to inhibit growth of xenographs in nude mice and induces regression of large tumors with well tolerated intravenous dose regimens.
5 mg
Cat. No.: 88-Q71
$150.00
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BIBW-2992
BIBW-2992 is a irreversible and dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) kinases. The potency of BIBW-2992 on the EGFR and HER2 kinases revealed IC₅₀ values of 0.5 nM and 14 nM, respectively. BIBW-2992 is highly selective for these kinases and no additional inhibition of other kinases has been observed. BIBW-2992 has also been shown to suppress EGF-induced EGFR phosphorylation and cellular proliferation in various cell lines.
5 mg
Cat. No.: 72-C33
$89.00
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Brefeldin A
Brefeldin A (BFA) (IC50 value of 0.2 μM) is an inhibitor of ATPase.
ATPase is a chemical enzyme. It is essential in the ADP/ATP exchange providing chemical potential energy. ATP supplies the energy for such physiological activities such as importing metabolites necessary for cell metabolism, exporting toxins, wastes, and solutes that can hinder cellular processes, cell proliferation, ER stress and so forth.
When tested with cell line HEK293 cells (stably express wild-type (wt) CRELD2), BFA treatment nearly abolished the secretion of wtCRELD2 completely via inhibiting the transportation of proteins from the ER to the Golgi apparatus [4]. In MCF-7 cells and Hela cells, treatment with BFA induced p53 expression via inhibiting ATP which enhanced ER stress [5]. When treated with colorectal cancer cell line HCT116 cells, BFA treatment induced cells apoprosis by inhibiting ATP which functioned in the process of cellular vesicle trafficking
Treatment with BFA could attenuate stimulus-dependent hyperalgesia phenomenon via inhibiting vesicular exocytosis which process is important for ATP release.
BFA also is reported as an inhibitor for GTP/GDP exchange in a dose-dependent way, which is important in vesicular trafficking.
Cat. No.: 23-S79
$54.00
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CH5424802
CH5424802, also known as AF802, is a potent and selective Anaplastic lymphoma kinase (ALK) inhibitor. ALK is a tyrosine kinase that is constitutively activated in certain cancers, following gene alterations such as chromosomal translocation, amplification, or point mutation. It has shown limited inhibition of other kinases, GAK and LTK. LTK is known to show greatest sequence similarity to ALK.
5 mg
Cat. No.: 73-P27
$180.00
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CI-994
CI-994 is a histone deacetylase (HDAC) inhibitor that induces hyperacetylation in living cells. CI-994 mediates G1 cell cycle arrest, inhibits proliferation and induces apoptosis in vitro and in vivo. CI-994 originally was developed as an anticonvulsant agent and later was reported to have antitumor activity.
10 mg
Cat. No.: 46-F92
$75.00
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Crizotinib
Crizotinib is a potent ATP competitive inhibitor of c-MET and anaplastic lymphoma kinase (ALK). It has been shown to display antitumor efficacy in multiple tumor models and has been shown to inhibit c-MET dependent proliferation, migration and invasion of tumor cells in vitro. Crizotinib is selective for c-MET and ALK against over 120 different kinases.
5 mg
Cat. No.: 61-V83
$129.00
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Cyclopamine
Cyclopamine is a small molecule inhibitor of the sonic hedgehog pathway (Hh) by binding to the heptahelical bundle of Smoothened. It inhibits the growth of medulloblastoma cells. Hedgehog signaling is involved in embryogenesis as well as cancer progression. It is a steroid alkaloid and originally identified as a teratogenic agent.
5 mg
Cat. No.: 29-O52
$199.00
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Dacomitinib
Dacomitinib, also known as PF-00299804, is a second-generation irreversible pan-erbB (HER) receptor tyrosine kinase inhibitor. It is believed to irreversibly inhibit erbB tyrosine kinase activity through binding at the ATP site and covalent modification of nucleophilic cysteine residues in the catalytic domains of erbB family members. The HER family of tyrosine kinases included receptors HER-1 (EGFR), HER-2,3 and 4. The HER signaling pathway plays a role in the normal regulation of cell growth and proliferation, differentiation, and apoptosis. Activation of HER receptors drives signal transduction pathways; dysregulated signaling through the HER receptors may lead to malignant transformation and growth.
5mg
Cat. No.: 21-Q15
$199.00
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Daidzin
Daidzin is a glucoside of the isoflavone daidzein found in soy beans. It demonstrates chemopreventive activities by inhibiting the bioactivation of carcinogenic arylamines. It is also a potent, selective inhibitor of human mitochondrial aldehyde dehydrogenase.
1mg
Cat. No.: 30-Z35
$39.00
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Dorsomorphin
Dorsomorphin (also known as Compound C) is a potent, reversible, AMPK inhibitor with Ki of 109 NM in the absence of AMP. In addition, it has been found to selectively inhibit bone morphogenetic protein (BMP) signaling.
Cat. No.: 08-D89
$99.00
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Dovitinib
Dovitinib is a small molecule receptor tyrosine kinase inhibitor. It potently inhibits receptor tyrosine kinases including FLT3, c-KIT, CSF-1R/c-fms, FGFR1, FGFR3, VEGFR1/Flt1,VEGFR2/Flk1, VEGFR3/Flt4, PDGFRβ, and PDGFRα. Dovitinib shows both antitumor and antiangiogenic activities in vivo. It has also been used as an effective treatment in xenograft mouse models of FGFR3 multiple myeloma (MM).
10 mg
Cat. No.: 80-Z03
$99.00
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Enzastaurin
Enzastaurin inhibits PKCβ, PKCα, PKCγ and PKCε with IC50’s of 0.006, 0.039, 0.083 and 0.110 µM, respectively. It has a direct effect on human tumor cells by inducing apoptosis and suppressing the proliferation of cultured tumor cells. Enzastaurin suppresses VEGF-induced angiogenesis in the rat corneal micropocket assay and decreases microvessel density. It also prevents VEGF secretion from human tumor cell xenographs in nude mice. Prolonged courses of Enzastaurin increases chemotherapy or radiation tumor growth delay of breast, glioma and small cell lung cancer xenographs.
10 mg
Cat. No.: 19-P20
$99.00
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Everolimus
Everolimus inhibits mTOR (mammalian target of rapamycin), a serine-threonine kinase, by binding with high affinity to the FK506 binding protein-12 (FKBP-12) thus inducing cell growth arrest and apoptosis. It is chemically very similar to Rapamycin. It is also used to prevent rejection of organ transplants.
10 mg
Cat. No.: 55-X21
$114.00
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Fludarabine
Fludarabine, also known as Fludara, F-ara-A, and NSC 118218, is a purine antimetabolite. It’s activity occurs as the result of activation to 2-fluoro-ara-ATP and includes inhibition of DNA synthesis primarily in the S-phase of cell division by inhibition of ribonucleotide reductase and the DNA polymerases. It is also postulated that fludarabine interferes with RNA by decreased incorporation of uridine and leucine into RNA and protein, respectively. Fludarabine is also active against non-proliferating cells.
10mg
Cat. No.: 31-V88
$55.00
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FTY720
FTY720 is a potent sphingosine-1-phosphate (S1P) receptors agonist that reverses the effects of BCR-ABL kinase. It is phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5.) FTY720 is a novel immunomodulating agent that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.
5 mg
Cat. No.: 14-F83
$69.00
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GANT 61
GANT 61 is a GLI antagonist. It inhibits the hedgehog (Hh) signaling pathway downstream of SMO and SUFU causing GL1 nuclear accumulation. GANT 61 has been shown to inhibit proliferation of PANC1 and 22Rv1 cancer cells in vitro. In Vivo, it has displayed display antiproliferative effects and antitumor activity. GANT 61 has also been shown to block cell growth in vivo xenograft models using human prostate cancer cells.
5 mg
Cat. No.: 89-J92
$99.00
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Showing 1–24 of 71 results