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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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A-922500
A-922500 is a diacylglycerol acyltransferase 1 (DGAT-1) inhibitor for both human and mouse. DGATs catalyze the final reaction step in the synthesis of triglyceride.
5 mg
Cat. No.: 44-K21
$150.00
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A769662
A769662 is a potent and reversible small molecule that activates AMP-activated protein kinase (AMPK). The activation of AMPK inhibits mTOR (mammalian target of rapamycin) signaling, which is a positive effector of cell growth, proliferation and survival. A769662 has been shown to inhibit the Na⁺K⁺-ATPase at higher concentrations. It also inhibits the differentiation of adipocytes.
10 mg
Cat. No.: 46-D13
$99.00
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A83-01
A83-01 is a TGFβ kinase/activin receptor like kinase (ALK5) inhibitor. It blocks the phosphorylation of Smad2 and inhibits TGFβ-induced epithelial-to-mesenchymal transition. A83-01 is more potent than small molecule SB431542, and has been shown to inhibit differentiation of rat induced pluripotent stem cells (iPSCs) and increases clonal expansion efficiency. Small molecule A83-01 helps maintain homogeneity and long-term in vitro self-renewal of human iPSCs.
2 mg
Cat. No.: 63-A05
$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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Anacardic Acid
Anacardic acid is a histone acetyltransferase (HAT) inhibitor. It inhibits the HAT activity of the transcription co-activators p300 and p300/CREB-biding protein associated factor (pCAF) with IC50 values of 8.5 and 5 µM. It has been shown to display a variety of biological activities, including antibacterial, antimicrobial, prostaglandin synthase inhibition, tyrosinase, and lipoxygenase inhibition. Anacardic acid has been shown to decrease expression of NF-κB regulated gene products including, invasion, inflammation, proliferation and cell survival. It has also been linked to be a potent activator of Aurora Kinase A (ARK-1) mediated phosphorylation of histone H3.
5 mg
Cat. No.: 08-N16
$89.00
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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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BIO
BIO is a potent, reversible and ATP-competitive inhibitor of GSK3α/β. The inhibition of GSK by BIO has been shown to activate the Wnt signaling pathway and sustain pluripotency in murine and human embryonic stem cells. BIO is the first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells. It has also been shown to induce the differentiation of neonatal cardiomyocytes.
2 mg
Cat. No.: 45-H38
$79.00
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BIX01294
BIX01294 is a histone lysine methyltransferase (HMTase) inhibitor that modulates the epigenetic status of chromatin. It selectively inhibits the G9a HMTase and the generation of histone H3 lysine 9 methylation. BIX01294, when used in combination with HDAC inhibitor Valproic Acid has been used as a replacement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS) recipes. BIX01294 is a useful for the study of histone lysine methylation, differentiation and reprogramming.
5 mg
Cat. No.: 74-O89
$99.00
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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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BX-795
BX-795 is a potent inhibitor of both PDK1 and TBK1 as well as IKKε. It acts by blocking phosphorylation and is reversible.
2 mg
Cat. No.: 68-J23
$84.00
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Cabozantinib
Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.
Cat. No.: 05-Y29
$700.00
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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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CHIR99021
CHIR99021 is the most selective inhibitor of glycogen synthase kinase 3β (GSK3β). CHIR99021 does not show cross-reactivity against cyclin-dependent kinases (CDKs) with a 350 fold selectivity toward GSK3β compared to CDKs with a Kᵢ of <10nM in vitro. CHIR99021 has been shown in long term expansion of murine embryonic stem cells in conjunction with MEK/MAPK inhibitor PD184352 and fibroblast growth factor receptor (FGFR) inhibitor SU5402.
Sale!2 mg
Cat. No.: 27-H76
Original price was: $219.00.$89.00Current price is: $89.00.
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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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Ciglitazone
Ciglitazone is an antihyperglycemic agent of the thiazolidinedione structural class, selective agonist at PPARγ (peroxisome proliferator-activated receptor γ). It activates PPARγ with an EC50 value of 3 μM in vitro, and is at least 33-fold selective over PPARα and δ. Antihyperglycemic in vivo. Ciglitazone inhibits HUVEC differentiation and angiogenesis and also stimulates adipogenesis and decreases osteoblastogenesis in human mesenchymal stem cells.
5mg
Cat. No.: 48-A90
$90.00
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CP690550
CP690550 is a novel Janus kinase 3 (JAK3) inhibitor. JAK3 is a critical cytoplasmic tyrosine kinase in the signaling pathways of multiple cytokines associated with T cell function.  CP690550 displays greater antiproliferative and pro-apoptotic activity against murine multipotent factor-dependent cell Patersen-erythropoietin receptor (FDCP-EpoR) cells harboring JAK2(V617F) compared with JAK2(WT).
5 mg
Cat. No.: 59-W26
$99.00
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Showing 1–24 of 109 results