| Product Name | Description |
AG 490
(Cat. No. 658401) | Potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM). Inhibition of JAK2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal hematopoiesis. Inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3.
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| AG 490, m-CF3 (Cat. No. 658408) | A cell-permeable, m-trifluoromethyl derivative of AG 490 (Cat. No. 658401) that displays apoptotic and antiproliferative properties (IC50 = 1.7 mM, 2.8 mM and 6.1 mM in 2E8, Baf/3 and Jurkat cells, respectively). Shown to inhibit IL-7-induced JAK3 tyrosine phosphorylation in 2E8 cells in vitro and significantly reduce lymph node cellularity in a murine B and T cell lymphoma model (1 mg per animal, i.p.) in vivo.
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Cucurbitacin I, Cucumis sativus L.
(Cat. No. 238590) | A cell-permeable, bitter triterpenoid compound (NCI identifier: NSC 521777) that displays anti-proliferative and antitumor properties both in vitro and in vivo. Acts as a potent and highly selective inhibitor of Janus kinase/signal transducer and activator of transcription 3 (JAK/STAT3) signaling pathway. It suppresses STAT3 tyrosine phosphorylation in v-Src-transformed NIH 3T3 cells and human lung adenocarcinoma A549 cells (IC50 = 500 nM), resulting in inhibition of STAT3 DNA-binding and STAT3-mediated gene transcription. Shown to inhibit the growth of STAT3-transformed tumors in nude mice. Does not affect oncogenic pathways mediated by Ras, Akt, Erk1/2, or JNK.
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Indirubin Derivative E804
(Cat. No. 402081) | A cell-permeable indirubin derivative (IDR) that blocks the Src-Stat3 signaling pathway and displays anti-tumor properties. Shown to be a potent, ATP-competitive inhibitor of the kinase activities of Src (IC50 = 430 nM), Cdk1/cyclin E (IC50 = 210 nM), Cdk2/cyclin A (IC50 = 540 nM), and Cdk1/cyclin B (IC50 = 1.65 mM). Reduces the tyrosine phosphorylation levels of Src, JAK1, and Stat3 in MDA-MB-468 cells in a time- and dose-dependent manner. Selectively induces apoptosis in cells expressing high levels of active Stat3, but not cells lacking activated Stat3. The apoptotic effect of E804 is shown to be due to the down-regulation of antiapoptotic proteins Mcl-1 and survivin.
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P3-AHNP Peptide Carrier
(Cat. No. 573094) |
A cell-permeable peptide carrier that is composed of a 9-mer TAT-derived internalization sequence (P3), a glycine spacer, and a 12-mer anti-HER-2/neu peptide mimetic (AHNP) and is used for targeted delivery of therapeutic agents to ErbB2 high-expressing cells. A necessary control for P3-AHNP-based deliveries, such as studies that utilize P3-AHNP-STAT3BP (Cat. No. 573092).
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Piceatannol
(Cat. No. 527948) | A plant metabolite that inhibits the activity of rat liver protein kinase A catalytic subunit (IC50 = 3 mM), PKC (IC50 = 8 mM), MLCK (IC50 = 12 mM). In RBL-2H3 cells, the selective inhibition of Syk by piceatannol results in inhibition of FceR1-mediated signaling. Also inhibits wheat embryo Ca2+-dependent protein kinase (CDPK) (IC50 = 19 mM), and p72syk (IC50 = 10 mM), a non-receptor tyrosine kinase, relative to Lyn in isolated enzyme preparations. Also possesses anti-leukemic properties.
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STAT3 Inhibitor Peptide
(Cat. No. 573095) | A Stat3-SH2 domain binding phospho-peptide that acts as a selective inhibitor of Stat3 signaling with a DB50 of 235 mM. Significantly lowers the DNA-binding activity of Stat3 by forming an inactive Stat3:peptide complex and reduces the levels of active Stat3:Stat3 dimers that can bind DNA. Displays greater affinity for Stat3, and to a lesser extent Stat1 over Stat5.
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STAT3 Inhibitor Peptide, Cell-Permeable
(Cat. No. 573096) | A cell-permeable analog of the Stat3-SH2 domain binding phospho-peptide (Cat. No. 573095) that acts as a highly selective, potent blocker of Stat3 activation. Also supresses constitutive Stat3 dependent Src transformation with no effect on Stat3 independent Ras transformation.
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STAT3 Inhibitor Peptide II, ErbB2-Selective, Cell-Permeable
(Cat. No. 573092) | The SH2 domain-binding motif- (Cat. No. 573095) derived STAT3 inhibiting sequence, PpYL (STAT3BP), is conjugated with a cell-permeant carrier sequence P3-AHNP (Cat. No. 573094), to allow its preferential delivery to ErbB2 high-expressing cells for STAT3 inhibition. P3-AHNP-STAT3BP has been shown to selectively inhibit the growth of ErbB2-overexpressing cancer cells both in vitro and in vivo.
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STAT3 Inhibitor III, WP1066
(Cat. No. 573097) | A cell-permeable AG 490 (Cat. No. 658401) analog that acts as an effective STAT3 pathway inhibitor (IC50 = 5.6 and 3.7 mM in U87-MG and U373-MG cells, respectively). |
STAT3 Inhibitor V, Stattic
(Cat. No. 573099) | A cell-permeable inhibitor of STAT3 cellular function that targets the STAT3-SH2 domain and prevents its association with upstream kinases. |
STAT3 Inhibitor VI, S31-201
(Cat. No. 573102) | A cell-permeable inhibitor of STAT3 cellular function that targets the STAT3-SH2 domain and blocks Stat3-dependent transcription. |
Tyrene CR4
(Cat. No. 655230) | A cell-permeable hydroxystryrylacrylonitrile tyrosine kinase inhibitor that displays anti-tumor properties. Potently inhibits the kinase activities of JAK2 and Bcr-Abl (IC50 ~100-600 nM and 500-700 nM, respectively), and displays excellent selectivity over other tyrosine kinases, Btk, Lck, Lyn, Src, Syk and ZAP-70 (IC50 > 5 mM). Shown to preferentially induce apoptosis in acute lymphoblastic (ALL) and myeloid leukemia cells (AML), while exhibiting little deleterious effect towards normal bone marrow cell differentiation and proliferation. Reported to be much more potent than AG 490 (Cat. No. 658401) in inducing ALL cells growth arrest (IC50 ~ 120 nM vs. 5-25 mM). Its in vivo efficacy in cancer reduction has been successfully demonstrated in NOD-SCID mice engrafted with human Ph+ ALL cells.
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