Inhibitors related stem cell from Cellagen (3)
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Inhibitors related stem cell from Cellagen (3)
Product Name: LY2157299 | TGF-β receptor (TβR) inhibitor (#C5921)
LY2157299, a specific and potent TGF-β receptor (TβR) inhibitor that competitively binds to the active site of its kinase
domain1, inhibiting TGF-β-mediated SMAD2 phosphorylation/activation and down streaming signaling.
LY2157299 inhibited hematopoetic suppression in primary hematopoietic stem cells, such that it improved anemia in a
TGF-β overexpressing transgenic mouse model, and stimulated hematopoiesis from primary MDS bone marrow
specimens2. Daily oral administration of LY2157299 in patients with advanced/metastatic cancer was tolerated well with
an expected pharmacokinetic profile3,4.
gDetails
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Chemical Formula:
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C22H19N5O
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CAS No.:
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700874-72-2, 912477-03-3
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Molecular weight:
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369.42
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Purity:
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> 98%
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Appearance:
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Off white solid
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Chemical name:
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4-[2-(6-Methyl-pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-quinoline-6- carboxylic acid amide
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Solubility:
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Up to 50 mM in DMSO
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Storage:
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Store solid powder at 4oC, or store DMSO solution at -20oC
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References
1. Yingling, J. et al. Targeting the TGF-ß RI kinase with LY2157299: A PK/PD-driven drug discovery and clinical development
program. Proc Amer Assoc Cancer Res, 46, SY13-2, (2005).
2. Zhou L., et al. Reduced SMAD7 leads to overactivation of TGF-beta signaling in MDS that can be reversed by a specific
inhibitor of TGF-beta receptor I kinase. Cancer Res. 71(3):955-63. (2011).
3. Bueno, L.,et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor
TGF-b kinase antagonist, in mice. Eur J Cancer., 44(1):142-150, (2008).
4. E. Calvo-Aller et al. First human dose escalation study in patients with metastatic malignancies to determine safety and
pharmacokinetics of LY2157299, a small molecule inhibitor of the transforming growth factor-beta receptor I kinase.
J Clin Oncol 26: (May 20 suppl; abstr 14554), (2008)
Product Name: NVP-LDE225 | Smo inhibitor (#C5332)
LDE225 is a novel and specific, orally bioavailable Smo inhibitor with an IC50 of 11 nM. It has been shown to potentially
inhibit Hh-and Smo-dependent proliferation in vivo. It also induced the regression of preformed basaloid lesions with an
IC50 of <150 nM and almost complete regression at 1.5 μM. Topical application of a 1% LDE225 solution to depilated skin
of C57/BL6 mice completely inhibited hair growth during anagen phase as well as the expression of the Hh-pathway
target genes (Gli1, Gli2, Sox9, and N-Myc) and partial inhibition was obtained when applying a 0.3% solution.
Details
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Chemical Formula:
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C26H26F3N3O3
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CAS No.:
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956697-53-3
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Molecular weight:
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485.5
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Purity:
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> 98%
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Appearance:
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White solid
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Chemical name:
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N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4'-(trifluoromethoxy)biphenyl-3-carboxamide
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Solubility:
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Up to 50 mM in DMSO
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Storage:
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Store solid powder at 4oC, or store DMSO solution at -20oC
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Reference
1. Shifeng Pan et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med. Chem. Lett.,
2010, 1 (3), pp 130–134.
Product Name: NVP-XAV939 | Wnt/β-catenin Inhibitor (#C9289)
XAV939 is a small molecule which selectively inhibits β-catenin-mediated transcription. It stimulates β-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. Using a quantitative chemical
proteomic approach, XAV939 was found to stabilize axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 and
tankyrase 2 with IC50 of 11 nM and 4 nM.
Details
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Chemical Formula:
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C14H11F3N2OS
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CAS No.:
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284028-89-3
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Molecular weight:
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312.31
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Purity:
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> 98%
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Appearance:
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White solid
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Chemical name:
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2-(4-(trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol
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Solubility:
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Up to 50 mM in DMSO
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Storage:
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Store solid powder at 4oC, or store DMSO solution at -20oC
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References
1. Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling; Shih-Min A. Huang et al. Nature (2009) 461, 614-620
2. Hedin, L. et al. Forskolin effects on the cAMP system and steroidogenesis in the immature rat ovary. Mol Cell Endocrinol
(1983) 33: 69-80.
Product Name: PS48 | PDK1 inhibitor (#C7748)
PS48 is an allosteric small molecule activator of phosphoinositide-dependent protein kinase 1 (PDK1). It binds to the
HM/PIF binding pocket instead of the ATP-binding site. PS48 has been used to enhance reprogramming of neonatal
human epidermal keratinocytes (NHEKs).
Details
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Chemical Formula:
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C17H15CIO2
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CAS No.:
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1180678-32-7
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Molecular weight:
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286.75
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Purity:
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> 98%
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Appearance:
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White solid
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Chemical name:
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5-(4-Chloro-phenyl)-3-phenyl-pent-2-enoic acid
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Solubility:
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Up to 100 mM in DMSO
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Storage:
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Store solid powder at 4oC, or store DMSO solution at -20oC
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References:
1. Hindie et al. Structure and allosteric effects of low-molecular- weight activators on the protein kinase PDK1. Nature Chem
Biol. (2009) 5: 758-764.
2. Bobkova et al. Discovery of PDK1 Kinase Inhibitors with a novel mechanism of action by ultra-high throughput screening.
J Biol Chem. (2010) 285: 18838-18846.
3. Zhu et al. Reprogramming of Human Primary Somatic Cells by Oct4 and Chemical Compounds. Cell Stem Cell. (2010) 7
(6)651-655.
Product Name: Pyroxamide | HDAC inhibitor (#C7376)
Pyroxamide is a potent histone deacetylase (HDAC) inhibitor with IC50 of 100nM. Pyroxamide induced terminal
differentiation in murine erythroleukemia (MEL) cells, and inhibited the growth by cell cycle arrest or apoptosis in a variety
of tumor cells1-4. An accumulation of acetylated histones and increased levels of p21/WAF1 expression were detected in
cancer cells and in prostate xenografts treated with pyroxamide1,2.
Details
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Chemical Formula:
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C13H19N3O3
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CAS No.:
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382180-17-8
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Molecular weight:
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265.31
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Purity:
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> 98%
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Appearance:
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Off white solid
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Chemical name:
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N-Hydroxy-N'-3-pyridinyloctanediamid
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Solubility:
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Up to 50 mM in DMSO
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Storage:
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Store solid powder at 4oC, or store DMSO solution at -20oC
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References:
1. Butler et al. Inhibition of transformed cell growth and induction of cellular differentiation by pyroxamide, an inhibitor of
histone deacetylase. Clin.Cancer Res. 7 962. (2001)
2. Kutko, MC., et al. Histone deacetylase inhibitors induce growth suppression and cell death in human rhabdomyosarcoma
in vitro. Clin Cancer Res. Nov 15;9(15):5749-55.(2003)
3. Kouraklis G, Theocharis S. Histone deacetylase inhibitors and anticancer therapy. Curr Med Chem Anticancer Agents.
Jul;2(4):477-84.(2002)
4. Kouraklis G, Theocharis S Histone deacetylase inhibitors: a novel target of anticancer therapy (review). Oncol Rep.
Feb;15(2):489-94. (2006)
Product Name: RO4929097 | γ-secretase inhibitor (#C7649)
RO4929097 is a potent and selective small molecule inhibitor of γ-secretase (IC50=4nM), producing inhibitory activity of
Notch signaling in tumor cells. It inhibits Notch processing in tumor cells as measured by the reduction of intracellular
Notch expression by Western blot. This leads to reduced expression of the Notch transcriptional target gene Hes1.
RO4929097 does not block tumor cell proliferation or induce apoptosis but instead produces a less transformed,
flattened, slower-growing phenotype. Current it is in phase I study in patients with advanced solid tumors.
Details
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Chemical Formula:
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C22H20F5N303
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CAS No.:
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847925-91-1
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Molecular weight:
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469.40
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Purity:
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> 98%
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Appearance:
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White solid
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Chemical name:
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2,2-dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b, d]azepin-7-yl)-N′- (2,2,3,3,3-pentafluoro-propyl)-malonamide
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Solubility:
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Up to 50 mM in DMSO
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Storage:
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Store solid powder at 4oC, or store DMSO solution at -20oC
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Reference
1. Luistro L, He W et al. Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo
efficacy and pharmacodynamic properties. Cancer Res. 2009;69(19):7672-80.
Ordering informations
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Catalog No.
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Product Name
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Size
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C5921
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GDC-0449 (Vismodegib) | Hedgehog pathway inhibitor
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2mg, 10mg & 50mg
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C5332
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NVP-LDE225 | Smo inhibitor
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2mg, 10mg & 50mg
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C9289
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NVP-XAV939 | Wnt/β-catenin Inhibitor
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2mg, 10mg & 50mg
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C7748
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PS48 | PDK1 inhibitor
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5mg, 25mg & 100mg
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C7376
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Pyroxamide | HDAC inhibitor
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5mg, 25mg & 100mg
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C7649
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RO4929097 | γ-secretase inhibitor
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2mg, 10mg & 50mg
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