Inhibitors related stem cell from Cellagen (1)
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Inhibitors related stem cell from Cellagen (1)
Product Name: (+)-ITD-1 | TGF-β pathway inhibitor (#C4832)
(+)-ITD-1 is a resolved enantiomer of ITD-1 that possesses a greater than 2-fold increase in TGF-β inhibition (~400 nM)
and 1.3-fold increase in cardiogenesis compared to the racemic ITD-1. (+)-ITD-1 is largely responsible for TGF-β pathway-
selective inhibition that inhibits TGF-β activity by selectively degrading the TGF-β2 receptor at the proteosome level.
(+)-ITD-1 does not block the closely related Activin A signaling pathway. (+)-ITD-1 has been formulated as a salt to
increase stability and improve water solubility (~0.1 mg/mL) for ease of handling. As a salt, ITD-1 is chemically and
metabolically stable and can be used to study a wide range of biological questions in cellular processing and TGF-β
signaling.
Details
Chemical Formula: |
|
C27H29F3NO3 |
CAS No.: |
|
N/A |
Molecular weight: |
|
412.52 |
Purity: |
|
> 98% |
Appearance: |
|
Yellow solid |
Chemical name: |
|
ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-
carboxylate |
Solubility: |
|
Up to 50 mM in DMSO |
Storage: |
|
Store solid powder at 4oC, or store DMSO solution at -20oC |
Reference
1. Willems E, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic
stem cells. Cell Stem Cell. 2012;11(2):242-52. PMID: 22862949
Product Name: (-)-ITD-1 | TGF-β pathway inhibitor (#C4831)
(-)-ITD-1 is a resolved enantiomer of ITD-1 that possesses significantly less TGF-β inhibition and cardiogenesis compared
to either racemic ITD-1 or (+)-ITD-1. Compared to racemic ITD-1 or (+)-ITD-1, (-)-ITD-1 can serve as a control for non-
specific effects of ITD-1. (-)-ITD-1 has been formulated as a salt to increase stability and improve water solubility
(~0.1 mg/mL) for ease of handling. As a salt, (-)-ITD-1 is chemically and metabolically stable and can be used as a control in the study a wide range of biological studies in cellular processing and TGF-β signaling.
Details
Chemical Formula: |
|
C27H29NO3 |
CAS No.: |
|
N/A |
Molecular weight: |
|
415.52 |
Purity: |
|
> 98% |
Appearance: |
|
Yellow solid |
Chemical name: |
|
ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-
carboxylate |
Solubility: |
|
Up to 50 mM in DMSO |
Storage: |
|
Store solid powder at 4oC, or store DMSO solution at -20oC |
Reference
1. Willems E, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in
embryonic stem cells. Cell Stem Cell. 2012;11(2):242-52. PMID: 22862949
Product Name: 53AH | Wnt pathway inhibitor (#C5324)
53AH is a selective Wnt pathway inhibitor. It is a cyclohexyl analog of IWR-1 with defined centers of chirality. In the Wnt
assay, the 53AH has 5-fold greater potency in Wnt inhibition. Compared to IWR-1, 53AH is more potent at promoting
stem cell differentiation into cardiomyocytes. The increase in Wnt pathway inhibition potency correlates with a 1.4-fold
increase in cardiogenesis. 53AH possesses superior physicochemical properties compared to IWR-1 including improved
water solubility and significantly increased chemical stability at pH = 7.4 and low cytotoxicity. Accordingly, 53AH is
significantly more robust for long-term cell-based experiments and potency in cardiogenesis because of its superior
chemical properties.
Details
Chemical Formula: |
|
C26H28N2O3 |
CAS No.: |
|
N/A |
Molecular weight: |
|
416.51 |
Purity: |
|
> 98% |
Appearance: |
|
Off white solid |
Chemical name: |
|
(1R,4r)-4-((2s,3aR,4R,7S,7aS)-1,3-dioxooctahydro-1H-4,7-methanoinden-2-yl)-N-
(quinolin-8-yl)cyclohexanecarboxamide |
Solubility: |
|
Up to 50 mM in DMSO |
Storage: |
|
Store solid powder at 4oC, or store DMSO solution at -20oC |
Reference
1. Willems E, et al, Small-molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human
embryonic stem cell-derived mesoderm. Circ Res. 2011;109(4):360-4. PMID: 21737789
Product Name: A83-01 | ALK4/5/7 inhibitor (#C2831)
A83-01 is a selective inhibitor of ALK5 (12nM), ALK4 (45nM), and ALK7 (7.5 nM), and only weakly inhibits ALK1, 2, 3,
and 6. It inhibits the TGF-β-induced epithelial-to-mesenchymal transition (EMT) via the inhibition of Smad2
phosphorylation. A83-01 has been used to generate rat and human iPS cells towards a mouse ES cell like self-renewal
state.
Details
Chemical Formula: |
|
C25H19N5S |
CAS No.: |
|
909910-43-6 |
Molecular weight: |
|
421.52 |
Purity: |
|
> 98% |
Appearance: |
|
Pale yellow solid |
Chemical name: |
|
3-(6-methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide |
Solubility: |
|
Up to 100 mM in DMSO |
Storage: |
|
Store solid powder at 4oC, or store DMSO solution at -20oC |
References:
1. Tojo M, Hamashima Y, et al. The ALK-5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal
transition by transforming growth factor-beta. Cancer Science (2005), 96(11), 791-800.
2. Li W, Wei W, et al. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming
and chemical inhibitors. Cell Stem Cell (2009), 4(1), 16-19.
Product Name: Cyclopamine | Hedgehog pathway inhibitor (#C2925)
Cyclopamine is a naturally-occurring chemical that belongs to the group of steroidal jerveratrum alkaloids, a teratogen
isolated from the corn lily (Veratrum californicum). It is a specific Inhibitor of hedgehog (Hh) signaling, likely via direct
inhibition of Smoothened. Because hedgehog signaling pathway is involved in embryogenesis and cancer progression,
Cyclopamine could be used as the inducer of stem cell differentiation towards definitive endoderm pancreatic islet cells,
and as a modulator controlling cell proliferation, and as a drug to kill stem-like cancer cells and block tumor engraftment.
Details
Chemical Formula: |
|
C27H41NO2 |
CAS No.: |
|
4449-51-8 |
Molecular weight: |
|
411.62 |
Purity: |
|
> 98% |
Appearance: |
|
White solid |
Chemical name: |
|
(2'R,3S,3'R,3a'S,6aS,6bS,6'S,7a'R,11aS,11bR)-3',6',10,11b-tetramethyl-1,2,3,3a',4,4',5',6,6a,6b,6',7,7',7a',8,11,11a,11b-octadecahydro-3'H-spiro[benzo[a]fluorene-9,2'-furo[3,2-b]pyridin]-3-ol |
Solubility: |
|
Up to 100 mM in DMSO |
Storage: |
|
Store solid powder at 4oC, or store DMSO solution at -20oC |
References:
1. Chen JK et al. Inhibition of Hedgehog signaling by direct binding of cyclopamine to Smoothened. Genes Dev.
(2002); 16(21):2743-8.
2. Jiang J. et al. Hedgehog signaling in development and cancer. Dev Cell. (2008) 15(6):801-12.
3. D'Amour KA et al. Production of pancreatic hormone-expressing endocrine cells from human embryonic stem cells.
Nat Biotechnol. (2006). 24(11): 1392-401.
4. Gallo R. et al. Hedgehog signaling during expansion of human pancreatic islet-derived precursors. Ann N Y Acad Sci.
(2008) Dec;1150:43-5
5. Matthew P. Scott. Cancer: A twist in a hedgehog's tale. Nature(2003) 425, 780-782.
6. Eli E. Bar, et al. Cyclopamine-Mediated Hedgehog Pathway Inhibition Depletes Stem-Like Cancer Cells in Glioblastoma.
Stem Cells.( 2007) 25(10): 2524–2533.
Product Name: DAPT | γ-secretase inhibitor (#C3178)
DAPT is a γ-secretase inhibitor and indirectly an inhibitor of Notch, a γ-secretase substrate. Since the Notch pathway is
involved in the development of both the nervous system and pancreas, DAPT may be useful in modulating Notch activity in embryonic stem cell differentiation studies.
Details
Chemical Formula: |
|
C23H26F2N2O24 |
CAS No.: |
|
208255-80-5 |
Molecular weight: |
|
432.46 |
Purity: |
|
> 98% |
Appearance: |
|
White solid |
Chemical name: |
|
N-[(3,5-Difluorophenyl)acetyl]-L-alanyl-2-phenylglycine-1,1-dimethylethyl ester |
Solubility: |
|
Up to 35 mM in DMSO |
Storage: |
|
Store solid powder at 4oC, or store DMSO solution at -20oC |
References:
1. Dovey, HF. et al. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J Neurochem.
2001 Jan;76(1):173-81.
2. Crawford, T. and Roelink, H. (2007) The Notch Response inhibitor DAPT enhances neuronal differentiation in
embryonic stem cell-derived embryoid bodies independently of Sonic Hedgehog Signaling. Dev Dyn. 2007 Mar;236(3):
886-92.
Ordering information
Catalog No. |
Product Name |
Size |
C4832 |
(+)-ITD-1 | TGF-β pathway inhibitor |
2mg, 10mg & 50mg |
C4831 |
(-)-ITD-1 | TGF-β pathway inhibitor |
2mg, 10mg & 50mg |
C5324 |
53AH | Wnt pathway inhibitor |
2mg, 10mg & 50mg |
C2831 |
A83-01 | ALK4/5/7 inhibitor |
2mg, 10mg & 50mg |
C2925 |
Cyclopamine | Hedgehog pathway inhibitor |
2mg, 10mg & 50mg |
C3178 |
DAPT | γ-secretase inhibitor |
5mg, 25mg & 100mg |
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