Inhibitors related stem cell from Cellagen (2)
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Inhibitors related stem cell from Cellagen (2)
Product Name: GDC-0449 (Vismodegib) | Hedgehog pathway inhibitor (#C4044)
GDC-0449 (Vismodegib) is a potent, orally bioavailable, specific hedgehog pathway small-molecule inhibitor with IC50 of
3 nM. It blocks the activities of the Hedgehog-ligand cell surface receptor SMO and suppresses Hedgehog signaling [1].
The hedgehog (HH) pathway, a key signaling pathway in embryological development, is normally inactive in differentiated
cells, with the exception of roles in tissue maintenance and repair. Constitutive reactivation of the HH pathway via
mutations and aberrant autocrine/paracrine HH ligand stimulation has been linked to a number of cancers5. GDC-0449
has been shown to target SMO with an EC50 of 2.8nmol/L on a human palatal mesenchymal cell line (HEPM) stably
expressing a GLI-responsive luciferase reporter gene, and to induce rapid regression of the tumor and suppression of the
hedgehog pathway in the Ptc1+/? murine medulloblastoma model. Furthermore, GDC-0449 inhibits the growth of
primary pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation in vitro [1-3]. GDC-0449 is also
an inhibitor of two multiple ATP-binding cassette (ABC) transporters, ABCG2/BCRP and ABCB1/Pgp, and is a mild inhibitor of ABCC1/MRP1. The overexpression of ABC transporters is associated with multidrug resistance. The IC50 values for
inhibition of ABCG2 and Pgp were approximately 1.4 and 3.0 µM, respectively [4].
Details
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Chemical Formula: |
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C19H14Cl2N2O3S |
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CAS No.: |
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879085-55-9 |
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Molecular weight: |
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421.3 |
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Purity: |
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> 98% |
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Appearance: |
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White |
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Chemical name: |
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2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide |
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Solubility: |
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Up to 100 mM in DMSO |
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Synonyms: |
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GDC-0449, GDC0449, Vismodegib, Erivedge |
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Storage: |
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Store solid powder at 4oC, or store DMSO solution at -20oC |
Reference
1. Robarge KD, et al. GDC-0449-a potent inhibitor of the hedgehog pathway. Bioorg Med Chem Lett.
2009. 19(19):5576-81. Pubmed ID: 19716296
2. Wong H, et al. Pharmacokinetic-pharmacodynamic analysis of vismodegib in preclinical models of mutational and
ligand-dependent Hedgehog pathway activation. Clin Cancer Res. 2011.17(14):4682-92. Pubmed ID: 21610148
3. Rudin CM, et al. Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449. N Engl J Med.
2009. 361(12):1173-8. Pubmed ID: 19726761
4. Zhang Y, Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp. Neoplasia.
2009. 11(1):96-101. Pubmed ID: 21610148
Product Name: ICG-001 | Wnt signaling inhibitor (#C4001)
ICG-001 is a small-molecule antagonist of b-catenin/TCF-mediated transcription (IC50 = 3 uM) and specifically
downregulates the expression of a subset of b-catenin/TCF-responsive genes. ICG-001 binds specifically to cyclic AMP
response element-binding protein (CBP), therby disrupting interaction of CBP with b-catenin. [1] ICG-001 selectively
induces apoptosis in transformed, but not normal colon cells, and reduces in vitro growth of colon carcinoma cells.
ICG-001 has also been shown to attenuate bleomycin-induced lung fibrosis in mice by selective inhibition of Wnt/
b-catenin-dependent transcription. [2]
ICG-001 is believed to correct defects in neuronal stem cell differentiation by inhibition of this pathway [3] and associated
polytopic protein Presenilin-1 (PS-1), which suggests potential therapies in Alzheimer's disease.
The wnt/b-catenin signalling pathway has been implicated in regulation of cancer stem cells and ICG-001 has been
studied in this regard. [4]
Details
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Chemical Formula: |
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C33H32N4O4 |
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CAS No.: |
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847591-62-2;780757-88-2 |
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Molecular weight: |
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548.63 |
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Purity: |
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> 98% |
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Appearance: |
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White |
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Chemical name: |
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(6S,9aS)-6-(4-hydroxybenzyl)-N-benzyl-8-(naphthalen-1-ylmethyl)-4,7-dioxo-hexahydro-
2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide |
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Solubility: |
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Up to 100 mM in DMSO |
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Synonyms: |
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ICG-001, ICG001 |
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Storage: |
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Store solid powder at 4oC, or store DMSO solution at -20oC |
Reference
1. Emami et al., A small molecule inhibitor of beta-catenin/CREB-binding protein transcription. Proc. Natl. Acad. Sci.
2004, 101(34), 12682-12687. Pubmed ID: 15314234
2. Henderson et al., Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis.
Proc. Natl. Acad. Sci. 2010, 107(32), 14309-14314. Pubmed ID: 20660310
3. Teo et al., Specific inhibition of CBP/beta-catenin interaction rescues defects in neuronal differentiation caused by a
presenilin-1 mutation. Proc. Natl. Acad. Sci. 2005, 102(34), 12171-12176. Pubmed ID: 16093313
4. Takahashi-Yanaga et al., Targeting Wnt signaling: can we safely eradicate cancer stem cells? Clin. Cancer Res.
2010, 16, 3153-3162. Pubmed ID: 20660310
Product Name: ITD-1 | TGF-β pathway inhibitor (#C4830)
ITD-1 is a novel selective TGF-β pathway-selective inhibitor 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
stimulates embryonic stem cells to differentiate into cardiomyocytes (IC50 0.4-0.8 µM) by degrading the receptor and
inhibiting intracellular signaling. 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 is non-cytotoxic. ITD-1 can
be used to study a wide range of biological questions in cellular processing and TGF-β signaling.
Details
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Chemical Formula: |
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C27H29NO3 |
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CAS No.: |
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N/A |
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Molecular weight: |
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415.52 |
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Purity: |
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> 98% |
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Appearance: |
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Yellow solid |
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Chemical name: |
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ethyl 4-([1,1'-biphenyl]-4-yl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-
carboxylate |
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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 |
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: ITDts | TGF-β pathway inhibitor (#C4838)
ITDts is a novel selective TGF-β pathway-selective inhibitor that inhibits TGF-β activity by selectively degrading the TGF-
β2 receptor at the proteosome level. Racemic ITDts is 2-fold selective over the closely related Activin A signaling
pathway. ITDts stimulates embryonic stem cells to differentiate into cardiomyocytes (IC50 0.7 µM) by degrading the
receptor and inhibiting intracellular signaling. ITDts has been formulated as a salt to increase stability and improve water
solubility (~0.1 mg/mL) for ease of handling. As a salt, ITDts is chemically and metabolically stable and is non-cytotoxic.
ITDts can be used to study a wide range of biological questions in cellular processing and TGF-β signaling.
Details
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Chemical Formula: |
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C27H26F3NO3 |
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CAS No.: |
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N/A |
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Molecular weight: |
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469.5 |
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Purity: |
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> 98% |
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Appearance: |
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Yellow solid |
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Chemical name: |
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methyl 2,7,7-trimethyl-5-oxo-4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1,4,5,6,7,8-
hexahydroquinoline-3-carboxylate |
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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 |
References:
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: IWP-3 | Wnt inhibitor (#C4971)
IWP-3 is a selective small molecule wnt inhibitor, prevents palmitylation of Wnt proteins by Porcupine (Porcn), a
membrane-bound O-acyltransferase, thereby blocking Wnt secretion and activity1. It blocks phosphorylation of the Lrp6
receptor and accumulation of both Dvl2 and β-catenin. It has an IC50 of 40 nM which is 100 folds less potent than Wnt-C59, but it can still efficiently promote cardiomyocyte differentiation from human ESCs.
Details
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Chemical Formula: |
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C22H17FN4O2S3 |
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CAS No.: |
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687561-60-0 |
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Molecular weight: |
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484.59 |
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Purity: |
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> 98% |
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Appearance: |
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Light yellow solid |
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Chemical name: |
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2-(3-(4-fluorophenyl)-3,4,6,7-tetrahydro-4-oxothieno[3,2-d]pyrimidin-2-ylthio)-N-
(6-methylbenzo[d]thiazol-2-yl)acetamide |
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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 |
References:
1. Baozhi Chen, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer.
Nature Chemical Biology (2009); 5(2), 100-107.
2. Willems E, et al. Small-Molecule Inhibitors of the Wnt Pathway Potently Promote Cardiomyocytes From Human
Embryonic Stem Cell-Derived Mesoderm. Circ Res. 2011
Product Name: LDN-193189 | BMP type I receptors ALK2/3 inhibitor (#C5361)
LDN193189 is a highly potent BMP inhibitor, prevents Smad1, Smad5, and Smad8 phosphorylation through inhibition of
BMP type I receptors ALK2 (IC50=5nM) and ALK3 (IC50=30 nM). Its inhibitions against ALK4, ALK5, and ALK7 are weak
(IC50 >500 nM). As BMP signaling coordinates developmental patterning and has essential physiological roles in mature
organisms, LDN-193189 is used to reduce ectopic ossification in a mouse model.
Details
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Chemical Formula: |
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C25H22N6 |
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CAS No.: |
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1062368-24-4 |
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Molecular weight: |
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406.48 |
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Purity: |
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> 98% |
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Appearance: |
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Yellow solid |
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Chemical name: |
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4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline |
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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 |
References:
1. Paul B Yu, et al. BMP type I receptor inhibition reduces heterotopic ossification. Nature Med. (2008) 14: 1363-1369.
2. Cuny GD, et al. Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors.
Bioorg Med Chem Lett. (2008) 18(15):4388-92.
3. Paul B Yu, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.
Nature Chem Biol. (2008) 4: 33-41.
Ordering informations
|
Catalog No. |
Product Name |
Size |
|
C4044 |
GDC-0449 (Vismodegib) | Hedgehog pathway inhibitor |
5mg, 25mg & 100mg |
|
C4001 |
ICG-001 | Wnt signaling inhibitor |
5mg, 25mg & 100mg |
|
C4830 |
ITD-1 | TGF-β pathway inhibitor |
2mg, 10mg & 50mg |
|
C4838 |
ITDts | TGF-β pathway inhibitor |
2mg, 10mg & 50mg |
|
C4971 |
IWP-3 | Wnt inhibitor |
2mg, 10mg & 50mg |
|
C5361 |
LDN-193189 | BMP type I receptors ALK2/3 inhibitor |
5mg, 25mg & 100mg |
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