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ALK5 Inhibitor II

TGF-β type I receptor kinase (ALK5) inhibitor
ALX-270-445-M001 1 mg 94.00 USD
ALX-270-445-M005 5 mg 382.00 USD
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  • Potent ATP-competitive inhibitor of the TGF-β type I receptor ALK5
  • Useful for cellular reprogramming and the culture of human pluripotent stem cells
  • Active in vitroand in vivo
ALK5 inhibitor II is a cell permeable, potent, selective and ATP-competitive inhibitor of TGF-β RI kinase (IC50=23nM, 4nM and 18nM for binding, auto-phosphorylation, and cellular assay in HepG2 cells of TGF-β RI kinase, respectively). It minimally affects a panel of nine closely related kinases including p38 MAPKand GSK3 (IC50>16µM). It can be used for the induction of the pluripotency of stem cells by replacing the transcription factor SOX2 via the inhibition of TGF-β signaling and inducing the expression of the transcription factor Nanog.

Product Details

Alternative Name:TGF-β RI Kinase Inhibitor II, 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
Purity:≥97% (HPLC)
Identity:Identity determined by NMR.
Appearance:White to off-white or yellow solid.
Solubility:Soluble in DMSO (5 mg/ml) or methanol (5 mg/ml).
Shipping:Ambient Temperature
Long Term Storage:-20°C
Use/Stability:Stable for 2 years after receipt when stored at -20°C. Stock solutions are stable for up to 6 months when stored at -20°C.
Handling:Protect from light.
Regulatory Status:RUO - Research Use Only
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Product Literature References

Insulin regulates human pancreatic endocrine cell differentiation in vitro: P. Cota, et al.; Mol. Metab. 79, 101853 (2023), Abstract;
An HNF1α truncation associated with maturity-onset diabetes of the young impairs pancreatic progenitor differentiation by antagonizing HNF1β function: A. Cujba, et al.; Cell Rep. 38, 110425 (2022), Abstract; Full Text
Differentiation of beta-like cells from human induced pluripotent stem cell-derived pancreatic progenitor organoids: S. Pedraza-Arevalo, et al.; STAR Protoc. 3, 101656 (2022), Abstract; Full Text
Generation of isogenic hiPSCs with targeted edits at multiple intronic SNPs to study the effects of the type 2 diabetes associated KCNQ1 locus in American Indians: A.K. Nair, et al.; Cells 11, 1446 (2022), Abstract; Full Text
Angiopoietins stimulate pancreatic islet development from stem cells: S. S. Karanth, et al.; Sci. Rep. 11, 13558 (2021), Abstract;
Generation of insulin-producing pancreatic β cells from multiple human stem cell lines: N.J. Hogrebe, et al.; Nat. Protoc. 16, 4109 (2021), Abstract;
Selective deletion of human leukocyte antigens protects stem cell-derived islets from immune rejection: A.V. Parent, et al.; Cell Rep. 36, 109538 (2021), Abstract;
The postnatal pancreatic microenvironment guides β cell maturation through BMP4 production: L. Sakhneny, et al.; Dev. Cell 56, 2703 (2021), Abstract;
A human ESC-based screen identifies a role for the translated lncRNA LINC00261 in pancreatic endocrine differentiation: B. Gaertner, et al.; Elife. 9, e58659 (2020), Abstract; Full Text
A non-coding disease modifier of pancreatic agenesis identified by genetic correction in a patient-derived iPSC line: S. Kishore, et al.; Cell Stem Cell 27, 137 (2020), Abstract; Full Text
A specialized niche in the pancreatic microenvironment promotes endocrine differentiation: C. Cozzitorto, et al.; Dev. Cell 55, 150 (2020), Abstract; Full Text
BCL-xL/BCL2L1 is a critical anti-apoptotic protein that promotes the survival of differentiating pancreatic cells from human pluripotent stem cells: L.S.W. Loo, et al.; Cell Death Dis. 11, 378 (2020), Abstract; Full Text
Bioinformatic analyses of miRNA–mRNA signature during hiPSC differentiation towards insulin-producing cells upon HNF4α mutation: L. Ghila, et al.; Biomedicines 8, 179 (2020), Abstract; Full Text
Generation of pancreatic β cells from CD177+ anterior definitive endoderm: P.U. Mahaddalkar, et al.; Nat. Biotechnol. 38, 1061 (2020), Abstract;
Human T cells expressing a CD19 CAR-T receptor provide insights into mechanisms of human CD19-Positive β cell destruction: H. Ma, et al.; Cell Rep. Med. 1, 100097 (2020), Abstract; Full Text
Modeling type 1 diabetes in vitro using human pluripotent stem cells: N.C. Leite, et al.; Cell Rep. 32, 107894 (2020), Abstract; Full Text
Single-cell lineage analysis reveals extensive multimodal transcriptional control during directed beta-cell differentiation: C. Weng, et al.; Nat. Metab. 2, 1443 (2020), Abstract; Full Text
Targeting the cytoskeleton to direct pancreatic differentiation of human pluripotent stem cells: N.J. Hogrebe, et al.; Nat. Biotechnol. 38, 460 (2020), Abstract; Full Text
A hydrogel platform for in vitro three dimensional assembly of human stem cell-derived islet cells and endothelial cells: P. Augsornworawat, et al.; Acta Biomater. 97, 272 (2019), Abstract;
Acquisition of Dynamic Function in Human Stem Cell-Derived β Cells: L. Velazco-Cruz, et al.; Stem Cell Reports 12, 351 (2019), Application(s): Treatment of hESC culture, Abstract; Full Text
Glucose-Responsiveness of Pancreatic β-Like (GRP β-L) Cells Generated from Human Pluripotent Stem Cells: B. Rajaei, et al.; Curr. Protoc. Hum. Genet. 100, e71 (2019), Abstract;
Point mutations in the PDX1 transactivation domain impair human β-cell development and function: X. Wang, et al.; Mol. Metab. 24, 80 (2019), Abstract; Full Text
Generation and selection of pluripotent stem cells for robust differentiation to insulin-secreting cells capable of reversing diabetes in rodents: S.M. Southard, et al.; PLoS One 9, e0203126 (2018), Abstract; Full Text
Intrinsic Immunity Shapes Viral Resistance of Stem Cells: X. Wu, et al.; Cell 3, 423 (2018), Abstract; Full Text
Modeling signaling-dependent pluripotency with Boolean logic to predict cell fate transitions: A. Yachie-Kinoshita, et al.; Mol. Syst. Biol. 14, e7952 (2018), Abstract; Full Text
Cultured circulating tumor cells and their derived xenografts for personalized oncology: R. Wang, et al.; Asian J. Urol. 4, 240 (2016), Abstract; Full Text
Economic 3D-printing approach for transplantation of human stem cell-derived β-like cells: J. Song, et al.; Biofabrication 9, 015002 (2016), Abstract;
ERRγ Is required for the metabolic maturation of therapeutically functional glucose-responsive β cells: E. Yoshihara, et al.; Cell Metab. 23, 622 (2016), Abstract; Full Text
Long-term glycemic control using polymer-encapsulated human stem cell-derived beta cells in immune-competent mic: A.J. Vegas, et al.; Nat. Med. 22, 306 (2016), Abstract; Full Text
Emdogain-regulated gene expression in palatal fibroblasts requires TGF-βRI kinase signaling: A. Stähli, et al.; PLoS One 9, e105672 (2014), Abstract; Full Text
Generation of functional human pancreatic β cells in vitro: F.W. Pagliuca, et al.; Cell 159, 428 (2014), Abstract; Full Text
Reversal of diabetes with insulin-producing cells derived in vitro from human pluripotent stem cells: A. Rezania, et al.; Nat. Biotechnol. 32, 1121 (2014), Application(s): Treatment of human iPSC-derived pancreatic endocrine precursors, Abstract;
Inhibitors of Src and focal adhesion kinase promote endocrine specification: impact on the derivation of β-cells from human pluripotent stem cells: I. Afrikanova, et al.; J. Biol. Chem. 286, 36042 (2011), Abstract; Full Text
A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog: J.K. Ichida, et al.; Cell Stem Cell 5, 491 (2009), Abstract;
Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors: F. Gellibert, et al.; J. Med. Chem. 47, 4494 (2004), Abstract;

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