TGF-β type I receptor kinase (ALK5) inhibitor
- 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 vitro and in vivo
- GMP format available
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.
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Product Details
Alternative Name |
TGF-β RI Kinase Inhibitor II, 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine, RepSox, E-616452, SJN 2511 |
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Appearance |
White to off-white or yellow solid. |
CAS |
446859-33-2 |
Couple Target |
TGF-beta receptor |
Couple Type |
Inhibitor |
Formula |
C17H13N5 |
Identity |
Identity determined by NMR. |
MW |
287.3 |
Purity |
≥98% (HPLC) |
Solubility |
Soluble in DMSO (5 mg/ml) or methanol (5 mg/ml). |
Handling & Storage
Use/Stability |
As indicated on product label or CoA when stored as recommended. 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. |
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Handling |
Protect from light. |
Long Term Storage |
-20°C |
Shipping |
Ambient Temperature |
Regulatory Status |
RUO – Research Use Only |
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- Controlling Human Stem Cell-Derived Islet Composition Using Magnetic Sorting: Kelley, A. B., Shunkarova, M., et al.; Biotechnol. Bioeng. 122, 2206 (2025), Abstract
- Depolymerizing F-actin accelerates the exit from pluripotency to enhance stem cell-derived islet differentiation: Hogrebe, N. J., Schmidt, M. D., et al.; bioRxiv , (2024)
- Cell identity dynamics and insight into insulin secretagogues when employing stem cell-derived islets for disease modeling: Wang, C., Abadpour, S., et al.; Front. Bioeng. Biotechnol. 12, 1392575 (2024), Abstract
- Controlling human stem cell-derived islet composition using magnetic sorting: Kelley, A. B., Shunkarova, M., et al.; bioRxiv , (2024)
- Prediction of diabetes mellitus after kidney transplantation using patient-specific induced pluripotent stem cells: Lim, S. W., Shin, Y. J., et al.; Kidney Res. Clin. Pract. 43, 236 (2024), Abstract
- Pump-Less, Recirculating Organ-on-Chip (rOoC) Platform to Model the Metabolic Crosstalk between Islets and Liver: Aizenshtadt, A., Wang, C., et al.; Adv. Healthc. Mater. 13, e2303785 (2024), Abstract
- NEUROD2 function is dispensable for human pancreatic β cell specification: Cota, P., Saber, L., et al.; Front. Endocrinol. (Lausanne) 14, 1286590 (2023), Abstract
- Regulation of CTCF loop formation during pancreatic cell differentiation: Lyu, X., Rowley, M. J., et al.; Nat. Commun. 14, 6314 (2023), Abstract
- Insulin regulates human pancreatic endocrine cell differentiation in vitro: P. Cota, et al.; Mol. Metab. 79, 101853 (2023), Abstract
- Prediction of diabetes mellitus development after kidney transplantation using patient-specific induced pluripotent stem cells: Lim, S. W., Shin, Y. J., et al.; Research Square , (2022)
- PAX4 loss of function alters human endocrine cell development and influences diabetes risk: Lau, H. H., Krentz, N. A. J., et al.; bioRxiv , (2022)
- 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
- 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
- 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
- A Method for Encapsulation and Transplantation into Diabetic Mice of Human Induced Pluripotent Stem Cells (hiPSC)-Derived Pancreatic Progenitors: Ghila, L., Legøy, T. A., et al.; Methods Mol. Biol. 2454, 327 (2021), Abstract
- The postnatal pancreatic microenvironment guides β cell maturation through BMP4 production: L. Sakhneny, et al.; Dev. Cell 56, 2703 (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
- Generation of insulin-producing pancreatic β cells from multiple human stem cell lines: N.J. Hogrebe, et al.; Nat. Protoc. 16, 4109 (2021), Abstract
- Angiopoietins stimulate pancreatic islet development from stem cells: S. S. Karanth, et al.; Sci. Rep. 11, 13558 (2021), Abstract
- Generation of pancreatic β cells from CD177+ anterior definitive endoderm: P.U. Mahaddalkar, et al.; Nat. Biotechnol. 38, 1061 (2020), Abstract
- 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
- 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 specialized niche in the pancreatic microenvironment promotes endocrine differentiation: C. Cozzitorto, et al.; Dev. Cell 55, 150 (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 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 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
- Identification of Embryonic Neural Plate Border Stem Cells and Their Generation by Direct Reprogramming from Adult Human Blood Cells: Thier, M. C., Hommerding, O., et al.; Cell Stem Cell 24, 166 (2019), Abstract
- Hydrogel platform for i>in vitro/i> three-dimensional assembly of human stem cell-derived β cells and endothelial cells: Augsornworawat, P., Velazco-Cruz, L., et al.; bioRxiv , (2019)
- Establishment of a high-resolution 3D modeling system for studying pancreatic epithelial cell biology in vitro: Bakhti, M., Scheibner, K., et al.; Mol. Metab. 30, 16 (2019), Abstract
- Assessment of the i>in vitro/i> function of human stem cell-derived β cells: Srivatsava, A. R., Shahan, S. T., et al.; bioRxiv , (2019)
- 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
- 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
- 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
- Intrinsic Immunity Shapes Viral Resistance of Stem Cells: X. Wu, et al.; Cell 3, 423 (2018), 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
- Cultured circulating tumor cells and their derived xenografts for personalized oncology: R. Wang, et al.; Asian J. Urol. 4, 240 (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
- Economic 3D-printing approach for transplantation of human stem cell-derived β-like cells: J. Song, et al.; Biofabrication 9, 15002 (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
- Emdogain-regulated gene expression in palatal fibroblasts requires TGF-βRI kinase signaling: A. Stähli, et al.; PLoS One 9, e105672 (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
- Generation of functional human pancreatic β cells in vitro: F.W. Pagliuca, et al.; Cell 159, 428 (2014), Abstract — Full Text
- 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
Resources
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Alternative Name | TGF-β RI Kinase Inhibitor I, 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole |
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CAS | 396129-53-6 |
Couple Type | Inhibitor |
Purity | ≥97% (TLC) |

Alternative Name | FS, Activin-binding protein, FSH-suppressing protein |
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Purity | ≥95% (SDS-PAGE using Coomassie Staining) |
Source | Produced in E. coli. Non-glycosylated protein, containing 289 amino acids. |

Alternative Name | FS, Activin-binding protein, FSH-suppressing protein |
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Purity | ≥90% (Reducing and Non-reducing SDS-PAGE) |
Source | Produced in E. coli. Non-glycosylated protein, containing 289 amino acids. |
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