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LDN 193189

LDN 193189 is a small-molecule inhibitor that selectively targets glycogen synthase kinase-3 (GSK-3).
It has been studied for its potential therapeutic applications in various disease contexts, including neurodegenerative disorders, cancer, and metabolic conditions.
LDN 193189 has been shown to modulate GSK-3-dependent signaling pathways, potentially leading to neuroprotective, anti-proliferative, and metabolic effects.
Reserach on the pharmacological properties, mechanisms of action, and clinical utility of LDN 193189 is ongoing to further elucidate its therapeutic potential and optimize its use in biomedical applications.

Most cited protocols related to «LDN 193189»

1
Directed Differentiation of hPSCs into SC-β Cells
Cited 63 times

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Publication 2014
Betacellulin Cell Lines Cells Chir 99021 Differentiations, Cell Human Embryonic Stem Cells Human Induced Pluripotent Stem Cells Humidity LDN 193189 Population Group Stem Cells Y 27632
2
Neural Induction and Nociceptor Differentiation
Cited 58 times
Neural induction was performed as previously reported6 (link). Briefly, cells were rendered to single cells using accutase plated on gelatin for 30 minutes to remove MEFs. Non-adherent cells were collected and plated on matrigel treated dishes at a density of 20-40,000 cells/cm2 (link) in the presence of MEF-conditioned hESC media containing 10 ng/ml FGF-2 and 10 μM Y-27632. Neural differentiation was initiated when the cells were confluent using KSR media containing 820 ml of Knockout DMEM, 150 ml Knockout Serum Replacement, 1 mM L-glutamine, 100 μM MEM non-essential amino acids, and 0.1 mM β-mercaptoethanol. To inhibit SMAD signaling, 100nM LDN-193189 and 10 μM SB431542 were added on days 0 through 5. Cells were fed daily, and N2 media was added in increasing 25% increments every other day starting on day 4 (100% N2 on day 10). Nociceptor induction was initiated with the addition of the three inhibitors 3 μM CHIR99021, 10 μM SU5402, 10 μM DAPT on days 2 through 10. Cell passage to lower density can promote maturation of SOX10+ progenitors, and long-term culture media consisted of N2 containing 25ng/ml human-b-NGF, BDNF, and GDNF.
Chambers S.M., Qi Y., Mica Y., Lee G., Zhang X.J., Niu L., Bilsland J., Cao L., Stevens E., Whiting P., Shi S.H, & Studer L. (2012). Combined small molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors. Nature biotechnology, 30(7), 715-720.
Publication 2012
1,2-dilinolenoyl-3-(4-aminobutyryl)propane-1,2,3-triol 2-Mercaptoethanol 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide accutase Amino Acids, Essential Cardiac Arrest Cells Chir 99021 Culture Media Culture Media, Conditioned Fibroblast Growth Factor 2 Gelatins Glial Cell Line-Derived Neurotrophic Factor Glutamine Homo sapiens Human Embryonic Stem Cells Hyperostosis, Diffuse Idiopathic Skeletal inhibitors LDN 193189 matrigel Nervousness Nociceptors Serum SOX10 Transcription Factor SU 5402 Y 27632
3
Differentiation of hPSCs into Neurons
Cited 36 times

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Publication 2018
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide accutase Adrenal Cortex Cells Ciliary Neurotrophic Factor Doxycycline Hyclate Glial Cell Line-Derived Neurotrophic Factor LDN 193189 Mus Neuroglia Neurotrophic Factor, Brain-Derived Puromycin Tetracycline Trans-Activators XAV939 Y 27632
4
Monolayer Differentiation of hPSCs to Paraxial and Lateral Mesoderm
Cited 25 times

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Publication 2016
accutase Activins Becaplermin BMP4 protein, human Cartilage Fibroblast Growth Factor 2 Fibroblasts LDN 193189 Mesoderm Paraxial Mesoderm PD-0325901 Serum Somites thiazovivin transforming growth factor beta1.2 vismodegib XAV939
5
Differentiation of hESCs and iPSCs into Neurons
Cited 22 times

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Publication 2013
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide accutase Ascorbic Acid Bucladesine Cells Dietary Supplements dispase Embryo Fibroblast Growth Factor 2 Fibroblasts Growth Factor Human Embryonic Stem Cells Induced Pluripotent Stem Cells LDN 193189 Mus Nervousness Neurons NKX2-1 protein, human noggin protein Promega purmorphamine XAV939

Most recents protocols related to «LDN 193189»

1
Differentiation of Excitatory Neurons from iPSCs
The iPSC cultures were maintained in NutriStem hPSC XF Medium (Biological Industries, 01-0005). When iPSCs reached confluency, the cells were differentiated into excitatory neurons on Geltrex (ThermoFisher, A1413202) coated plates. Cells were maintained in N2/B27 media containing 485 mL Neurobasal medium (Life Technologies), 5 mL N2 (Gibco, 17502001), 5 mL Glutamax (ThermoFisher Scientific), 5 mL penicillin–streptomycin), 10 mL B27 supplement (Gibco, 17504044). For the first 7 days, the medium was supplemented with 10 μM SB431542 (Sigma-Aldrich, S4317), 1 μM dorsomorphin (Sigma-Aldrich, P5499) and 100 nM LDN193189 (Sigma-Aldrich, SML0559). On days 8–29, the N2/B27 media was changed daily, without supplementing the media with SB431542, dorsomorphin or LDN193189. On day 30, cells were transitioned in Brainphys Neuronal Medium (Stemcell Technologies, 05790) supplemented with B-27, with media change twice weekly. Methods for differentiation of cerebral organoids and extraction of RNA had been described in our previous studies [19 (link), 20 (link)].
Kathuria A., Lopez-Lengowski K., McPhie D., Cohen B.M, & Karmacharya R. (2023). Disease-specific differences in gene expression, mitochondrial function and mitochondria-endoplasmic reticulum interactions in iPSC-derived cerebral organoids and cortical neurons in schizophrenia and bipolar disorder. Discover Mental Health, 3(1), 8.
Publication 2023
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide Biopharmaceuticals Cells dorsomorphin Induced Pluripotent Stem Cells LDN 193189 Neurons Organoids Penicillins Stem Cells Streptomycin
2
Differentiation of Excitatory Neurons from iPSCs
The iPSC cultures were maintained in NutriStem hPSC XF Medium (Biological Industries, 01-0005). When iPSCs reached confluency, the cells were differentiated into excitatory neurons on Geltrex (ThermoFisher, A1413202) coated plates. Cells were maintained in N2/B27 media containing 485 mL Neurobasal medium (Life Technologies), 5 mL N2 (Gibco, 17502001), 5 mL Glutamax (ThermoFisher Scientific), 5 mL penicillin–streptomycin), 10 mL B27 supplement (Gibco, 17504044). For the first 7 days, the medium was supplemented with 10 μM SB431542 (Sigma-Aldrich, S4317), 1 μM dorsomorphin (Sigma-Aldrich, P5499) and 100 nM LDN193189 (Sigma-Aldrich, SML0559). On days 8–29, the N2/B27 media was changed daily, without supplementing the media with SB431542, dorsomorphin or LDN193189. On day 30, cells were transitioned in Brainphys Neuronal Medium (Stemcell Technologies, 05790) supplemented with B-27, with media change twice weekly. Methods for differentiation of cerebral organoids and extraction of RNA had been described in our previous studies [19 (link), 20 (link)].
Kathuria A., Lopez-Lengowski K., McPhie D., Cohen B.M, & Karmacharya R. (2023). Disease-specific differences in gene expression, mitochondrial function and mitochondria-endoplasmic reticulum interactions in iPSC-derived cerebral organoids and cortical neurons in schizophrenia and bipolar disorder. Discover Mental Health, 3(1), 8.
Publication 2023
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide Biopharmaceuticals Cells dorsomorphin Induced Pluripotent Stem Cells LDN 193189 Neurons Organoids Penicillins Stem Cells Streptomycin
3
Differentiation of iPSCs into NPCs
Differentiation of iPSCs into NPCs was initiated, as previously described (Maguire et al, 2016 (link)) with indicated modification. Briefly, cultures were treated with daily media changes containing SB431542 (10 μM; Tocris), LDN193189 (1 μM, Tocris), and endo‐IWR1 (1.5 μM; Tocris) and supplemented with B27 without vitamin A (Invitrogen) and passaged at days 4 and 8 of differentiation. From days 8 to 14 of differentiation, NPCs were expanded in Invitrogen neural expansion media, containing Neural Induction Supplement in Advanced DMEM/F12 and Neurobasal Medium (Invitrogen, per manufacturer instructions). On Day 14, NPCs were cryopreserved after confirmation of NPC identity with > 90% expression of Forse‐1.
Schlotawa L., Tyka K., Kettwig M., Ahrens‐Nicklas R.C., Baud M., Berulava T., Brunetti‐Pierri N., Gagne A., Herbst Z.M., Maguire J.A., Monfregola J., Pena T., Radhakrishnan K., Schröder S., Waxman E.A., Ballabio A., Dierks T., Fischer A., French D.L., Gelb M.H, & Gärtner J. (2023). Drug screening identifies tazarotene and bexarotene as therapeutic agents in multiple sulfatase deficiency. EMBO Molecular Medicine, 15(3), e14837.
Publication 2023
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide Dietary Supplements Endometriosis Induced Pluripotent Stem Cells LDN 193189 Nerve Expansion Nervousness Vitamin A
4
Midbrain Organoid Generation from iPSCs
The method for generating midbrain organoids from iPSCs was adapted from a previously published literature (Qian et al., 2018 (link)). Briefly iPSCs (Corriel) were dissociated into single cells with Versene solution (Gibco) and plated into a well of an Aggrewell plate (Stemcell Technologies Inc.) at 3,000 cells per microwell. The plate was spun down according to manufacturer’s recommendation in StemFlex medium (Gibco) supplemented with 10 µM ROCK inhibitor Y-27632 (Tocris 1254). After overnight incubation, about 300 spheroids were collected and transferred into a well of a 6-well ultralow attachment plate (Corning) containing midbrain differentiation medium one consisting of DMEM/F12 (Gibco), 20% Gibco KnockOut Serum Replacement (Gibco), 1X Glutamax (Gibco), 1X MEM Non-essential Amino Acid solution (Gibco), 55 µM 2-Mercaptoethanol (Gibco 21985023), 1X Pen/Strep (Gibco), 100 nM LDN-193189 (Tocris 6053), 10 µM SB-431542 (Tocris 1614), 2 µM Purmorphamine (Tocris 4551), 200 ng/mL Sonic hedgehog (Peprotech 100–45), and 200 ng/mL FGF-8b (Peprotech 100–25). After 5 days of culture, the medium was replaced with midbrain differentiation medium two consisting of DMEM/F12, 1X N-2 Supplement (Gibco), 1X Glutamax, 1X MEM Non-essential Amino Acid solution, 1X Pen/Strep, 100 nM LDN-193189, 3 µM CHIR-99021 (Tocris 4953), 2 µM Purmorphamine, 200 ng/mL Sonic hedgehog, and 200 ng/mL FGF-8b. At this stage and thereafter, the plate was placed on an orbital shaker rotating at 120 RPM in an incubator. On day 7, midbrain organoid differentiation medium three consisting of DMEM/F12, 1X N-2 Supplement, 1X Glutamax, 1X MEM Non-essential Amino Acid, 1X Pen/Strep, 100 nM LDN-193189, 3 µM CHIR-99021 was added. After seven additional days of incubation, the medium was replaced with final midbrain organoid differentiation medium consisting of Neurobasal medium (Gibco), 1X B-27 Supplement (Gibco), 1X Glutamax, 55 µM 2-Mercaptoethanol, 1X Pen/Strep, 0.2 mM Ascorbic acid (Sigma Aldrich A92902), 0.5 mM cAMP (Acros Organics), 20 ng/mL Brain-derived neurotrophic factor (Peprotech 450–02), 20 ng/mL Glial-derived neurotrophic factor (Peprotech 450–10), 1 ng/mL Transforming growth factor beta (Peprotech 100–21).
Abbott J., Tambe M., Pavlinov I., Farkhondeh A., Nguyen H.N., Xu M., Pradhan M., York T., Might M., Baumgärtel K., Rodems S, & Zheng W. (2023). Generation and characterization of NGLY1 patient-derived midbrain organoids. Frontiers in Cell and Developmental Biology, 11, 1039182.
Publication 2023
2-Mercaptoethanol 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide Amino Acids, Essential Ascorbic Acid Cells Chir 99021 Dietary Supplements Erinaceidae Glial Cell Line-Derived Neurotrophic Factor Induced Pluripotent Stem Cells LDN 193189 Mesencephalon Neurotrophic Factor, Brain-Derived Organoids purmorphamine Serum Stem Cells Streptococcal Infections Transforming Growth Factor beta Versene Y 27632
5
Dual SMAD-Mediated Neural Differentiation of hiPSCs
Once hiPSC reached approximately 90% confluence, neural differentiation was performed according to a modified dual SMAD protocol (Shi et al., 2012 (link)). Neural induction was initiated by changing the media into neural induction media containing 50% DMEM/F12 (Thermo Fisher Scientific, 11330057), 50% advanced neurobasal medium (Thermo Fisher Scientific, 21103049), 1% N2 (Thermo Fisher Scientific, 17502048), 1% B27 without retinoic acid (Thermo Fisher Scientific, 1258010), 1% Glutamax™ (Thermo Fisher Scientific, 35050061), 1% non-essential amino acid (NEAA, Thermo Fisher Scientific, 11140-050), 0.1% Pen/Strep (Sigma-Aldrich, United States, P0781-100ML), supplemented with the inhibitors 10 μM SB431542 (SMAD inhibitor, SMS-gruppen, S1067) and 0.1 μM LDN193189 (Noggin analog, Sigma-Aldrich, SML0559). The cells were maintained in induction media for 12 days with daily media change. On day 12, a uniform neuroepithelial sheet appeared, and the neural progenitor cells (NPCs) were passaged with Accutase (Thermo Fisher Scientific, A1110501) into neural expansion media containing growth factors 10 ng/ml FGF2 (ProSpec, CYT-557) and 10 ng/ml EGF (ProSpec, CYT-217) instead of the inhibitors. NPCs were expanded and banked. Following expansion, NPCs were plated onto Poly-L-Ornithine (PLO, Sigma-Aldrich, P4957)/laminin (Sigma-Aldrich, L2020-1 mg) coated dishes with a seeding density of 50,000 cells/cm2, and terminal neural differentiation was performed in neural maturation media, supplemented with 50 μM db-cAMP (Sigma Aldrich, D0627-100 mg), 200 μM Ascorbic acid (Sigma Aldrich, A4403-100MG), 20 ng/ml BDNF (ProSpec, CYT-207) and 10 ng/ml GDNF (ProSpec, CYT-305). The maturation process was carried out for 5 weeks for MitoTracker™ and Golgi ICC analysis and 7 weeks for assessment of Aβ secretion and Tau phosphorylation as well as MitoTracker™, Golgi and synaptic evaluation, with partial media change every third day, before the neurons were fixed or harvested for further analyses.
Haukedal H., Corsi G.I., Gadekar V.P., Doncheva N.T., Kedia S., de Haan N., Chandrasekaran A., Jensen P., Schiønning P., Vallin S., Marlet F.R., Poon A., Pires C., Agha F.K., Wandall H.H., Cirera S., Simonsen A.H., Nielsen T.T., Nielsen J.E., Hyttel P., Muddashetty R., Aldana B.I., Gorodkin J., Nair D., Meyer M., Larsen M.R, & Freude K. (2023). Golgi fragmentation – One of the earliest organelle phenotypes in Alzheimer’s disease neurons. Frontiers in Neuroscience, 17, 1120086.
Publication 2023
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide accutase Amino Acids, Essential Ascorbic Acid Cells Factor X Fibroblast Growth Factor 2 Glial Cell Line-Derived Neurotrophic Factor Golgi Apparatus Human Induced Pluripotent Stem Cells Hyperostosis, Diffuse Idiopathic Skeletal inhibitors Laminin LDN 193189 Nerve Endings Nerve Expansion Nervousness Neural Stem Cells Neurogenesis Neurons noggin protein Phosphorylation polyornithine Prospec secretion Streptococcal Infections Tretinoin

Top products related to «LDN 193189»

1
Ldn193189 by Merck Group
Sourced in United States, United Kingdom, Germany
LDN193189 is a small molecule inhibitor of the ALK2 (ACVR1) receptor. It functions by blocking the kinase activity of ALK2, a type I bone morphogenetic protein (BMP) receptor. This inhibition can modulate BMP signaling pathways.
2
Ldn193189 by Selleck Chemicals
Sourced in United States
LDN193189 is a small molecule that acts as an inhibitor of the bone morphogenetic protein (BMP) signaling pathway. It is commonly used as a tool compound in research applications to study the role of BMP signaling in various biological processes.
3
Sb431542 by Bio-Techne
Sourced in United Kingdom, United States, Canada, China
SB431542 is a potent and selective inhibitor of the transforming growth factor-beta (TGF-β) type I receptor activin receptor-like kinase (ALK) 4, ALK5, and ALK7. It blocks TGF-β signaling by inhibiting the phosphorylation and activation of Smad2 and Smad3.
4
Dmem f12 by Thermo Fisher Scientific
Sourced in United States, United Kingdom, Germany, China, France, Japan, Canada, Australia, Italy, Switzerland, Belgium, New Zealand, Spain, Denmark, Israel, Macao, Ireland, Netherlands, Austria, Hungary, Holy See (Vatican City State), Sweden, Brazil, Argentina, India, Poland, Morocco, Czechia
DMEM/F12 is a cell culture medium developed by Thermo Fisher Scientific. It is a balanced salt solution that provides nutrients and growth factors essential for the cultivation of a variety of cell types, including adherent and suspension cells. The medium is formulated to support the proliferation and maintenance of cells in vitro.
5
Sb431542 by Merck Group
Sourced in United States, Germany, United Kingdom, China, Japan, Australia, Sao Tome and Principe
SB431542 is a small molecule that inhibits the transforming growth factor-beta (TGF-β) signaling pathway. It acts as a selective and potent inhibitor of the activin receptor-like kinase (ALK) receptors, primarily ALK4, ALK5, and ALK7. This compound can be used in cell culture and research applications to investigate the role of the TGF-β signaling pathway.
6
Glutamax by Thermo Fisher Scientific
Sourced in United States, Germany, United Kingdom, France, Switzerland, Canada, Japan, Australia, China, Belgium, Italy, Denmark, Spain, Austria, Netherlands, Sweden, Ireland, New Zealand, Israel, Gabon, India, Poland, Argentina, Macao, Finland, Hungary, Brazil, Slovenia, Sao Tome and Principe, Singapore, Holy See (Vatican City State)
GlutaMAX is a chemically defined, L-glutamine substitute for cell culture media. It is a stable source of L-glutamine that does not degrade over time like L-glutamine. GlutaMAX helps maintain consistent cell growth and performance in cell culture applications.
7
N2 supplement by Thermo Fisher Scientific
Sourced in United States, Germany, Japan, United Kingdom, France, Italy, China, Canada, Czechia, Belgium, Australia, Switzerland
The N2 supplement is a laboratory-grade nitrogen enrichment solution used to support the growth and development of cell cultures. It provides an additional source of nitrogen to cell culture media, which is essential for cellular metabolism and protein synthesis.
8
Ldn193189 by Bio-Techne
Sourced in United Kingdom
LDN193189 is a small molecule inhibitor that specifically targets the BMP (Bone Morphogenetic Protein) signaling pathway. It acts as an ATP-competitive inhibitor of the BMP type I receptors ALK2, ALK3, and ALK6.
9
Fibroblast growth factor 2 (fgf2) by Thermo Fisher Scientific
Sourced in United States, United Kingdom, Germany, France, Canada, Israel, Japan, Macao, Italy
FGF2 is a recombinant human fibroblast growth factor 2 protein. It is a heparin-binding growth factor that stimulates the proliferation of a variety of cell types, including fibroblasts, myoblasts, and vascular endothelial cells.
10
B27 supplement by Thermo Fisher Scientific
Sourced in United States, United Kingdom, Germany, Japan, Canada, China, Italy, France, Switzerland, Spain, Israel, Australia, Austria, Poland, Denmark, Palestine, State of
B27 supplement is a serum-free and animal component-free cell culture supplement developed by Thermo Fisher Scientific. It is designed to promote the growth and survival of diverse cell types, including neurons, embryonic stem cells, and other sensitive cell lines. The core function of B27 supplement is to provide a defined, optimized combination of vitamins, antioxidants, and other essential components to support cell culture applications.

More about "LDN 193189"

LDN 193189 is a small-molecule inhibitor that selectively targets glycogen synthase kinase-3 (GSK-3), a pivotal enzyme involved in various disease processes.
This compound has garnered significant attention for its potential therapeutic applications in diverse medical contexts, including neurodegenerative disorders, cancer, and metabolic conditions.
Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase that plays a crucial role in regulating numerous cellular pathways.
By selectively inhibiting GSK-3, LDN 193189 has been shown to modulate GSK-3-dependent signaling cascades, potentially leading to neuroprotective, anti-proliferative, and metabolic effects.
In the realm of neurodegenerative disorders, such as Alzheimer's disease and Parkinson's disease, LDN 193189 has been investigated for its ability to mitigate disease progression and promote neuronal survival.
The compound's inhibition of GSK-3 may help to reduce the accumulation of tau protein tangles and amyloid-beta plaques, which are hallmarks of neurodegenerative pathologies.
Similarly, in the context of cancer, LDN 193189 has demonstrated anti-proliferative properties, potentially by disrupting the aberrant cell signaling pathways that drive uncontrolled cell growth and tumor development.
Ongoing research is exploring the use of LDN 193189 as a adjuvant therapy or in combination with other anti-cancer agents.
Moreover, LDN 193189's ability to influence metabolic processes, such as glucose homeostasis and lipid metabolism, has garnered interest in its potential applications for metabolic disorders, including type 2 diabetes and non-alcoholic fatty liver disease.
Complementary compounds, such as SB431542 (a selective inhibitor of the transforming growth factor-beta (TGF-β) signaling pathway), DMEM/F12 (a cell culture medium), GlutaMAX (a glutamine supplement), N2 supplement (a serum-free supplement), FGF2 (a growth factor), and B27 supplement (a serum-free supplement), have also been investigated in the context of LDN 193189 research, as they may contribute to the overall understanding of cellular mechanisms and therapeutic strategies.
Ongoing research continues to elucidate the pharmacological properties, mechanisms of action, and clinical utility of LDN 193189, with the aim of optimizing its use and harnessing its therapeutic potential in various biomedical applications.