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Stem cell reprogramming and differentiation reagents are small molecules that steer cell identity in culture. Chemical cocktails can replace or support transcription factors when somatic cells are reprogrammed into induced pluripotent stem cells (iPSCs). Frequent components include the histone deacetylase (HDAC) inhibitor valproic acid and the lysine-specific demethylase 1 (LSD1) inhibitor tranylcypromine. RepSox blocks the transforming growth factor beta (TGF-β) type I receptor and can replace the transcription factor Sox2. Inhibition of glycogen synthase kinase 3 (GSK-3) with CHIR-99021 and of MAP kinase kinase (MEK) with PD0325901 keeps mouse embryonic stem cells in the ground state. Differentiation protocols use retinoic acid, the Hedgehog pathway agonists SAG and purmorphamine, and IDE1 for definitive endoderm.
Cardiogenol C is a potent and cell permeable inducer of embryonic stem cell differentiation in cardiomyocytes displaying an Ec50 of 100nm.
Synonyms: Isoxazole 9
ISX-9 is a small molecule inducer of adult neural stem cell differentiation.
O4I2 is a potent inducers of Oct3/4. O4I2 showed high activity in enforcing Oct3/4 expression. O4I2 is a new class of small molecules suitable for iPSC generation.
Synonyms: Cardiogenol C
Cardiogenol C is a diaminopyrimidine compound that induces the differentiation of MHC- (myosin heavy chain) positive cardiomyocytes from embryonic stem cells with an EC50 value of 0.1 uM. Cardiogenol C upregulates cardiac markers and induces cardiac functional properties in lineage-committed progenitor cells.
Synonyms: GSK3 Inhibitor IX; MLS 2052
BIO is a cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β with IC50 value of 5 nM.
Synonyms: SKF 385 hemisulfate
Tranylcypromine hemisulfate is an irreversible, nonselective inhibitor of monoamine oxidase (MAO) and also acts as a lysine-specific demethylase 1 (LSD1) inhibitor. This compound demonstrates notable antidepressant effects and is utilized in the treatment of depression. Additionally, tranylcypromine hemisulfate has been shown to suppress lesion growth and alleviate generalized hyperalgesia in mouse models of induced endometriosis, making it a valuable tool for research in both psychiatric and pain-related studies.
Synonyms: CHIR99021; CT99021 monohydrochloride; CT 99021
CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
Synonyms: CT99021 trihydrochloride; CT 99021; CHIR99021
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM.
SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.
Epiblastin A is an inhibitor of Casein Kinase 1 (CK1) that engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).
RSC133 is a dual epigenetic modulator that inhibits both histone deacetylases (HDACs) and DNA methyltransferases (DNMTs). It effectively enhances the reprogramming of human somatic cells into induced pluripotent stem cells (iPSCs) and supports the maintenance of pluripotency by promoting an undifferentiated state. RSC133 is a valuable tool for stem cell research and epigenetic reprogramming studies.
IDE2 is a cell-permeable small molecule that promotes definitive endoderm formation in both mouse and human embryonic stem cells (ESCs) through activation of the TGF-β signaling pathway.
Neurodazine is a neurogenesis inducer that promotes the differentiation of pluripotent cells into neuronal lineages. This compound activates the Wnt and Shh signaling pathways, facilitating neural development and potentially improving neuroregeneration applications. Neurodazine is suitable for research in developmental biology, neuroscience, and regenerative medicine.
BIX-01294 hydrochloride hydrate is a selective inhibitor of histone-lysine methyltransferase (HMTase), specifically targeting G9a with an IC50 of 1.7 μM. This compound effectively reduces methylation of histone H3 at lysine 9 (H3K9me), promoting autophagy and apoptosis in human glioma cells. BIX-01294 serves as a valuable tool in epigenetic research and the study of cancer biology.
BIX-01294 trihydrochloride is a reversible and selective inhibitor of G9a and GLP histone methyltransferases, with reported IC50 values of 1.7 μM and 0.9 μM, respectively. It functions by competing for binding at the N-terminal site of substrate lysine residues, thereby inhibiting methylation processes. BIX-01294 trihydrochloride has been shown to induce necroptosis and autophagy, demonstrating antitumor activity particularly in recurrent tumor cells. Its utilization in research may further elucidate the roles of histone methylation in cancer biology and potential therapeutic strategies.
Synonyms: Magnesium valproate; VPA magnesium; 2-Propylpentanoic acid magnesium
Valproic acid magnesium is an orally active histone deacetylase (HDAC) inhibitor that exhibits an IC50 range of 0.5 to 2 mM, specifically inhibiting HDAC1 with an IC50 of 400 μM while promoting the proteasomal degradation of HDAC2. This compound activates Notch1 signaling and demonstrates anti-proliferative effects in small cell lung cancer (SCLC) cells. Valproic acid magnesium has diverse therapeutic applications, including the treatment of epilepsy, bipolar disorder, metabolic diseases, HIV infection, and the prevention of migraine headaches.
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Synonyms: E-616452 hydrochloride; SJN 2511 hydrochloride
RepSox hydrochloride is a highly selective inhibitor of transforming growth factor-β receptor I (TGF-β-RI) and activin-like kinase 5 (ALK5). It effectively inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. This reagent is valuable for investigating the roles of TGF-β signaling in obesity and metabolic disorders, including type 2 diabetes.
Synonyms: CHIR-99021 dihydrochloride; CT99021 dihydrochloride
Laduviglusib dihydrochloride is a selective inhibitor of glycogen synthase kinase-3 (GSK-3), an enzyme involved in numerous cellular processes including glycogen synthesis, cell differentiation, and apoptosis. By inhibiting GSK-3, Laduviglusib dihydrochloride promotes cell survival and has been extensively studied in the context of neurodegenerative diseases, diabetes, and cancer research. This compound serves as a valuable tool for elucidating the role of GSK-3 in various signaling pathways and therapeutic applications.
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Kyoto Probe 1 is a fluorescent probe specifically designed for labeling human induced pluripotent stem cells (hiPSCs). It exploits the unique expression patterns of ATP-binding cassette (ABC) transporters in hiPSCs compared to differentiated cells, making it a valuable tool for studying stem cell biology and differentiation processes. This probe facilitates the visualization and tracking of hiPSCs in various research applications, including regenerative medicine and developmental biology.
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PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). This compound effectively eliminates undifferentiated human pluripotent stem cells (hPSCs), making it a valuable tool for stem cell research and differentiation studies. Its ability to precisely target TOP2A provides researchers with a means to manipulate pluripotency and investigate cellular differentiation processes.
Synonyms: SR1 hydrochloride
Stemregenin 1 hydrochloride is a purine derivative that acts as an antagonist of the aryl hydrocarbon receptor (AhR). It has been shown to inhibit AhR signaling in CD34+ cells with an IC50 value of 127 nM. This compound is utilized in stem cell research to enhance the pluripotency and expansion of hematopoietic stem cells (HSC), providing valuable insights into stem cell biology and regenerative medicine.
Mesendogen is a selective TRPM6 inhibitor that plays a crucial role in the regulation of magnesium homeostasis. It enhances the differentiation of human embryonic stem cells (hESCs) and human induced pluripotent stem cells (hiPSCs) into mesodermal and definitive endoderm lineages. This compound is valuable for research focused on early embryonic development and the role of magnesium in cellular processes.
Synonyms: SKF 385
Tranylcypromine is a potent monoamine oxidase (MAO) inhibitor that increases levels of neurotransmitters such as serotonin, norepinephrine, and dopamine in the brain. This compound is primarily used in the research of mood disorders and depression therapies, offering insights into the biochemical pathways involved in these conditions. Its specific mechanism of action makes it valuable for studying the modulation of neurotransmitter systems and the pharmacological effects of MAO inhibition.
Oct4 inducer-1 is a potent activator of the Oct4 transcription factor, significantly enhancing the expression of Oct4 and Nanog promoters. This compound promotes the formation of induced pluripotent stem cells (iPSCs) and improves the efficiency of cell reprogramming while reducing the overall reprogramming time. It is a valuable tool for research applications in stem cell biology and regenerative medicine.
Oct4 inducer-2 is a compound that promotes the expression of endogenous OCT4, facilitating the maintenance and proliferation of human induced pluripotent stem cells (hiPSCs). This inducer is valuable for research applications focused on stem cell biology, regenerative medicine, and anti-aging studies. By enhancing OCT4 levels, Oct4 inducer-2 supports the maintenance of pluripotency, making it an essential tool for scientists investigating cellular reprogramming and differentiation.
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