embryonic stem cells

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

Stemazole is a novel small molecule human stem progenitor cell proliferation activator that promotes the survival of human embryonic stem cells and maintains stemness, and promotes the survival of oligodendrocyte precursor cells in vitro. Stemazole significantly increased cell survival and clone formation in a dose-dependent manner, reduced apoptosis, and promoted recovery of motor dysfunction and myelin repair. Stemazole can be used as a therapeutic agent in demyelinating disorders, promoting OPC survival in vitro and regeneration in vivo.

GSK-3484862 is a non-covalent Dnmt1 inhibitor that induces DNA hypomethylation, offering potential therapeutic benefits against cancer.

Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.

Phthalazinone pyrazole is potent, selective, and orally bioavailable inhibitor of Aurora-A kinase. Aurora-A is overexpressed in a variety of tumor types and displays oncogenic activity.

Epiblastin A is an inhibitor of Casein Kinase 1 (CK1). Epiblastin A engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).

IWP-2 is a Wnt pathway inhibitor (IC50=27 nM) and an ATP-competitive CK1δ inhibitor (IC50=40 nM for M82FCK1δ). IWP-2 inhibits self-renewal of embryonic stem cells and has been used in stem cell and organoid research.

MitoBloCK-6 is a potent Erv1 ALR inhibitor with IC50 values of 900 nM and 700 nM, respectively, and also inhibits Erv2 with an IC50 of 1.4 μM. Additionally, MitoBloCK-6 can induce apoptosis via cytochrome c release in human embryonic stem cells (hESCs) [1].

IDE1 can induce definitive endoderm from embryonic stem cells. It has been shown to induce the differentiation of Sox17+/FoxA2+-expressing pancreatic progenitors from human and mouse embryonic stems cells (EC50: 125.5 nM in vitro) by activating the TGF-β signaling pathway. IDE1-derived endodermal cells injected into E8.75 mouse embryos ex vivo have been shown to incorporate into the developing gut tube, contributing to its formation.

Cardiogenol C hydrochloride (Cardiogenol C) can induces the differentiation of ESCs into cardiomyocytes (EC50= 100 nM).

OAC2 is an Oct4 activator which activates expression through the Oct4 gene promoter; enhances reprogramming efficiency by increasing the rate of production of induced pluripotent stem cells (iPSCs) from embryonic fibroblasts; an analog of OAC1.

Oct3/4-inducer-1 (2-(4-(4-methoxybenzyloxy)phenyl)acetonitrile) is an OCT3/4 inducer that promotes the expression and stabilization of OCT3/4 and enhances its transcriptional activity in a variety of human cells.

TWS-119 is an inhibitor of glycogen synthase kinase-3β (GSK-3β) that induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).

MS351 is an antagonist of chromobox 7 (CBX7) that acts by binding the CBX7 chromodomain. It enhances the binding of long noncoding RNA to the CBX7 chromodomain when used at 25 μM. MS351 induces transcriptional derepression of CBX7 target genes, including p16 (INK4a), in mouse embryonic stem cells and human prostate cancer PC3 cells.

Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA (Cyclo RGDfC) TFA, a cyclic RGD peptide, displays a high affinity for αvβ3 integrin, effectively disrupting cell-integrin interactions. It suppresses pluripotent marker expression in embryonic stem cells (ESCs) and reduces the tumorigenic capability of mESCs in vivo, making it valuable in tumor research [1].

Pyrintegrin, a β1-integrin agonist, promotes the survival of embryonic stem cells, can be used as a podocyte-protective agent, and enhances cell-extracellular matrix adhesion-mediated integrin signaling.

SB 202190 hydrochloride is a selective, cell-permeable p38 MAPK inhibitor that targets p38α and p38β2 (IC50 = 50 100 nM). It exhibits anti-tumor activity and induces differentiation of human embryonic stem cells into cardiomyocytes.

Cardiogenol C is a cardiomyogenesis inducer in embryonic stem cells.

ELA-32(human) TFA is a potent apelin receptor agonist with high affinity, demonstrating an IC50 of 0.27 nM and a Kd of 0.51 nM. This compound does not bind to GPR15 or GPR25. It activates the PI3K AKT signaling pathway, facilitating self-renewal of human embryonic stem cells (hESCs) through cell-cycle progression and protein synthesis. Additionally, ELA-32(human) TFA enhances the TGFβ pathway, predisposing hESCs towards an endoderm lineage, and promotes angiogenesis in HUVEC cells.

Elsinochrome A is a perylenequinone fungal metabolite that has been found inHypomycesand has anticancer activity.1Photoactivation of elsinochrome A induces the production of singlet oxygen and apoptosis in R366.4 rhesus monkey embryonic stem cells and HCe-8693 colorectal carcinoma cells when used at concentrations ranging from 1 to 100 μM. 1.Ma, L., Tai, H., Li, C., et al.Photodynamic inhibitory effects of three perylenequinones on human colorectal carcinoma cell line and primate embryonic stem cell lineWorld J. Gastroenterol.9(3)485-490(2003)

Thymopentin acetate, primarily secreted by the epithelial cells of the thymic cortex and medulla, serves as an effective immunomodulatory agent. It possesses a short plasma half-life of 30 seconds and significantly enhances the generation of T-cell lineage from human embryonic stem cells (hESCs) [1] [2].

Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit. It stimulates phosphorylation of several ecto-type protein kinase substrates on the surface of GOTO human neuroblastoma cells when used at a concentration of 5 nM. Ganglioside GQ1b promotes differentiation of murine embryonic stem cells (mESCs) to neuronal precursor and glial cells via activation of the ERK1/2 pathway. It also induces differentiation of murine keratinocytes through phosphoinositide turnover. Ganglioside GQ1b mixture contains ganglioside GQ1b molecular species with C18:1 and C20:1 sphingoid backbones.

MEDS433 is a dihydroorotate dehydrogenase inhibitor (IC50 1.2 nM). MEDS433 inhibited the in vitro replication of hCoV-OC43 and hCoV-229E, as well as of SARS-CoV-2, at low nanomolar range. Notably, the anti-SARS-CoV-2 activity of MEDS433 against SARS-CoV-2 was also observed in kidney organoids generated from human embryonic stem cells.

Synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. Thymopentin (TP5) is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies.