reprogramming

OAC1 (BAS 00287861) is a compound activating Octamer-binding transcription factor 4 (Oct4). It enhances the iPSC reprogramming efficiency and accelerates the reprogramming process.

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).

4'-bromo-Resveratrolis a potent inhibitor of the deacetylases sirtuin 1 (SIRT1) and 3 (SIRT3)

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

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.

YX0798 is a selective, orally active CDK9 inhibitor (Kd: 0.28 nM). It downregulates the oncogenic protein c-MYC and the pro-survival protein MCL-1. YX0798 disrupts the cell cycle and causes transcriptome reprogramming, ultimately leading to apoptosis. The compound exhibits antitumor activity.

TE-11 is a MIF tautomerase inhibitor with an IC50 of 5.63 μM. This compound can alleviate Crohn's-like colitis, reduce MIF-induced migration of eosinophils and neutrophils, and prevent M1 polarization and associated metabolic reprogramming.

ML 083 is a highly specific allosteric activator of the tumor-associated M2 isoform of human pyruvate kinase that modulates phosphoenolpyruvate binding cooperativity, and it is used as a metabolic research tool to investigate tumor-specific glycolytic regulation and cancer-associated metabolic reprogramming.

FHND5032 is an orally active miR-124 inducer that significantly enhances miR-124 expression in macrophages. It inhibits the PIK3R2/PI3K/Akt axis to block inflammatory signaling, facilitates macrophage reprogramming, and restores epithelial barrier function. FHND5032 alleviates colitis and reduces inflammatory burden in ulcerative colitis mouse models, making it useful for ulcerative colitis research.

ZD-1-186 is a non-degradable molecular glue that effectively inhibits MYC expression in diffuse large B-cell lymphoma cells and significantly induces the expression of CDKN1A (p21). This compound facilitates the binding of BCL6 to BRD9, a non-canonical BAF complex bromodomain protein involved in sustaining MYC transcriptional activity in certain lymphoma contexts. ZD-1-186 is applicable for research in targeted transcriptional reprogramming.

promotes the reprogramming of human somatic cells to pluripotent stem cells

MM-401 is a specific inhibitor of histone H3K4 methyltransferase MLL1 activity that acts by reprogramming mouse epiblast stem cells to naive pluripotency.

Hh-Ag1.5 (SAG-1.5) is a potent Hedgehog (Hh) agonist (EC50: 1 nM) and Smoothened (Smo) receptor agonist, with an EC50 of 1 nM and Ki values between 0.5 and 2.3 nM for Smo. Hh-Ag1.5-mediated reprogramming breaks the quiescent state of non-injured hepatic stem cells and thus rescues liver failure. Hh-Ag1.5 induced differentiation of hiPSCs into skin precursor cells, spinal motor neurons and spinal sensory neurons.

GNE-140 is a novel and potent lactate dehydrogenase A (LDHA) inhibitor that disrupts glycolytic metabolism in MIA PaCa-2 human pancreatic cancer cells, inducing rapid metabolic reprogramming prior to delayed cell death, with intrinsic resistance observed in OXPHOS-dependent pancreatic cell lines that can be reversed by phenformin, while acquired resistance is driven by AMPK-mTOR-S6K pathway activation, highlighting its value for studying metabolic plasticity and therapeutic resistance.

BRD0418 acts as an upregulator of TRIB1 expression by leading to reprogramming of hepatic lipoprotein metabolism from adipogenesis to clearance it.

AS8351 (NSC51355) is a histone demethylase inhibitor. It has been used in combination with CHIR99021, A 83-01, BIX01294, SC-1, Y-27632, OAC2, SU 16f, and JNJ-10198409 to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.

L-Lactic acid-13C3 is a stable-isotope-labeled analog of L-Lactic acid (T4845) in which three carbon atoms are substituted with the non-radioactive 13C isotope, enabling precise tracing of lactate flux within metabolic pathways. L-Lactic acid-13C3 is widely used in metabolic profiling, isotope-tracing experiments, and studies of glycolytic reprogramming, offering high analytical sensitivity for quantifying lactate turnover in physiological and pathological settings.

NAT is a nicotinamide phosphoribosyltransferase (NAMPT) activator that increases intracellular NAD levels and induces subsequent metabolic and transcriptional reprogramming. It exhibits neuroprotective effects in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model and may be employed in studies of neurodegenerative diseases or conditions associated with reduced NAD levels.

SLMP53-1 is a p53 activator with anti-tumor activity, inhibits wt and mutp53, activates reprogramming of glucose metabolism in xenografted human tumor tissues, and interferes with angiogenesis and migration. SLMP53-1 inhibits tumor cell growth and can be used to study human rectal cancer.

CSF1R-IN-3 is an orally effective CSF-1R inhibitor with an IC50 value of 2.1 nM. CSF1R-IN-3 has anti-proliferative activity against colorectal cancer cells. CSF1R-IN-3 exhibits anti-tumour effects and immune enhancing effects by inhibiting the migration of macrophages and inducing the reprogramming of M2-type macrophages to M1-type macrophages, thus exhibited activity against colorectal cancer cells.

Adrixetinib (Q702) is an orally active triple inhibitor against CSF1R, Mer, and Axl, with Kd values of 8.7 nM, 0.8 nM, and 0.3 nM, respectively. Adrixetinib (Q702) acts as a potent immune modulator that remodels the tumor microenvironment, increasing M1 macrophages and CD8⁺ T cells while decreasing M2 macrophages and myeloid-derived suppressor cells (MDSCs). Adrixetinib (Q702) upregulates MHC class I and E-cadherin in tumor cells and shows efficacy in syngeneic mouse tumor models. Adrixetinib (Q702) is utilized in oncology research focused on tumor microenvironment reprogramming, macrophage polarization dynamics, and immune cell infiltration in breast cancer, renal adenocarcinoma, colon carcinoma, and melanoma models.

Misetionamide is an orally active oxathiazin-like compound that functions as a glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with antineoplastic activity, Misetionamide is widely used in cancer research to investigate metabolic reprogramming, glycolytic dependency, and metabolism-targeted anticancer therapeutic strategies.

Murlentamab (GM102) is a humanized anti-AMhRII antibody. Murlentama has potential antitumor activity that induces macrophage-mediated antitumor-dependent cell-mediated cytotoxic effects (ADCC). Murl can stimulate the pro-inflammatory and anti-tumor internal environment by recruiting, collecting and activating T cells. Murlentama exerts antitumor activity by promoting naive macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming.

CYT296 is a chromatin de-condensation agent that enhances the efficiency of induced pluripotent stem cell (iPSC) generation mediated by defined factors (OSKM) and promotes an open chromatin state in Mouse Embryonic Fibroblast (MEFs), aiding in somatic cell reprogramming. This compound has potential applications in cell replacement therapies and drug screening research [1].