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.

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.

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).

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.

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

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.

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.

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.

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].

DG1 (Compound 8Nc), a Thymidylate Synthase (TS) inhibitor, impedes angiogenesis and alters metabolic reprogramming in NSCLC cells, while effectively suppressing the expression of CD26, ET-1, FGF-1, and EGF. Additionally, it notably inhibits cancer tissue proliferation in the A549 xenograft mouse model [1].

MCI, a chemical compound demonstrating significant anti-inflammatory effects, particularly in collagen-induced arthritis (CIA) models, modulates inflammation through macrophage reprogramming by enhancing ROS scavenging and promoting COX-2 downregulation. It effectively inhibits COX-2, exhibiting an IC50 of 1.23 μM. Additionally, MCI holds potential for research applications in rheumatoid arthritis (RA) [1].

NOX-6-18 (GPR132-B-160) is a highly potent and selective GPR132 antagonist with insulinotropic activity that modulates macrophage reprogramming in pancreatic islets and reduces weight gain.

MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor with an IC50 of 2.4 nM. This compound prevents the interaction between mixed lineage leukemia 1 (MLL1) and WD Trp-Asp repeat domain 5 (WDR5), inhibiting MLL1 H3K4 histone methyltransferase (HMT) activity and down-regulating H3K4me3, which facilitates the epigenetic reprogramming of porcine somatic cell nuclear transfer embryos.

PLX-4545 has oral biological activity and is a cereblon based IKZF2 (zinc finger transcription factor Helios) molecular gel degrading agent that acts on immune suppressive regulatory T cells, reprogramming them into pro-inflammatory effector T cells and enhancing anti-tumor immune response.