cultures

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.

DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115 200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.

CS-722 Free base is a synthetic central muscle relaxant exhibiting muscle relaxant effects and inhibition of spinal reflexes. In hippocampal cultures, CS-722 Free base may suppress spontaneous inhibitory and excitatory post-synaptic currents by inhibiting sodium and calcium currents.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].

Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP human prostatic adenocarcinoma cell cultures, positioning it as a potent agent for prostate cancer research [1] [2].

Tylosin (Tylosine) is a macrolide antibiotic obtained from cultures of Streptomyces fradiae. The drug is effective against many microorganisms in animals but not in humans.

Vidarabine (Adenine Arabinoside) is a nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA viruses in cell cultures and significant antiviral activity against infections caused by a variety of viruses such as the herpes viruses, the VACCINIA VIRUS and varicella zoster virus.

Diflufenican (M&B 38544) increases the production of phytoene in carrot cell cultures by inducing the inhibition of phytoene desaturase gene expression.

3-(Methylthio)propionic acid (4-Thiapentanoic acid) is one of the metabolites of methionine (especially of D-methionine). Cultures of Streptomyces lincolnensis accumulated 3-methylthioacrylic acid in amounts directly related to the concentration of methionine in the medium. The first intermediate in the pathway may be the keto acid, which is then oxidatively decarboxylated to 3-methylthiopropionic acid.

L-Cystine dihydrochloride is an Nrf2 inducer with whitening and anti-dark spot effects.L-Cystine dihydrochloride has cytoprotective effects in cells, and is often added to various fungal cultures as a carbon source.

Methyl jasmonate ((-)-Methyl jasmonate) is a hormone involved in plant signaling, inducing oxidative stress and accumulation of secondary metabolites in plant cells and organ cultures, and regulating the biosynthesis of other plant hormones. Methyl jasmonate induces plant defense responses against Andean lupin insects. Methyl jasmonate has anti-inflammatory activity.

Calycosin (Cyclosin) acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K Akt pathways. Calycosin has antineoplastic effects against osteosarcoma through inducing apoptosis showing in vitro and in vivo investigations. Calycosin was shown to induce angiogenesis in human umbilical vein endothelial cell cultures (HUVEC) in vitro. Calycosin may be an effective skin-lightening agent that regulates the expression of melanogenic enzymes. Calycosin exhibited tyrosinase inhibitory activity with an IC(50) value of 38.4 microM.

Auten-99 HBr (Auten-99) is a myotubularin phosphatase Jumpy inhibitor exerting potent neuroprotective effects. AUTEN-99 activates autophagy in cell cultures and animal models. AUTEN-99 appears to effectively penetrate through the blood-brain barrier, and impedes the progression of neurodegenerative symptoms in Drosophila models of Parkinson's and Huntington's diseases. Furthermore, the molecule increases the survival of isolated neurons under normal and oxidative stress-induced conditions. Thus, AUTEN-99 serves as a potent neuroprotective drug candidate for preventing and treating diverse neurodegenerative pathologies, and may promote healthy aging.

Dibenz[a,h]anthracene (CCRIS 208) has induced DNA damage and gene mutations in bacteria and gene mutations and transformation in several types of mammalian cell cultures.

TTBK1-IN-2 (N-[4-(4-chlorophenoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine) is an inhibitor of Tau-Tubulin kinase (TTBK1) with IC50s of 0.24 and 4.22 µM. TTBK1-IN-2 reduces TDP-43 phosphorylation both in cell cultures and the spinal cord of transgenic TDP-43 mice.

10-Isobutyryloxy-8,9-epoxythymol isobutyrate, a major constituent of Inula helenium and Inula royleana root cultures,

Dihydrocytochalasin B (H2CB) is a cell division inhibitor that prevents cytokinesis, alters cell morphology, disrupts actin structures in Swiss 3T3 mouse fibroblasts, and inhibits DNA synthesis induced by serum growth factors in quiescent cultures. Low doses of H2CB lead to cell rounding and the loss of actin microfilament bundles.

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

Obscurolide A1 is a butenolide isolated from Streptomyces viridochromogenes cultures that shows weak inhibitory activity against Ca2+ CaM-dependent and non-Ca2+ CaM-dependent phosphodiesterases in cattle.

BMS-986104 is an effective selective modulator of the S1P1 receptor. It demonstrates efficacy in the mouse EAE model, comparable to that of FTY720. Furthermore, BMS-986104 shows promising remyelination properties in three-dimensional brain cell cultures subjected to lysophosphatidylcholine (LPC)-induced demyelination.

UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 values of 15 nM and 19 nM, respectively. It is effective in inhibiting invasion and migration of TNBC cells in vitro. Additionally, UNC0638 hydrate acts as an inhibitor of EHMT1 2 and induces the expression of fetal hemoglobin (HbF) in cultures of human erythroid progenitor cells. Furthermore, it exhibits antiviral activity against FMDV (foot-and-mouth disease virus) and VSV (vesicular stomatitis virus), demonstrating remarkable potency and selectivity across various epigenetic and non-epigenetic targets.

Perfluoroenanthic acid (Perfluoroheptanoic acid) is a perfluoroalkyl substance (PFAS) that negatively impacts spermatogenic development and testicular m6A RNA methylation in offspring exposed during gestation, thus impeding spermatogenesis and inducing reproductive toxicity. Additionally, in primary cortical neuron cultures, Perfluoroenanthic acid alters dendritic spine morphology and synaptogenesis, enhances neural activity and synaptic transmission, and increases the expression of excitatory synapse-associated proteins Synaptophysin and PSD95.

AGH-107 is a highly selective 5-HT7 receptor agonist that can cross the blood-brain barrier, featuring a Ki value of 6 nM and an EC50 value of 19 nM. Demonstrating high selectivity for central nervous system targets, AGH-107 also exhibits high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.