β-cells

Cisplatin-resistant cells-IN-1 (Compound 8) exhibits high cytotoxicity against Cisplatin-resistant cells and effectively diminishes metabolic activity at low nanomolar concentrations, with an IC50 ranging from 0.14 to 1.79 μM in various resistant cell lines, including A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR [1].

Specnuezhenide (Nuezhenide) significantly protects human neuroblastoma SH-SY5Y cells from 6-hydroxydopamine-induced neurotoxicity.Nuezhenide is the main inhibitory compound of fruits, it shows a clear inhibitory effect to the seeds of wheat and Chinese cabbage.

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.

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.

GLP-1(7-36), amide (MKC 253) is a peptide hormone released from intestinal L-cells upon nutrient consumption. It binds the GLP-1 receptor in the pancreas and displays various antidiabetic effects by potentiating glucose-induced secretion of insulin from pancreatic β-cells, increasing insulin expression.

SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.

Glycitin (Glycitein 7-O-β-glucoside), a natural isoflavone isolated from legumes, can promote the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.

Indacaterol (Onbrez; Arcapta) is a β2-Adrenergic Agonist. The mechanism of action of indacaterol is as an Adrenergic beta2-Agonist.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

Cinnamic acid (β-Phenylacrylic acid) has potential use in cancer intervention,The concentration causing a 50% reduction of cell proliferation (IC50) ranged from 1 to 4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt/β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

Genistin (Genistoside) is the major isoflavonoid of soybeans and soy products.It has been reported to possess various therapeutic effects, including anti-inflammatory and anticancer activities

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

HAEGTFTSDVS acetate is the first N-terminal 1-11 residues of GLP-1 which stimulates insulin secretion from pancreatic β-cells.

Foxy-5 Ammonium Salt is a WNT5A agonist, a mimetic peptide of WNT5A, a non-classical member of the Wnt family.Foxy-5 Ammonium Salt triggers cytoplasmic free calcium signaling without affecting β-catenin activation and inhibits migration and invasion of epithelial cancer cells.Foxy-5 Foxy-5 Ammonium Salt effectively reduces the metastatic spread of prostate cancer cells with low WNT5A expression in an in situ mouse model.

Alethine (β-Alethine) is a small molecule compound with antitumour activity and is used to treat tumours and infections. The alethine-induced up-regulation of TNFα increases the cytotoxicity of T cells.

γ-1-MSH, amide acetate (72629-65-3 free base), a putative hormone in the N-terminal region of the ACTH/beta- endorphin (beta-EP) precursor protein, was studied by RIA with an antiserum against gamma 3-MSH in ACTH-producing mouse pituitary tumor cells, AtT-20/D16v.

β-Pompilidotoxin Acetate is a wasp venom peptide. β-Pompilidotoxin Acetate can slow sodium channel inactivation and increase steady-state sodium current in cells.

β-CGRP, human acetate is one of calcitonin peptides and acts via the complex of receptor-activity-modifying protein (RAMP) and calcitonin-receptor-like receptor (CRLR) (IC50s: 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells).

Amyloid β-Protein 10-20 acetate (Amyloid β-Protein 10-20 acetate (152286-31-2 free base)) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.Amyloid β protein fragment containing the α-secretase processing site (Lys16-Leu17 bond). It also contains the HHQK domain (residues 13-16) responsible for binding to microglial cells.

DIPQUO hydrochloride is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO hydrochloride promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.

Tetrahydroxystilbene-2-O-β-D-glucoside (EH-201) is a low MW inducer of erythropoietin. Tetrahydroxystilbene-2-O-β-D-glucoside induces expression of erythropoietin, PPAR-γ coactivator 1α (PGC-1α) and haemoglobin in astrocytes and PC12 neuronal-like cells. In vivo, Tetrahydroxystilbene-2-O-β-D-glucoside treatment restores memory impairment, as assessed by the passive avoidance test, in SD, Aβ and KA mouse models. In the hippocampus of mice given Tetrahydroxystilbene-2-O-β-D-glucoside in their diet, levels of erythropoietin, PGC-1α and haemoglobin were increased. Treatment with Tetrahydroxystilbene-2-O-β-D-glucoside might be a therapeutic strategy for memory impairment in neurodegenerative disease, physiological ageing or traumatic brain injury.

NCGC00135472 (DRV1 (GPR32) agonist C2A) is a human Resolvin DI receptor DRV1 agonist with pro-catabolic properties that activates the human soluble protein D1 receptor DRV1/GPR32 receptor in beta-blocker and cAMP assays with EC50s of 0.37 uM and 0.05 uM, respectively.NCGC00135472 induces in cells overexpressing recombinant DRV1 rapid impedance changes that stimulate phagocytosis of serum-treated zymoglycans.

GSK-J4 (GSK J4 HCl) is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 μM and 6.6 μM towards KDM6B and KDM6A respectively. It is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.

Miclxin (DS37262926) is a novel MIC60 inhibitor that induces apoptosis through mitochondrial stress in mutant tumor cells via β-catenin.Miclxin is a potent inhibitor of mutant β-catenin, which is involved in the Wnt signaling pathway.Miclxin induces β-catenin-dependent apoptosis, leading to mitochondrial damage and loss of mitochondrial membrane. Miclxin has anti-tumor activity and kills tumors by targeting MIC60.

RH01386 is a small molecule that can prevent ER stress-induced β cell dysfunction and death, and inhibits proapoptotic gene expression,has the potential for type 2 diabetes treatment. RH01386 restores ER stress-impaired glucose-stimulated insulin secretio

EMD 527040 hydrochloride is an effective integrin αVβ6 inhibitor. The IC 50 values of EMD 527040 hydrochloride were 6 nM and 1.6 μM to inhibit αVβ6 binding to fibronectin and αVβ6 expression cells to fibronectin, respectively. EMD 527040 hydrochloride shows antifibrotic activity in animal models of biliary fibrosis and is active in vivo.

CGP52411 is an orally active, and ATP-competitive inhibitor of EGFR (IC50: 0.3 μM). CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells and dramatically inhibits and reverses the formation of β-amyloid Aβ42 fibril aggregates. CGP52411 can be used in studies about Alzheimer's diseases.

SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170

KT182 is a selective and  potent inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.

SSK1 is a compound that selectively kills senescent cells and is a precursor for β-galactosidase, which can reduce the inflammatory response of the body. SSK1 can activate the phosphorylation of p38 MAPK and MKK3/MKK6 in senescent cells, and promote mitochondrial DNA damage in senescent cells.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

Sabizabulin (ABI-231) is an effective and orally bioavailable inhibitor of α and β tubulin against panels of melanoma and prostate cancer cell lines. Sabizabulin inhibits tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7. Sabizabulin shows antiproliferative activity and can be used in prostate cancer studies.

AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation ( IC 50 =1 μM), does not blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].

BI 6015 is an antagonist of HNF4α. HNF4α is a nuclear receptor that regulates gene expression in the intestine cells, liver cells, and pancreas-β cells.

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

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).

Hydroxysafflor yellow A (Safflomin A) inhibited adipogenesis by increasing HSL promoter activities. Hydroxysafflor yellow A can effectively protect the liver from long-term alcohol injury by enhancing antioxidant capacity and inhibiting the expression of TGF-β. It prevents steroid-induced avascular necrosis of femoral head by inhibiting primary bone marrow-derived mesenchymal stromal cells. Also, Hydroxysafflor yellow A has anti-tumor effects.

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].

β,β-Dimethylacrylalkannin is a natural product isolated from Arnebia nobilis Reichb.f, increases collagen and involucrin content in skin cells.

PNU 74654 binds to β-catenin (Kd = 450 nM), inhibiting its interaction with the transcription factor T cell factor 4 (Tcf4) resulting in disruption of the Wnt signaling pathway.

DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].

Urolithin C is a gut metabolite of ellagic acid. Urolithin C induces apoptosis in PC12 cells through a mitochondria-mediated pathway.

QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor. Modulates ARF-GTP levels and synergizes with the Wnt/β-catenin signaling pathway to upregulate β-catenin nuclear translocation. Also reduces in vitro migration of metastatic human breast cancer cells.

Ch55 (3,5-Di-tert-butylchalcone) is an effective inducer of the differentiation of HL60 cells (EC50 = 200 nM) and shows high affinity with RAR-α and RAR-β receptors. Ch55 can be used in studies about cancer.

β-Aminopropionitrile (3-Aminopropionitrile) is a selective inhibitor of lysyl oxidase.

1. Peimisine (Ebeiensine) can affect M-receptor, excit β-receptor, restrain the release of internal calcium, and promote to releaseing nitrogen monoxidum in order to relax tracheal smooth muscle and relieve asthma. 2. Peimisine can attenuate lung tissue injury( ALI), LDH and MDA amount in ALI mice in a dose dependent manner, it also lower the total protein, total white blood cells, lymphocyte and neutrophilic leukocyte in bronchoalveolar lavage fluid( BALF); suggests that peimisine can play a protective role against LPS-induced acute lung injury. 3. Peimisine has the protective effect on the experimental hepatic fibrosis formation, the possible mechanisms are associated with inhibiting fibrogenesis and fibrosis accumulation, and decreasing lipid peroxidation. 4. Peimisine can inhibit angiotensin I converting enzyme activity in a dose-dependent manner, displaying 5 % inhibitory concentration values of 526.5 microM, thus, it may have antihypertensive action.

β-Catenin-IN-37 is a selective inhibitor of the protein-protein interaction between β-Catenin and T-cell factor (Tcf), known as β-catenin/Tcf PPI. It effectively inhibits canonical Wnt signaling and impedes the growth of colorectal cancer cells SW480 and HCT116, with IC50 values of 20 μM and 31 μM, respectively.

Ladanetin-6-O-β-(6′′-O-acetyl)glucoside, a flavonoid extracted from Dracocephalum tanguticum whole plants, exhibits antioxidant properties and cardioprotective effects, mitigating Doxorubicin-induced toxicity in H9c2 cells [1].