anti-proliferation activity

Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.

U-83836E (lazaroid ) has neuroprotective activity and anti-tumor activity, inhibits glioma cell proliferation, inhibits tumor necrosis factor and reverses endotoxin-induced shock.

Inflachromene (ICM) is an inhibitor of HMGB1 and HMGB expression with anti-inflammatory activity.Inflachromene reduces seizure severity in a mouse model of epilepsy by inhibiting HMGB1 translocation, inhibits endothelial proliferation through the HMGB1/2-regulated TLR4-NF-κB pathway, and inhibits autophagy by regulating Beclin 1 activity. Inflachromene can be used to study epilepsy.

Amiprilose (SM 1213) has anti-inflammatory activity and inhibits the proliferation of a variety of hyperproliferative cell types.Amiprilose induces lymphokine-induced macrophage activation and may be used in studies of rheumatoid arthritis and psoriasis.

KRM-III is an orally active T cell antigen receptor (TCR) inhibitor with anti-inflammatory activity that potently inhibits TCR and myristate acetate/fosfomycin/ionomycin-induced NFAT nuclear factor activation and T cell proliferation, with an IC50 of approximately 5 μM.

(±)4-HDHA (4-Hydroxy docosahexaenoic acid) is a PPARγ agonist with anti-inflammatory activity that directly inhibits endothelial cell proliferation and sprouting angiogenesis via PPARγ, which can be used in the study of diabetes.

Prinaberel (ERB 041) is a selective and potent estrogen receptor β (ERβ) agonist with anticancer activity that restores or increases ERβ expression and reduces cancer cell proliferation in mouse squamous cell carcinoma and human carcinoma cells. Prinaberel exhibits anti-inflammatory activity, inhibits the NFκB pro-inflammatory signaling pathway, and induces apoptosis of ovarian cancer cells. study endometriosis.

Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling. Icaritin at low concentration (4 or 8 μMol/L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.

Trypsin is a serine protease that can be isolated from fish to hydrolyze lysine or arginine carboxy-side proteins. With the anti-inflammatory activity, Trypsin could induce the cell membrane fusion of PDCoV-infected cells through the interaction between the S glycoprotein of PDCoV and pAPN, activate PAR2 and PAR4, and promote cell proliferation and differentiation. Trypsin can be used to promote wound healing and study neurogenic inflammation.

2,2-Dimethyl-2,3-dihydrobenzofuran-7-ol inhibits the proliferation of the THP-1 cell line and exhibits anti-infective activity against Leishmania and Toxoplasma gondii RH.

Rhapontigenin (Protigenin) is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. At higher concentrations, rhapontigenin inhibits the proliferation of HL-60R and HepG2 cancer cell lines (IC50: 48 μM).

CCR-11 is a tannin-containing derivative with antimicrobial activity. CCR-11 inhibits the proliferation of B. subtilis and HeLa cells. CCR-11 inhibits bacterial proliferation and bacterial cytoplasmic division by inhibiting FtsZ assembly and GTPase activity. CCR-11 has potential anti-tumor activity and can be used to study breast cancer and pediatric myelodysplasia.

ZINC194100678 is an effective PAK1 inhibitor with IC50 of 8.37μM. ZINC194100678 showed strong anti-proliferation activity, with IC50 value of 40.16μM against MDA-MB-231.

IMS2186 is a reagent with activity of antichoroidal neovascularization (CNV). IMS2186 could arrest cancer cell cycle in G2 M phase, result in exerting anti-proliferation and anti-angiogenesis effects. IMS2186 reduces the amount of eye leakage and diseased cells with no intraocular toxicity.

Topoisomerase II inhibitor 13 inhibits topoisomerase II (Topo II) that shows strong anti-proliferation activity against HL-60 MX2 cancer cells derived from HL-60 against Topo II toxicity.

Doxycycline hydrochloride (Hyclate) is an orally active tetracycline antibiotic with broad-spectrum matrix metalloproteinase (MMP) inhibitory activity, possessing both antibacterial and anti-cancer cell proliferation effects, and can be used to induce gene expression in ON-OFF systems.

Golotimod (SCV 07) is an antimicrobial dipeptide with immunomodulatory activity that significantly improves the efficacy of anti-tuberculosis therapy, induces thymic and splenic cell proliferation, modulates macrophage function, and inhibits STAT3 signaling.Golotimod has been used in the study of recurrent genital Herpes Simplex Virus 2 (HSV-2) infection and oral mucositis.

Puerarin-4'-O-β-D-glucopyranoside (Puerarin4'-O-glucoside) is a natural product isolated from Pueraria lobata root, exhibiting estrogenic activity and anti-proliferative effects in MCF-7 human breast carcinoma cells.

TC-S 7003 (Lck Inhibitor) is an orally active, selective and potent lymphocyte kinase (Lck) inhibitor with anti-inflammatory activity, inhibition of Lck, Lyn, Src, and Syk kinases, and inhibition of T-cell proliferation, and may be useful in the study of arthritis.

Radicicol (Monorden) is an antifungal antibiotic and a potent inhibitor of heat shock protein 90 (Hsp90), which leads to the degradation of Hsp90 by the proteasome by binding to its ATP-binding pocket. In addition, Radicicol inhibits the growth and proliferation of several tumor cell lines. It also has anti-malarial activity and acts as an inhibitor of adipose- and obesity-related proteins (FTO). Radicicol inhibits iNOS gene expression by blocking the p38 kinase signaling pathway and NF-kB/Rel

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. USL311 inhibits CXCR4 activation and decreases proliferation and migration of CXCR4-expressing tumor cells, with anti-tumor activ

MRT-92 is an antagonist of Smoothened (Smo) with anti-cancer activity, featuring a binding affinity (Ki) of 0.7 nM. It inhibits the Hedgehog signaling pathway by obstructing the overlapping binding sites within the transmembrane domain of the Smoothened receptor and suppresses the proliferation of cerebellar granule cells in rodents (IC50=0.4 nM). MRT-92 is utilized for research into cerebellar gliomas.

GPX4-IN-14 (compound 2c) acts as a GPX4 inhibitor, exhibiting both free radical scavenging activity (with a maximum scavenging rate of 72.52%) and anti-tumor proliferation activity in vitro. This compound targets GPX4 protein, elevating lipid peroxide and intracellular Reactive Oxygen Species (ROS) levels, which induces ferroptosis and contributes to its anti-tumor proliferation effects.

ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.