Autophagy

Cordycepin (3'-Deoxyadenosine) is a purine nucleoside antimetabolite and antibiotic isolated from the fungus Cordyceps militaris with potential antineoplastic

KJ Pyr 9 is an MYC inhibitor (Kd: 6.5 nM in vitro assay).

Clotrimazole (FB 5097), an imidazole derivative with a broad spectrum of antimycotic activity, inhibits biosynthesis of the sterol ergostol.

Amsacrine (AMSA) (mAMSA) an antineoplastic agent which can intercalate into the DNA of tumor cells.

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. It demonstrates excellent tumor stroma remodeling capabilities and is applicable in research on solid tumors, such as glioblastoma.

Tozasertib (MK-0457) is a pan-Aurora kinase inhibitor (Kis: 0.6/18/4.6 nM for Aurora A/Aurora B/Aurora C).

Autophagyagonist-1 (compound 22) is an autophagy agonist. It exhibits significant anticancer activity against HepG2 cells and normal cells, with IC50 values of 8.8 μM and > 50 μM, respectively. The compound induces G1/S phase cell cycle arrest, suppresses the expression of CDK4 and CyclinD1, and upregulates P21. Additionally, Autophagyagonist-1 enhances autophagosome, LC3, and PINK1 accumulation, thereby promoting autophagy and mitophagy in HepG2 cells.

Bromocriptine mesylate (CB-154) is a potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM)

Clofarabine (Clofarex)m, a second generation purine nucleoside analog with antineoplastic activity, inhibits the enzymatic activities of ribonucleotide

3'-Hydroxypterostilbene suppresses colon cancer cell growth (COLO 205, HCT-116, HT-29) by triggering apoptosis and autophagy, affecting key pathways.

RSVA405 is an AMPK activator (EC50 = 1 μM), and is STAT3 inhibitor

Ethyl 3,4-dihydroxybenzoate (EDHB): a prolyl hydroxylase inhibitor attenuates acute hypobaric hypoxia mediated vascular leakage in brain.

3BDO is a new mTOR activator. 3BDO inhibits autophagy.

Sitagliptin (MK0431), an oral DPP-4 inhibitor, treats type 2 diabetes alone or with metformin/thiazolidinedione by increasing incretins and insulin.

Tenovin-6 HCl: Inhibits SIRT1 (21µM), SIRT2 (10µM), HDAC8; potent p53 activator.

Esmolol is a cardioselective beta-blocker used in parenteral forms in the treatment of arrhythmias and severe hypertension.

GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay.

Norepinephrine bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.

JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Perifosine (KRX-0401) is an oral-active, alkyl-phosphocholine Akt inhibitor with potential antineoplastic activity.

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP-IV with IC50 of 19 nM in Caco-2 cell extracts.

Enzastaurin (LY317615) (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα/γ/ε.

Guggulsterone (Guggulsterone E&Z) E&Z is a 3-hydroxy steroid. It has a role as an androgen.

Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is an neurotransmitter dopamine antagonist.

CA77.1(CA) is a novel chaperon-mediated autophagy (CMA) activator for the treatment of Alzheimer's disease (AD).

Cilengitide (EMD 121974) is a potent integrin inhibitor for the αvβ3/5 receptor (IC50: 4.1/79 nM, in cell-free assays); ~10-fold selectivity against gpIIbIIIa.

Ginkgolide K induces protective autophagy through the AMPK/mTOR/ULK1 signalling pathway. It possesses neuroprotective activity.

Pemetrexed disodium treats lung cancer/mesothelioma; may cause moderate serum enzyme elevation, rarely acute liver injury.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM).

Entinostat (MS-275) is an HDAC class I with oral activity. Entinostat has antitumor activity. Cost-effective and quality-assured.

Bergapten (5-Methoxypsoralen), a psoralen, inhibits cell replication.

LAQ824 (Dacinostat (NVP-LAQ824)) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter.

Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β. Luminespib has antitumor activity. Cost-effective and quality-assured.

Leonurine hydrochloride (SCM-198 hydrochloride) , a major alkaloid compound extracted from Leonurus japonicas Houtt.

Isobavachalcone (Corylifolinin) is a chalcone constituent of Angelica keiskei, has potent anti-inflammatory activity, possible can ameliorate neuronal injury in

AMDE-1, an autophagy modulator, triggers Atg5-dependent autophagy, recruits Atg16, and induces LC3 lipidation.

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM).

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) (PIK-III analogue) is a potent and selective inhibitor of VPS34( IC50 : 15 nM)

Trifarotene (CD5789) is a RARγ agonist, 65x more selective than RARα and 16x than RARβ, with EC50 of 7.7 nM.

CCT128930 hydrochloride: Potent AKT inhibitor (IC50=6 nM), 28x selective over PKA, 20x over p70S6K, induces cell cycle arrest & DNA damage.

Dexamethasone: a glucocorticoid agonist; modulates IL receptors; reduces inflammatory miRNA-155 exosomes in macrophage responses.

Deoxypodophyllotoxin is cytotoxic, antineoplastic, anti-tumor, anti-angiogenic, antiviral, and anti-inflammatory.

Mefloquine hydrochloride (Mefloquin hydrochloride) is a quinoline derivative used for the prevention and therapy of P. falciparum malaria.

SLF is a synthetic ligand for FKBP12 and increases Ca2+ efflux and protein synthesis.

Trifluoperazine dihydrochloride (SKF5019) is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.

Calcineurin substrate acetate is from the regulatory RII subunit of cAMP-dependent protein kinase.

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability.

Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.

Cysteamine hydrochloride (Thioethanolamine Hydrochloride) is an agent for the treatment of nephropathic cystinosis and an antioxidant.

AICAR (Acadesine) 是一种AMPK 激活剂,引起ZMP积累,模拟AMP对AMPK和AMPKK的刺激作用,常用于糖尿病,心脑血管疾病以及肿瘤相关研究。

DL-Selenomethionine (SeMet) is a selenium analog of methionine, substituting sulfur with selenium, and can replace methionine in proteins.

UNC0638 inhibits G9a and GLP lysine methyltransferases with IC50 <15 nM and 19 nM, respectively, showing high selectivity.

Mefloquine (Ro 215998), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor.

Atorvastatin hemicalcium salt (Atorvastatin Calcium) is an orally HMG-CoA reductase inhibitor that lowers cholesterol. Cost-effective and quality-assured.

Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FKBP to form a complex.

Berberine chloride (Natural Yellow 18) is an alkaloid from Hydrastis canadensis L., Berberidaceae, and used orally for various fungal and parasitic infections.

(1E,6E)-Bis(demethoxy)curcumin (Curcumin III) is a natural demethoxy derivative of curcumin,with anti-inflammatory and anti-cancer activities.

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w. ABT-737 exhibits antitumor activity and anti-aging activity. Cost-effective and quality-assured.

D-CopA3 is an inhibitor of MDM2 and an activator of the p53 signaling pathway. It exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO with IC50 values of 15-18 μM and induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of the cell cycle inhibitor protein p21Cip1/Waf1, enhances mucosal barrier function, and reduces infiltration of inflammatory mediators. It shows anti-inflammatory properties in mouse models of acute enteritis induced by C. difficile toxin A and chronic colitis induced by DSS. Additionally, D-CopA3 demonstrates antitumor activity in a mouse HCT-116 xenograft model.

6-Mercaptopurine (6-MP) is an antimetabolite antineoplastic agent with immunosuppressant properties.

Nocodazole: synthetic microtubule polymerization blocker, also impedes Abl with low IC50; binds to beta-tubulin.

Penfluridol (TLP-607) is a highly potent antipsychotic.

Scriptaid (GCK1026) is an inhibitor of HDAC, and has a greater effect on acetylated H4 than H3.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer.

Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.

Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.

Nitroprusside disodium dihydrate (Sodium Nitroprusside Dihydrate) is a potent vasodilator working through releasing NO spontaneously in blood.

Dimethyl fumarate (DMF) is an orally Nrf2 activator. Dimethyl fumarate has antimicrobial and anti-inflammatory activities. Cost-effective and quality-assured.

Letrozole (CGS 20267) is an Aromatase Inhibitor. The mechanism of action of letrozole is as an Aromatase Inhibitor.

MRT68921 dihydrochloride is a potent ULK1 and ULK2 inhibitor (IC50 of 2.9 nM and 1.1 nM, respectively).

Eprenetapopt (PRIMA-1Met) restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells.