Autophagy

<p>SG31 is a potent activator of autophagy, exerting its effects through the AMPK/ULK1-dependent pathway.</p>

<p>Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) is a proton pump inhibitor drug, used for short-term treatment of erosion and ulceration of the esophagus</p>

<p>CXM102 is an activator of autophagy. This compound induces autophagy in aged BMSCs, rejuvenating them and promoting their preferential differentiation into osteoblasts. CXM102 enhances the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. In middle-aged male mice, it stimulates bone anabolic metabolism, reduces marrow adipocytes, delays bone loss, lowers serum inflammation levels, reduces organ fibrosis, and extends lifespan.</p>

<p>Myosin light chain kinase inhibitor; IC50=50 nM; 4000x more selective over CaM kinase II; no PKA inhibition; cell-permeable.</p>

<p>Autophagy/REV-ERB-IN-1 hydrochloride (Compound 24) is a dual inhibitor of autophagy and REV-ERB with anticancer properties. It enhances the efficacy of autophagy blockade and increases cytotoxicity against cancer cells. Autophagy/REV-ERB-IN-1 (hydrochloride) is applicable in melanoma research.</p>

<p>(S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-OH is a conjugate of an E3 ligase ligand and a linker (E3LigaseLigand-Linker Conjugates), consisting of Thalidomide and the corresponding Linker. It functions as a Cereblon ligand to recruit the CRBN protein and serves as a crucial intermediate for synthesizing complete PROTAC molecules.</p>

<p>Indomethacin-D4 is a deuterium labeled Indomethacin.</p>

<p>ALX40-4C is a small peptide inhibitor of the chemokine receptor CXCR4 that can inhibit X4 strains of HIV-1.</p>

<p>PDEδ autophagic degrader 1 (compound 12c) is an autophagosome-tethering compound (ATTEC) and a potent autophagic degrader of PDEδ. This compound effectively reduces PDEδ protein levels through lysosome-mediated autophagy without affecting PDEδ mRNA expression. Additionally, PDEδ autophagic degrader 1 inhibits the growth of KRAS mutant pancreatic cancer cells.</p>

<p>(S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-C2-OH is a conjugate combining an E3 ligase ligand with a linker (E3LigaseLigand-Linker Conjugates), composed of Thalidomide and the corresponding Linker. This compound functions as a Cereblon ligand, recruiting the CRBN protein and serving as a crucial intermediate in the synthesis of complete PROTAC molecules.</p>

<p>CXCL8 (54-72) is a C-terminal peptide segment of the chemokine CXCL8. This peptide features a long, highly positively charged C-terminal region that interacts with the negative charges on glycosaminoglycans (GAG) to facilitate binding. CXCL8 (54-72) inhibits neutrophil adhesion and migration, as well as adhesion to endothelial cells. It is useful in studying the role of chemokines in inflammatory responses.</p>

<p>(S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-CH2-COO-C(CH3)3 is an E3 ligase ligand-linker conjugate (E3LigaseLigand-Linker Conjugates) composed of thalidomide and its corresponding linker. This compound functions as a Cereblon ligand, facilitating the recruitment of CRBN protein, and serves as a crucial intermediate in the synthesis of complete PROTAC molecules.</p>

<p>(1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of an E3 ligase ligand and linker (E3LigaseLigand-Linker Conjugates), composed of Thalidomide and the corresponding linker. It acts as a Cereblon ligand, recruiting CRBN proteins, and serves as a crucial intermediate in the synthesis of complete PROTAC molecules.</p>

<p>Atorvastatin Sodium (Lipitor) is a competitive inhibitor of HMG-CoA reductase and increases the expression of low density lipoprotein (LDL) receptors on</p>

<p>CCR7 antagonist1 (30c) functions as a dual antagonist, targeting CXCR2 with an IC50 of 11.02 μM and CCR7 with an IC50 of 0.43 μM.</p>

<p>RCP168 is a highly selective and potent CXCR4 receptor antagonist with an IC50 of 5 nM. It exhibits superior capacity to inhibit HIV-1 (Human Immunodeficiency Virus type 1) from entering host cells via the CXCR4 receptor compared to natural chemokines. RCP168 suppresses HIV-1 infection by blocking viral binding sites or inducing receptor internalization. It can be utilized in research to study interactions between the CXCR4 receptor and other chemokine receptors.</p>

<p>Alx40-4C trifluoroacetate inhibits CXCR4 and is an APJ antagonist with IC50 of 2.9M.</p>

<p>PF-06835375 is a humanized IgG1 antibody that selectively targets CXCR5 expressed on B cells, Tfh cells, and circulating Tfh-like cells (cTfh). It is applicable for research into systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA).</p>

<p>Antitumor agent-133 (compound 4d) is a bis-santine derivative that demonstrates activity against Huh1 (IC50 = 17.13 μM) and Huh7 (IC50 = 8.27 μM). It induces autophagy and inhibits tumor growth by modulating the levels of the LC3BII, ATG5, and p62 proteins.</p>

<p>ATRA-biotin is a biotin-conjugated form of all-trans retinoic acid (ATRA). It is utilized for the purpose of tracking ATRA within cells or specific tissues.</p>

<p>Tigecycline hydrate: broad-spectrum, glycylcycline antibiotic, bacteriostatic, inhibits protein synthesis, effective against resistant bacteria.</p>

<p>Syntide-2 is a synthetic peptide recognized as a substrate by Ca2+/calmodulin-dependent protein kinase II (CaMKII; Km = 12 µM).</p>

<p>(1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of an E3 ligase ligand and linker (E3LigaseLigand-Linker Conjugates), composed of Thalidomide and the corresponding linker. This compound serves as a Cereblon ligand to recruit CRBN protein and acts as a crucial intermediate in the synthesis of complete PROTAC molecules.</p>

<p>AUTAC1 is a MetAP2-targeted autophagy-mediated degradator (AUTAC) that degrades MetAP2 and FKBP12 proteins and can be used to synthesize PROTAC.</p>

<p>Cabergoline (FCE-21336), an ergot-derived dopamine D2-like agonist, targets D2/D3/5-HT2B, normalizes prolactin, controls pituitary tumors.</p>

<p>MRL828 is a compound that combines a Tau pathology-binding ligand with a guanine group modified by ATTEC technology, allowing it to selectively target aggregated tau proteins for clearance via the autophagy-lysosome pathway (ALP). MRL828 reduces intracellular Tau aggregates and facilitates the secretion of Tau.</p>

<p>Biotin-16-UTP serves as an efficient substrate for RNA polymerase, capable of substituting UTP in vitro transcription reactions to facilitate RNA labeling [1].</p>

<p>Indole-3-glyoxylyl chloride (3-Indoleglyoxylyl chloride) can be used in chemical synthesis, such as bisindolylmaleimide.</p>

<p>LC3B recruiter 2 (34R) is an LC3B recruiting agent incorporated into the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), with a direct binding affinity for LC3B. It connects via a linker to the CDK9 inhibitor SNS-032, creating an ATTEC capable of targeting and degrading the CDK9 and Cyclin T1 complex, while also inhibiting them. Consequently, LC3B recruiter 2 exerts its function through an LC3B-dependent autophagy-lysosome pathway, interfering with the cancer cell cycle progression, thereby demonstrating antitumor activity.</p>

<p>Polyphyllin G (Polyphyllin VII), the the main member of polyphyllin family, shows strong anticancer activity against several carcinomas.</p>

<p>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 &gt; 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.</p>

<p>H1k is an eudistomin Y fluorescent derivative and lysosome-targeted antiproliferative agent that downregulates the expression of cell cycle protein B1.</p>

<p>Acetyl coenzyme A (Acetyl-CoA) is a pivotal molecule connecting multiple cellular metabolic pathways in the tricarboxylic acid cycle, fatty acid synthesis</p>

<p>Fumagilin-105, an autophagy-targeting chimera (AUTOTAC), induces self-oligomerization of p62 and exhibits a DC50 of 0.7 μM against MetAP2 in HEK293 cells.</p>

<p>Autocamtide-2: Selective peptide for CaMKII, a CAMK Ser/Thr kinase.</p>

<p>DB1113 is a bifunctional kinase degrader, targeting ABL1, ABL2, CDK4, MAPKs, and more for disease research.</p>

<p>SQA1 is a derivative of a phthalamide (SQA) and acts as a CCR6 antagonist with a Kd of 250 nM, as well as a CXCR2 inhibitor. It occupies an intracellular pocket that overlaps with the G protein binding site, stabilizing the pocket's closed conformation.</p>

<p>TRAF6 peptide inhibits TRAF6-p62, blocks TrkA ubiquitination, and shows promise for neurological disease research.</p>

<p>Microcolin H, a marine lipopeptide and phosphatidylinositol transfer protein ligand, targets PITPα/β. It enhances the conversion of LC3I to LC3II and decreases p62 levels in cancer cells, inducing autophagy cell death (Autophagy). Furthermore, Microcolin H effectively inhibits tumor growth and exhibits anti-proliferative activity in nude mouse subcutaneous tumor models [1].</p>

<p>PBA-1105b, a longer PEGylated derivative of PBA-1105, is an autophagy-targeting chimeric compound (AUTOTAC) that can induce self-oligomerization of p62. It enhances the autophagic flux of Ub-bound aggregates.</p>

<p>YTK-105 is a ligand targeting autophagy that binds to p62.</p>

<p>Ch55-O-C3-NH2, also known as RAR ligand 1, is a ligand derived from the Ch55 compound that specifically targets RAR.</p>

<p>LC3in-C42 is a covalent inhibitor of LC3A/B and autophagy active within cells. Selectively inhibiting the binding of P62 to LC3A/B both in vitro and at the cellular level, LC3in-C42 functions similarly to D5 and is effective at lower concentrations.</p>

<p>N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with anti-melanoma activity.</p>

<p>Bacilotetrin C analogue is a variant of Bacilotetrin C. It exhibits cytotoxicity against the triple-negative breast cancer cell line MDA-MB-231, with an IC50 of 0.48 μM. This compound induces autophagy (autophagy) in tumor cells and possesses antitumor activity.</p>

<p>Deoxy-thalidomide-Pip-C-PIP-boc, a conjugate of E3 ligase ligand and linker, comprises Thalidomide and the corresponding Linker. It functions as a Cereblon ligand to recruit CRBN protein and acts as a crucial intermediate in synthesizing complete PROTAC molecules.</p>

<p>Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [1].</p>

<p>PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.</p>

<p>Dusquetide TFA (SGX942) is an IDR that modulates immunity by targeting p62, reducing inflammation, and enhancing bacterial clearance.</p>

<p>HDAC6-IN-58 (compound 24c) is a selective HDAC6 inhibitor with IC50 values of 9.5 nM for HDAC6 and 7374.5 nM for HDAC1. It enhances tubulin acetylation, exhibits antiproliferative effects, and induces autophagy (autophagy).</p>

<p>FDW028 is a FUT8 inhibitor with antitumor activity that works by promoting B7-H3 lysosomal degradation through defucosylation and CMA pathways.</p>

<p>cGMP-HTL, an AUTAC, promotes K63-linked mitochondrial ubiquitination with a Cys-S-cGMP tag and target-specific warhead.</p>

<p>Peptide R, a cyclic CXCR4 antagonist, remodels tumor stroma, aiding cancer research.</p>

<p>Flavopiridol (Alvocidib) blocks CDK1/2/4/6 by competing with ATP (IC50 ~40 nM); 7.5x selectivity over CDK7; also inhibits EGFR, PKA. In Phase 1/2 trials.</p>

<p>STO-609 acetate is selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki: 80/15 ng/ml, for CaM-KKα/KKβ); competes for the</p>

<p>Zn-DPA-maytansinoid 1 targets checkpoints, shrinks tumors, and heats TME.</p>

<p>Cy5.5-SE DIPEA is a water-soluble CY dye often used for labeling proteins and antibodies, with simple mixing for conjugation. Store protected from light.</p>

<p>Corydalmine hydrochloride: antifungal, oral analgesic, soothes neuropathic pain by blocking NF-κB/CXCL1/CXCR2.</p>

<p>Fe-TMPyP binds to the prion protein PrP and inhibits misfolding. Fe-TMPyP is also a peroxynitrite decomposition catalyst.</p>

<p>Insecticidal agent 364 is a selective small molecule inhibitor of rapamycin kinase target protein.</p>

<p>Manzamine A hydrochloride: oral beta-carboline inhibiting GSK-3β &amp; CDK-5; blocks autophagy in cancer; antimalarial; fights HSV-1.</p>

<p>CXCR4-IN-3 (compound XVI) is an orally active inhibitor targeting the inflammation-related receptor CXCR4, with an IC50 of 3.2 nM. It exhibits potent anti-chemotactic effects, with an inhibition rate of 79.19±2.33%. Additionally, CXCR4-IN-3 possesses anti-inflammatory properties and can be utilized in research on IBD (inflammatory bowel disease).</p>

<p>Biotin-11-dCTP is a fluorescent dye for DNA labeling [1] .</p>

<p>MRT 67307 dihydrochloride inhibits IKKε/TBK-1, ULK1/2, and blocks autophagy, with IC50s of 160/19, 45/38 nM respectively.</p>

<p>(S)-Sitagliptin phosphate, less active enantiomer, is a potent DPP4 inhibitor with an IC50 of 19 nM.</p>

<p>Autophagy/REV-ERB-IN-1 is a dual inhibitor of autophagy and REV-ERB. It exhibits antitumor activity, with a CC50 value of 2.3 μM in BTB-474 cells.</p>

<p>Clionamine B, an aminosteroid from Cliona celata, enhances autophagy in MCF-7 breast cancer cells.</p>

<p>Tigecycline mesylate is a first-in-class, broad-spectrum antibiotic. It also has activity against antibiotic-resistant organisms.</p>

<p>Hoechst 33342 analog trihydrochloride, an analog of Hoechst 33342, serves as a fluorochrome by binding to the minor groove of DNA, facilitating the</p>

<p>Erlotinib-13C6 (CP-358774-13C6), a 13C-labeled direct EGFR inhibitor, IC50: 2 nM.</p>

<p>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.</p>

<p>Desethylamiodarone HCl, CYP3A product, antiarrhythmic inhibiting K+ channels, IC50 19.1 μM, main amiodarone metabolite.</p>

<p>Compound E1 selectively targets G-quadruplex DNA, fluoresces, enters cells with low toxicity.</p>

<p>Autocamtide-2, an amide, is a selective CaMKII substrate for CAMK family assays at 100 μM.</p>

<p>p62-ZZ Ligand-Linker Conjugate 1 is a conjugate of the p62-ZZ domain ligand and linker. This compound is utilized in the synthesis of AUTOTACVinclozolinM2-2204.</p>

<p>Tetramethylrhodamine-dUTP (TAMRA-dUTP) is used for end-labeling of DNA [1] .</p>

<p>Acridine homodimer (NSC 219743), a blue-green fluorescent dye, binds DNA, preferring AT-rich areas, useful for chromosome banding.</p>

<p>AZD4721, an oral CXCR2 antagonist, may be researched for treating inflammation.</p>

<p>PHTPP-1304, a chimeric autophagy-targeting compound (AUTOTAC) based on PHTPP, induces p62 self-oligomerization and degrades estrogen receptor ERβ (DC50: ~2 nM, HEK293T). Additionally, PHTPP-1304 facilitates the formation of p62+ERβ+ puncta in a dose-dependent manner, influencing autophagic flux.</p>

<p>Cyanine 5 Tyramide is a red dye used in HRP assays and nucleic acid hybridization. Store away from light.</p>

<p>Nictide, a peptide substrate for LRRK2 (leucine-rich repeat protein kinase-2), undergoes phosphorylation by the activated form of LRRK2[G2019S], exhibiting a Km value of 10 μM.</p>

<p>Tigecycline hydrochloride is a first-in-class, broad-spectrum antibiotic. It also has activity against antibiotic-resistant organisms.</p>

<p>Sodium valproate is an anti-epileptic, boosting brain GABA levels and possibly affecting potassium channels for membrane stability.</p>

<p>RK-682 inhibits PTPs, crucial in cell signaling, with IC50s: CD45 (54 μM), VHR (2 μM), and heparanase (17 μM), halting G1/S cell cycle transition.</p>

<p>Desethyl chloroquine (Monodesethylchloroquine) is a major metabolite of Chloroquine which is a TLR inhibitor. Desethyl chloroquine shows antiplasmodic activity.</p>

<p>TSPO Ligand-Linker Conjugates 1: a compound linking TSPO ligands to AUTACs for targeted mitophagy, aiding research in mitochondrial diseases.</p>

<p>Compound A3, an NAMPT degrader, has 0.023 μM IC50 and promotes NAMPT breakdown via autophagy, exhibiting strong anticancer effects.</p>

<p>CX4338 is a CXCL8-mediated chemotaxis inhibitor.</p>

<p>CXCR4 antagonist 1 is a potent inhibitor of the CXCR4 receptor, with notable anti-HIV activity.</p>

<p>BRD4 degrader-5 (Compound 23) is a protein degrader utilizing a hydrophobic tag (HyTag) that targets BRD4 for degradation through endoplasmic reticulum stress and the autophagy-lysosome pathway (DC50 = 24.7 μM). It also inhibits the proliferation of 4T1 cancer cells, with an IC50 of 20.6 μM.</p>

<p>DMTr-4'-CF3-5-Me-U-CED is a dye for oligonucleotide labeling in RNA research.</p>

<p>SHP2-IN-35 (Compound 3f) functions as an inhibitor of SHP2. It exhibits antiproliferative activity in cancer cell lines RKO, SW480, and CT26, with IC50 values of 5.72 μM, 3.71 μM, and 1.42 μM, respectively. SHP2-IN-35 inhibits the PI3K-Akt signaling pathway, regulates the expression of cell cycle-related genes, and induces mitochondrial autophagy (autophagy). Within the tumor microenvironment (TME), SHP2-IN-35 suppresses the expression of certain cytokines and chemokines, thereby modulating tumor progression.</p>

<p>MeCY5-NHS ester (potassium) is a reactive dye optimized for labeling proteins and nucleic acids [1].</p>

<p>(3R,5S)-Fluvastatin, a synthetic HMG-CoA reductase inhibitor (IC50: 8 nM), activates Nrf2 for antioxidant defense.</p>

<p>KRH-3955 hydrochloride is an orally available CXCR4 blocker with IC50 of 0.61 nM and EC50 of 0.3-1.0 nM against X4 HIV-1.</p>

<p>MW-150 hydrochloride is a selective p38α MAPK inhibitor with a 101 nM Ki, offering good CNS penetration and oral bioavailability.</p>

<p>Chlorotris (triphenylphosphine) copper (CuCl(TPP)₃) is a metal complex that targets DNA. Through non-covalent interactions of its copper (I) center, such as groove-binding, it affects DNA function and exhibits inhibitory activity against bacteria, fungi, and tumor cells. Chlorotris (triphenylphosphine) copper holds potential for research as an antimicrobial, antitumor, and antioxidant agent.</p>

<p>Hexidium iodide fluoresces, stains mammalian cells &amp; gram-positive bacteria, and binds to DNA with EDTA. Excitation/emission: ~518/600 nm.</p>

<p>Desfluoro-ezetimibe: a defluorinated ezetimibe impurity; a stable, potent cholesterol blocker and Nrf2 activator.</p>

<p>Cytochalasin E, from Aspergillus, disrupts actin, inhibits angiogenesis, and halts tumor growth.</p>