Autophagy

<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>