Autophagy

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

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.

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.

SJFα (SJF alpha) degrades p38α and p38δ and can be used in cancer research.

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.

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

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.

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.

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

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.

Tricyclic cytosine (tC) is a fluorescent analog of cytosine designed for RNA imaging within live cells, facilitating the study of RNA synthesis, degradation,

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].

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].

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

Peptide R, a cyclic CXCR4 antagonist, remodels tumor stroma, aiding cancer research.

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

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

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

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.

Zn-DPA-maytansinoid 1 targets checkpoints, shrinks tumors, and heats TME.

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

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

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

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

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

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

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

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

Cytochalasin E, from Aspergillus, disrupts actin, inhibits angiogenesis, and halts tumor growth.

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

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

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.

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

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

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

Vimnerixin (AZD4721) is an orally administered CXCR2 antagonist for inflammation studies.

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

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.

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

Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II

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

T140, a Polyphemusin II-derived peptide, inhibits HIV-1 entry and blocks anti-CXCR4 antibody (12G5) binding.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

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

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

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

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

Cy3-dCTP, a fluorescent cyanine-dye-labeled nucleotide triphosphate, serves as a DNA imaging probe.