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24

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16777	ROC-325	Apoptosis; Autophagy	Apoptosis; Autophagy
	ROC-325 是一种有效的口服活性自噬抑制剂，具有抗癌活性。 ROC-325 诱导肾细胞癌凋亡并表现出良好的特异性。
T1885	Siramesine hydrochloride Lu 28-179 hydrochloride,西拉美新盐酸盐	Ferroptosis; Sigma receptor; lysosomal autophagy	Apoptosis; Autophagy; GPCR/G Protein
	Siramesine hydrochloride (Lu 28-179 hydrochloride) 是一种选择性 sigma-2 受体激动剂，可引发 Y 细胞的细胞死亡并在体内表现出有效的抗癌活性。Siramesine 对 sigma-2 受体具有亚纳摩尔亲和力，并且对 sigma-2 受体的选择性是 sigma-1 受体的 140 倍。
T4620	Siramesine 西拉美新,Lu 28-179	Sigma receptor	GPCR/G Protein
	Siramesine (Lu 28-179) 是sigma-2受体激动剂，通过线粒体的不稳定溶酶体触发细胞死亡，有强大的抗癌活性。它对 sigma-2 受体具有亚纳摩尔亲和力，IC50为 0.12 nM。它对 sigma-2 受体的选择性是 sigma-1 受体的 140倍，IC50为 17 nM。
T60036	ML-SA5	Autophagy	Autophagy
	ML-SA5 是一种 MCOLN1 激动剂，通过扰乱自噬体和溶酶体之间的融合来阻止自噬通量。
T11142	EACC	Autophagy	Autophagy
	EACC 是自噬的可逆抑制剂，可阻断自噬通量。它对自噬体特异性的 SNARE Stx17 易位具有选择性抑制作用，从而阻止自噬体与溶酶体的融合。
T77945	TriGalNAc CBz	LYTACs	PROTAC
	TriGalNAc CBz 为 GalNAc 衍生物。作为一种 ASGPR 配体，TriGalNAc CBz 在 mRNA 药物递送及LYTAC研究中靶向溶酶体。
T77553	MHI-148 IR-808
	MHI-148 是一种具有肿瘤靶向性的近红外七甲氨酸菁染料，可用于检测、诊断和研究癌症。MHI-148 可被肿瘤细胞的溶酶体和线粒体吸收并积累，但在正常细胞的溶酶体和线粒体不吸收。
T1908	MHY1485	mTOR; Autophagy	Autophagy; PI3K/Akt/mTOR signaling
	MHY1485 是一种 mTOR 激活剂。它通过抑制自噬体和溶酶体之间的融合来抑制自噬过程，导致 LC3II 蛋白的积累和自噬体增大。
T21992	Vacuolin-1	PI3K; Autophagy	Autophagy; PI3K/Akt/mTOR signaling
	Vacuolin-1 是一种细胞渗透性抑制剂，可抑制 Ca2+ 依赖性溶酶体与细胞膜的融合。它通过抑制溶酶体内容物的释放起作用。它是一种有效的选择性 PIKfyve 抑制剂，通过损害溶酶体成熟来抑制晚期自噬。
T37885	1-Dodecylimidazole	Antifungal	Microbiology/Virology
	1-Dodecylimidazole 是溶酶体活性洗涤剂。1-Dodecylimidazole 通过在溶酶体中的酸依赖性积累、溶酶体膜的破坏和半胱氨酸蛋白酶释放到细胞质中而导致细胞死亡。它显示出降胆固醇和广谱抗真菌活性。
T33674	NIM-7 NIM7
	NIM-7 is a fluorescent probe, allowing lipid droplets and lysosomes to be labelled simultaneously and with high specificity, being visualized readily through yellow and red fluorescence, using different excitation and detection channels.
T39855	LysoTracker Red LysoTracker Red DND-99
	LysoTracker Red (LysoTracker Red DND-99) is a paraformaldehyde fixable probe that concentrates into acidic compartments of cells and tissues. LysoTracker Red is an indicator of cell death in a manner similar to other standard assays (Annexin, terminal dUTP nick end labeling, Nile blue sulfate, neutral red, and acridine orange). LysoTracker Red is a marker for late endosomes and lysosomes.
T35922	NAADP (sodium salt)
	Nicotinic acid adenine dinucleotide phosphate (NAADP) is a secondary messenger that induces calcium mobilization. It induces calcium release from endosomes and lysosomes via two-pore channel 2 (TPC2) and TPC1, which then stimulates large-scale calcium release from granules and the endoplasmic reticulum mediated by type 1 ryanodine receptors (RyR2s), RyR3s, and inositol-(1,4,5)-triphosphate receptors (IP3Rs). NAADP induces calcium mobilization in sea urchin and starfish eggs post fertilization to...
T61328	CO delivery molecule 1
	CO delivery molecule 1 (compound 4) exhibits subcellular localization in the endoplasmic reticulum, mitochondria, and lysosomes. Such localization leads to the manifestation of CO-induced toxicity effects. Notably, the anti-inflammatory properties of CO delivery molecule 1, quantified through TNF-α suppression, are evident at nanomolar concentrations even without CO release. Furthermore, visible-light-induced CO release further enhances its anti-inflammatory effects [1].
T78371	Ac2-26 ammonium
	Ac2-26 ammonium是一种具抗炎作用的annexin 1 N末端肽。该化合物能够通过伴侣介导的自噬(CMA)机制降低溶酶体中的IKKβ蛋白含量，从而改善肺缺血再灌注损伤，并在哮喘大鼠模型中抑制气道炎症以及高反应性的表现。
T79556	NDBM	Autophagy	Autophagy
	NDBM为一种结合Pim-1 kinase的肿瘤特异性探针，具备释放强荧光及细胞毒性，用于筛选及杀伤肿瘤细胞。该化合物特异性地靶向溶酶体并对pH值具有高度敏感性，适用于监测自噬(autophagy)过程及细胞内环境在外部刺激下的pH变化。
T36370	4-Methylumbelliferyl-α-L-Iduronide (free acid)
	4-Methylumbelliferyl-α-L-iduronide (free acid) is a fluorogenic substrate for α-L-iduronidase, an enzyme found in cell lysosomes that is involved in the degradation of glycosaminoglycans such as dermatan sulfate and heparin sulfate. 4-Methylumbelliferyl-α-L-iduronide is cleaved by α-L-iduronidase to release the fluorescent moiety 4-methylumbelliferyl (4-MU). 4-MU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high (7.12-10.3) pH, respectively, and an...
T35930	Ganglioside GM2 Mixture (sodium salt)
	Ganglioside GM2 is a glycosphingolipid component of cellular membranes, primarily the plasma membrane. Levels of ganglioside GM2 are elevated in the brain of patients with Sandhoff disease, as well as feline and mouse models of the disease. Ganglioside GM2 accumulates in the lysosomes of individuals with Tay-Sachs disease and GM2-activator deficiency, as well as in the CNS of patients with and animal models of mucopolysaccharide storage disorders and Niemann-Pick disease types A, C1, and C2. Gan...
T73550	CUR5g
	CUR5g 是一种有效的自噬 (autophagy) 抑制剂。CUR5g 通过阻断自噬体-溶酶体融合选择性地抑制癌细胞中的自噬体降解。CUR5g 通过依赖 UVRAG 的机制阻止 STX17 募集到自噬体，导致自噬体无法与溶酶体融合。CUR5g 可提高顺铂 (Cisplatin) 在体外和体内对 A549 细胞的抗癌作用。
T77876	Py-MAA-Val-Cit-PAB-MMAE AAJ8D6-PY-Val-Cit-MMAE
	Py-MAA-Val-Cit-PAB-MMAE (AAJ8D6-PY-Val-Cit-MMAE) 是一款ADC Linker，专用于合成抗体药物偶联物Zapadcine-3a (ADC)。Zapadcine-3a 对抗多种肿瘤表现出高效的活性，其作用机理为定位TRAILR2并通过肿瘤细胞内的溶酶体被摄取，进而针对性释放致死的小分子，从而特异性消灭TRAILR2阳性的肿瘤细胞，并能够有效地治愈肿瘤。
T77186	Zilovertamab vedotin
	Zilovertamab vedotin (VLS-101) 是一种抗体-活性分子偶联物 (ADC), 主要由人源化单克隆抗体 zilovertamab 和单甲基 vedotin 组成的抗微管细胞毒素。该药物通过与肿瘤细胞表面的ROR1结合, 触发快速内化及向溶酶体的转运, 进而裂解释放单甲基 vedotin, 诱导细胞凋亡。适用于癌症的研究领域。
T77131	Clervonafusp alfa
	Clervonafusp alfa (VAL-1221) 作为一种融合蛋白，针对胞浆及溶酶体糖原进行靶向。该化合物结合了穿透细胞的抗体Fab部分与重组人酸性葡萄糖苷酶 (rhGAA)，通过核苷转运体ENT-2进入细胞质，再利用甘露糖-6-磷酸受体(M6PRs)导向溶酶体。主要应用于晚发型庞贝病的研究领域。
T36805	TPC2-A1-N TPC2-A1-N
	TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2 through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner[1].
T36806	TPC2-A1-P TPC2-A1-P
	TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na2+ mobilisation from TPC2 than TPC-A1-N . TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells[1][2][3]. Two-pore channels (TPC1-3) are ancient members of the voltage-gated ion channel superfamily. TPCs are expressed throughout the en...

化合物

Cat.No: T16777

Target: Apoptosis, Autophagy

Siramesine hydrochloride

Cat.No: T1885

Synonym: Lu 28-179 hydrochloride,西拉美新盐酸盐

Target: Ferroptosis, Sigma receptor, lysosomal autophagy

Cat.No: T4620

Synonym: 西拉美新,Lu 28-179

Target: Sigma receptor

Cat.No: T60036

Target: Autophagy

Cat.No: T11142

Target: Autophagy

Cat.No: T77945

Target: LYTACs

Cat.No: T77553

Synonym: IR-808

Cat.No: T1908

Target: mTOR, Autophagy

Cat.No: T21992

Target: PI3K, Autophagy

1-Dodecylimidazole

Cat.No: T37885

Target: Antifungal

Cat.No: T33674

Synonym: NIM7

LysoTracker Red

Cat.No: T39855

Synonym: LysoTracker Red DND-99

NAADP (sodium salt)

Cat.No: T35922

CO delivery molecule 1

Cat.No: T61328

Ac2-26 ammonium

Cat.No: T78371

Cat.No: T79556

Target: Autophagy

4-Methylumbelliferyl-α-L-Iduronide (free acid)

Cat.No: T36370

Ganglioside GM2 Mixture (sodium salt)

Cat.No: T35930

Cat.No: T73550

Py-MAA-Val-Cit-PAB-MMAE

Cat.No: T77876

Synonym: AAJ8D6-PY-Val-Cit-MMAE

Zilovertamab vedotin

Cat.No: T77186

Clervonafusp alfa

Cat.No: T77131

Cat.No: T36805

Synonym: TPC2-A1-N

Cat.No: T36806

Synonym: TPC2-A1-P

Cat. No.	Product Name	Target	Signaling Pathways
T6564	Leupeptin Hemisulfate 亮肽素	Serine Protease; Cysteine Protease	Proteases/Proteasome
	Leupeptin hemisulfate 是一种蛋白酶抑制剂，具有细胞膜渗透性、可逆性、竞争性和口服活性。Leupeptin hemisulfate 可以抑制 Cathepsin B、Cathepsin H、Cathepsin L 的活性，阻断两性溶酶体的融合。Leupeptin hemisulfate 还具有抗炎活性。
T6740	Bafilomycin A1 巴佛洛霉素A1,巴佛洛霉素 A1	Apoptosis; Proton pump; Antibacterial; Antibiotic; Autophagy	Apoptosis; Autophagy; Membrane transporter/Ion channel; Microbiology/Virology
	Bafilomycin A1 属于大环内酯类抗生素，是一种 V-ATPase (IC50=0.44 nM)，具有特异性和可逆性。Bafilomycin A1 是自噬晚期阶段抑制剂，阻断自噬体与溶酶体的融合。Bafilomycin A1 也诱导凋亡。

天然产物

Leupeptin Hemisulfate

Cat.No: T6564

Synonym: 亮肽素

Target: Serine Protease, Cysteine Protease

Cat.No: T6740

Synonym: 巴佛洛霉素A1,巴佛洛霉素 A1

Target: Apoptosis, Proton pump, Antibacterial, Antibiotic, Autophagy

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