ceramidase

Ceranib-2 (3-[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]-4-phenyl-1H-quinolin-2-one) 是一种神经酰胺酶抑制剂，在 SKOV3 细胞中的 IC50 为 28 μM。 Ceranib-2 降低鞘氨醇和 S1P 的水平，诱导细胞凋亡并表现出抗癌活性。

ARN14974 是一种有效的全身活性的胞内酸性神经酰胺酶抑制剂 (IC50=79 nM)，是一种苯并恶唑酮甲酰胺化合物。

D-erythro-MAPP (D-e-MAPP) 是神经酰胺酶抑制剂，是一种神经酰胺类似物，具有潜在的抗癌活性。

Acid Ceramidase-IN-1 是一种可口服且具有良好的脑渗透性的酸性神经酰胺酶 (AC, ASAH-1) 抑制剂。Acid Ceramidase-IN-1 可用于研究神经系统疾病。

Acid Ceramidase-IN-2（compound 1）是一款针对酸性神经酰胺酶（ceramidase）的抑制剂，显示出抗增殖及细胞活性抑制的潜力。有研究表明，该化合物在前列腺癌细胞中可阻止人酸性神经酰胺酶的过度表达，从而揭示了其潜在的抗肿瘤能力。此外，Acid Ceramidase-IN-2被三种α-酮酰胺：GT85、GT98和GT99在体外有效抑制其水解作用。

Ceranib1 是一种神经酰胺酶 (ceramidase) 抑制剂， 能抑制细胞神经酰胺酶对外源性神经酰胺类似物的活性，诱导多种神经酰胺物质的积累，降低鞘氨醇和 S1P 水平。Ceranib1 能抑制细胞卵巢癌细胞增殖。

LCL521 能抑制溶酶体酸性鞘磷脂酶（ASMase）。LCL521 是一种酸性神经酰胺酶(ACDase)抑制剂。

Endoglycoceramidase II (EGCase II) 是一种能从糖鞘脂的神经酰胺部分释放完整聚糖的内切-β-葡萄糖苷酶。该酶专门催化多种糖鞘脂中寡糖与神经酰胺之间的 β-糖苷键的水解反应。

Endoglycoceramidase I (EGCase I)为糖苷酶，广泛应用于生化研究。该酶具有催化转糖基化反应的功能，能将GSL的糖组分高效转移至多种1-烷醇的伯羟基。

Galactosylceramidase 参与半乳糖神经酰胺在溶酶体中的代谢，并可用于克拉伯病的研究。

Glucocerebrosidase (Glucosylceramidase; GBA) 是溶酶体内的酶，负责催化GC中的β-糖苷键裂解，从而生成葡萄糖和神经酰胺。

Sinbaglustat (OGT2378) (OGT2378) 是葡萄糖神经酰胺合成酶 (GCS) 和非溶酶体葡萄糖神经酰胺酶 (GBA2) 的双重抑制剂。Sinbaglustat 是一种可透过血脑屏障的的口服N-烷基亚氨基糖。Sinbaglustat 可用于治疗溶酶体贮积症和研究溶酶体功能障碍相关的中枢神经退行性疾病。

Carmofur (HCFU) 是 5-氟尿嘧啶的衍生物，是一种抗肿瘤药物。它是一种酸性神经酰胺酶抑制剂，用于治疗乳腺癌和结直肠癌。它抑制 SARS-CoV-2主要蛋白酶，还抑制 Vero E6 细胞 SARS-CoV-2，EC50为 24.3 μM。

LCL521 dihydrochloride is a compound that functions as an inhibitor of both acid ceramidase (ACDase) and lysosomal acid sphingomyelinase (ASMase).

Antifungalagent 117 是一种双吡唑羧酰胺衍生物，展现出对抗真菌 Sclerotinia sclerotiorum 的活性，其EC50值达11.58 mg L。该化合物通过提高细胞膜通透性，引起细胞内外渗透压的失衡；同时通过促进活性氧 (ROS) 的累积，对细胞膜进行氧化破坏，导致细胞内容物外泄，最终诱导细胞死亡。RNA 测序分析揭示，Antifungalagent 117 通过下调过氧化氢酶基因及上调中性酰胺酶基因，破坏细胞膜结构，加速鞘脂类代谢和细胞死亡过程。此化合物因其在植物保护和抗真菌感染方面显示的应用潜力而被重视。

D-NMAPPD ((1R,2R)-B13) 是一种酸性神经酰胺酶抑制剂，也是神经酰胺类似物，具有潜在的抗增殖活性，可调节人黑色素瘤细胞中神经酰胺信号传导。D-NMAPPD 可用于研究结肠癌。

C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the 20S proteasome in HT-29 and HCT116, but not RIE-1, cells. It reduces tumor growth and increases C16, C18, C20, and C24 ceramide levels in tumor tissue in an HT-29 mouse xenograft model when administered at doses of 1.25, 2.5, and 5 mg/kg for five days. |1. García-Barros, M., Coant, N., Kawamori, T., et al. Role of neutral ceramidase in colon cancer. FASEB J. 30(12), 4159-4171 (2016).

ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme). It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide and C16 ceramide in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 μM, respectively).

C18 D-threoCeramide (d18:1 18:0) is a synthetic ceramide and stereoisomer of C18 ceramide .1It inhibits rat brain mitochondrial ceramidase (mt-CDase) with an IC50value of 16.6 μM.2[Matreya, LLC. Catalog No. 1855] 1.Koolath, S., Murai, Y., Suga, Y., et al.Chiral combinatorial preparation and biological evaluation of unique ceramides for inhibition of sphingomyelin synthaseChirality32(3)308-313(2019) 2.Usta, J., El Bawab, S., Roddy, P., et al.Structural requirements of ceramide and sphingosine based inhibitors of mitochondrial ceramidaseBiochemistry40(32)9657-9668(2001)

C18 L-threo Ceramide is a synthetic ceramide and stereoisomer of C18 ceramide that has been used for structural characterization of natural sphingolipids. It inhibits rat brain mitochondrial ceramidase (mt-CDase) with an IC50 value of 0.21 mol% (16.8 μM).

SABRAC inhibits acid ceramidase in PC3 MC metastatic prostate cancer cells (IC50 = <1 µM), as well as induces accumulation of ceramides in the same cells.

C16-Urea-Ceramide s a neutral ceramidase (nCDase) inhibitor. It is a bioactive ceramide.

SOCLAC, a derivative of the acid ceramidase inhibitor SABRAC, functions as an irreversible inhibitor of acid ceramidase with an inhibition constant (Ki) of 40.2 nM.

SOBRAC, a derivative of the acid ceramidase inhibitor SABRAC, acts as an irreversible inhibitor of acid ceramidase (Ki= 29.7 nM).