c 75

C75 是一种合成脂肪酸合酶 (FASN) 抑制剂，可抑制前列腺癌细胞 PC3 (IC50: 35 μM)。C75 增加 CPT1 活性，降低 DIO。

trans-C75 ((±)-C75) 是一种 C75 的对映异构体。其中 C75 是一种脂肪酸合成酶 (FASN) 的抑制剂。

Cis-C75是一种含有羧酸的五元氧杂环衍生物，可用于生物化学实验和药物合成研究。

SP600125 (JNK Inhibitor II) 是一种 JNK 抑制剂，抑制 JNK1、JNK2 和 JNK3 (IC50=40/40/90 nM)，具有口服有效性、可逆性和 ATP 竞争性。SP600125 是一种有效的铁死亡抑制剂,可以抑制自噬，诱导凋亡。

Sulfinpyrazone (NSC-75925) 是一种口服有效的尿酸剂，具有抗血栓和血小板抑制作用。它可作用于慢性和间歇性痛风性关节炎。

Trifluridine (NSC-75520) 是一种氟化胸苷类似物，具有潜在的抗肿瘤活性，还具有抗病毒活性。它掺入 DNA 并抑制胸苷酸合酶，从而抑制 DNA 合成、抑制蛋白质合成和细胞凋亡。

SC-75416 是一种选择性COX-2抑制剂，可用于研究疼痛。

LDC7559 通过在晚期阻断中性粒细胞胞外陷阱 (NET)来抑制gasdermin D (GSDMD)。

Odapipam is a selective and high affinity antagonist of benzazepine dopamine D1 receptor (Kd of 0.18 nM).

GANT 58 (NSC-75503) 是GLI 拮抗剂，能够抑制 GLI1 诱导的转录，其IC50=5 μM。

Pentaerythritol diacrolein acetal is an agent of biochemical.

NSC756093 可能抑制 GBP1:PIM1 相互作用。 NSC756093 可用于卵巢癌研究。

C.I. 62100 is a biochemical.

Purine (7H-Imidazo(4,5-d)pyrimidine) 是内源性代谢产物的一种。

SC75741 是NF-κB 抑制剂，对p65的IC50为 200 nM。它可阻断流感病毒复制。它通过损害NF-κB 亚基 p65 的 DNA 结合，导致细胞因子，趋化因子和促凋亡因子的表达降低，抑制 caspase 活化和阻断 caspase 介导的病毒核糖核蛋白的核输出。

Timelotem 是一种 1,2-并环1,4-苯二氮卓类药物，展现出明显的抗精神病特性。通过增强神经递质 γ-氨基丁酸 (GABA) 的作用，Timelotem 具有镇静、抗焦虑和抗惊厥等效果。Timelotem 可用于精神分裂症及其他精神障碍的研究。

Isoliquiritigenin (ISL) 属于黄酮类天然产物，抑制流感病毒复制 (EC50=24.7 μM)，也抑制 aldose reductase 的活性 (IC50=320 nM)。Isoliquiritigenin 具有抗肿瘤的活性。

CHMFL-ABL/KIT-155 is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s: 46 nM/75 nM). It arrests cell cycle progression and induces apoptosis.

PPO-IN-17 (Compound 6R) 是一种原卟啉原 IX 氧化酶（PPO）抑制剂，其能够抑制烟草 PPO（NtPPO），Ki 为 30.34 nM。PPO-IN-17 展现除草效果，在浓度为 37.5 g/hm² 时，对稗草（E. crus-galli）、狐尾草（D. sanguinalis）、苜蓿（M. sativa）及加拿大苍耳（C. canadensis）的抑制率超过95%。该化合物对水稻（浓度为 75 g/hm²）和蜜蜂（浓度为 6400 mg/kg）无毒性。

STAT-3/c-Src-IN-1 (Compound 12d) 是一种双重抑制剂，靶向STAT-3 (IC50=0.844 μM) 和c-Src (IC50=0.268 μM)。它能够阻止肿瘤细胞的增殖、迁移和血管生成信号通路。该化合物对黑色素瘤 (SK-MEL-2) 和中枢神经系统癌症 (SNB-75) 细胞系显示出强效的抗增殖活性 (GI50=-5.75 μM 和 -5.63 μM)，通过诱导G0/G1和G2/M期细胞周期停滞，使肿瘤细胞凋亡。STAT-3/c-Src-IN-1 可能在黑色素瘤和胶质母细胞瘤的研究中具有应用潜力。

Masitinib (AB1010) 是生物口服可利用的选择性 c-Kit 抑制剂 (对于人重组c-Kit，IC50=200 nM)，它还抑制PDGFRα/β(IC50s=540/800 nM)，Lyn(对 LynB 的IC50=510 nM)，Lck，较小程度上抑制FGFR3和FAK。它有抗增殖，促凋亡活性，且毒性低。

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)

Arecaidine propargyl ester is an agonist of M2muscarinic acetylcholine receptors (mAChRs).1It selectively binds to M2over M1, M3, M4, and M5mAChRs in CHO cells expressing the human receptors (Kis = 0.0871, 1.23, 0.851, 0.977, and 0.933 μM, respectively). Arecaidine propargyl ester induces contractions in isolated guinea pig atrium (pD2= 8.67). It induces apoptosis and the production of reactive oxygen species (ROS) in U87 and U251 glioblastoma cells when used at a concentration of 100 μM.2Arecaidine propargyl ester decreases mean arterial blood pressure in normotensive cats (ED25= 1.9 nmol/kg).3It is toxic to house flies (Musca) when administered at a dose of 75 μg/fly.4 1.Scapecchi, S., Matucci, R., Bellucci, C., et al.Highly chiral muscarinic ligands: the discovery of (2S,2’R,3’S,5’R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonistJ. Med. Chem.49(6)1925-1931(2006) 2.Di Bari, M., Tombolillo, B., Conte, C., et al.Cytotoxic and genotoxic effects mediated by M2 muscarinic receptor activation in human glioblastoma cellsNeurochem. Int.90261-270(2015) 3.Porsius, A.J., and Van Zwieten, P.A.Central action of some cholinergic drugs (arecaidine esters) and nicotine on blood pressure and heart rate of catsProg. Brain Res.47131-135(1977) 4.Honda, H., Tomizawa, M., and Casida, J.E.Insect muscarinic acetylcholine receptor: Pharmacological and toxicological profiles of antagonists and agonistsJ. Agric. Food Chem.55(6)2276-2281(2007)