lethality

AZD5305 是一种强效、选择性和口服活性 PARP 抑制剂，可用于肿瘤异体移植模型研究。

Syrosingopine 是 MCT1和 MCT4双重抑制剂，对 MCT4 的效力高 60 倍，可防止乳酸和 H+ 流出。Syrosingopine是可口服抗高血压药物，联合二甲双胍具有研究癌症疾病的潜力。

SSJ-183 是一种低毒性和可口服的和抗疟疾药物，对恶性疟原虫的IC50=7.6 nM，高达2000 mg kg po的剂量没有致死性。

Adenosine N1-oxide (1-Oxoadenosine) 是在蜂王浆中发现的腺苷 N1-氧化物，可抑制活化的巨噬细胞分泌炎症介质，并降低脂多糖 (LPS) 诱导的内毒素休克的致死率。

CM-10-18 is a potent inhibitor of ER α-glucosidase. CM-10-18 demonstrated superior in vitro antiviral activity against representative viruses from four viral families causing hemorrhagic fever. CM-10-18 efficiently protected the lethality of dengue virus

3-Acetyldeoxy nivalenol-13C17is intended for use as an internal standard for the quantification of 3-acetyldeoxy nivalenol by GC- or LC-MS. 3-Acetyldeoxy nivalenol is a mycotoxin that has been found inF. graminearum.1In vivo, 3-acetyldeoxy nivalenol (40 mg kg) induces duodenal and splenic cell necrosis, as well as lethality (LD50= 70 mg kg) in mice.2 1.Jiao, F., Kawakami, A., and Nakajima, T.Effects of different carbon sources on trichothecene production and Tri gene expression by Fusarium graminearum in liquid cultureFEMS Microbiol.Lett.285(2)212-219(2008) 2.Schiefer, H.B., Nicholson, S., Kasali, O.B., et al.Pathology of acute 3-acetyldeoxynivalenol toxicity in miceCan. J. Comp. Med.49(3)315-318(1985)

4-deoxy Nivalenol-13C15is intended for use as an internal standard for the quantification of 4-deoxy nivalenol by GC- or LC-MS. 4-deoxy Nivalenol is a trichothecene mycotoxin that has been found inFusarium.1It binds to eukaryotic ribosomes and inhibits protein synthesis in mice when administered at doses ranging from 5 to 25 mg kg. 4-deoxy Nivalenol (0.1 and 0.2 mg kg) induces emesis in pigs and decreases feed consumption in pigs when administered at a dose of 40 ppb in the diet.2It induces lethality in mice (LD50= 46-78 mg kg).34-deoxy Nivalenol has been found inF. graminearum-infected cereal grains such as wheat, barley, and corn. 1.Pestka, J.J., and Smolinski, A.T.Deoxynivalenol: Toxicology and potential effects on humansJ.Toxicol.Environ.Health B.Crit.Rev.8(1)39-69(2005) 2.Forsyth, D.M., Yoshizawa, T., Morooka, N., et al.Emetic and refusal activity of deoxynivalenol to swineAppl. Environ. Microbiol.34(5)547-552(1977) 3.Pestka, J.J.Deoxynivalenol: Mechanisms of action, human exposure, and toxicological relevanceArch. Toxicol.84(9)663-679(2010)

Aflatoxin G1-13C17is intended for use as an internal standard for the quantification of aflatoxin G1by GC- or LC-MS. Aflatoxin G1is a mycotoxin that has been found inA. terricola.1In vivo, aflatoxin G1is lethal to ducklings (LD50= 1.18 mg kg).2It induces hepatocellular carcinoma tumor formation and lethality in rats when administered at doses of 1.4 and 3 mg animal, respectively. Aflatoxin G1also inhibits liver and kidney succinate dehydrogenase and fumarase, as well as kidney cytochrome oxidase, NADH oxidase, α-glycerophosphate dehydrogenase, isocitrate dehydrogenase, and malate dehydrogenase in rats.3 1.Moubasher, A.H., el-Kady, I.A., and Shoriet, A.Toxigenic Aspergilli isolated from different sources in EgyptAnn. Nutr. Aliment.31(4-6)607-615(1977) 2.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins and analogsCancer Res.31(12)1936-1942(1971) 3.Bai, N.J., Pai, M.R., and Venkitasubramanian, T.A.Mitochondrial function in aflatoxin toxicityIndian J. Biochem. Biophys.14(4)347-349(1977)

Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg kg. Nitisinone (3 mg kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (FAH) deficiency in mice when administered to pregnant dams.2It exhibits hepatoprotective effects inFAH- -mice, such as prevention of increases in plasma levels of aspartate serine aminotransferase (AST) and conjugated bilirubin, when administration is continued following birth at a dose of 1 mg kg. Nitisinone (100 μg) decreases urinary excretion of homogentisate and increases urinary excretion of HPPA, HPLA, and 4-hydroxyphenylacetate in a mouse model of alkaptonuria induced by ethylnitrosourea.3Formulations containing nitisinone have been used in the treatment of hereditary tyrosinemia type 1 (HT-1). 1.Ellis, M.K., Whitfield, A.C., Gowans, L.A., et al.Inhibition of 4-hydroxyphenylpyruvate dioxygenase by 2-(2-nitro-4-trifluoromethylbenzoyl)-cyclohexane-1,3-dione and 2-(2-chloro-4-methanesulfonylbenzoyl)-cyclohexane-1,3-dioneToxicol. Appl. Pharmacol.133(1)12-19(1995) 2.Grompe, M., Lindstedt, S., al-Dhalimy, M., et al.Pharmacological correction of neonatal lethal hepatic dysfunction in a murine model of hereditary tyrosinaemia type INat. Genet.10(4)453-460(1995) 3.Suzuki, Y., Oda, K., Yoshikawa, Y., et al.A novel therapeutic trial of homogentisic aciduria in a murine model of alkaptonuriaJ. Hum. Genet.44(2)79-84(1999)

CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bagnolini, G., Milano, D., Manerba, M., et al.Synthetic lethality in pancreatic cancer: Discovery of a new RAD51-BRCA2 small molecule disruptor that inhibits homologous recombination and synergizes with olaparibJ. Med. Chem.63(5)2588-2619(2020)

Diquat dibromide 是一种水溶性除草剂，可快速而深刻的引起全身毒性。Diquat dibromide 可诱导急性肾损伤，具有很高的致死率。

PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC 50 s of 1.9 μM and 0.6 μM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.

Antitubercular agent-19 是一种抗结核剂。Antitubercular agent-19 对 MTB H37Rv 和 MDR-MTB 表现出良好的抗结核效果 (MIC＜0.016 μg ml)。Antitubercular agent-19 在 BALB c 小鼠中表现出较低的细胞毒性和相对较高的急性致死毒性。

Deoxycytidine triphosphate trisodium salt (2'-DEOXYCYTIDINE-5'-TRIPHOSPHATE TRISODI) 是可用于 DNA 合成的核苷三磷酸，可用于实时荧光定量 PCR、cDNA 合成和 DNA 测序。

Endotoxin inhibitor TFA 是一种可以与脂多糖(LPS)的成分脂质A高亲和力结合的合成肽，具有中和LPS毒性、预防LPS引发的细胞因子释放的作用。此外，Endotoxin inhibitor TFA能够有效抑制LPS引起的发热反应，同时具有极低的毒性和致死率。

ATR-IN-23 (Compound 34) 是一种选择性ATR抑制剂，其IC50为 1.5 nM。该化合物对LoVo细胞表现出抗增殖活性，并对HT-29细胞产生合成致死效果，适用于研究DNA损伤反应(DDR)缺陷癌症。

r8 Bid BH3是一种促凋亡的生物活性肽，属于 BCL-2家族 中的“仅具BH3功能域”的亚群，对Bcl-2表达的人类白血病细胞系显示出致死性。作为Bcl-2拮抗剂，它具备治疗癌症的潜力。此外，多聚-D-精氨酸（d-异构体，标记为rrrrrrrr）被融合到Bid BH3肽上，以提高其被细胞摄取的能力。

Ssm Spooky Toxin是从Scolopendra mutilans中分离出的化合物，其特点是有效抑制KCNQ（电压门控钾通道家族7）通道，表现出对血液和呼吸系统的致命毒性。Ssm Spooky Toxin对Kv7.4、Kv1.3和Shal通道的IC50值分别为2.8 μM、5.26 μM和0.1-0.3 M，且能够通过针对T细胞中的KV1.3通道抑制细胞因子的产生，在蜈蚣的循环系统中起着关键作用。

Byssochlamic acid, a mycotoxin identified in the agricultural fungal pathogen B. fulva, exhibits lethality in mice with an LD50 of 94 mg kg.

Spirotetramat is an insecticide that demonstrates efficacy against C. pyrinymphs in vitro (LC50= 6.51-12.53 mg AI L) and achieves a 99.2% mortality rate in C. pyrinymphs within European pear (P. communis) fields 15 days post-application at a dosage of 27 g hectare. Additionally, it reduces embryonic viability and nymph survival in O. insidiosus. Spirotetramat exhibits aquatic toxicity by altering protein levels in organisms, specifically by increasing glutathione peroxidase (GPX) and superoxide dismutase (SOD) levels, decreasing malondialdehyde (MDA) levels, and causing lethality in Chinese toad (B. gargarizans) tadpoles (LC50= 6.98 mg L). Its formulations are utilized in agricultural insect control. Spirotetramat is marketed exclusively for research and analytical applications, formulated for controlled laboratory settings without the availability of bulk sizes.

Cyclo(Pro-Leu) (Cyclo-L-prolyl-L-leucine) 是一种源自海洋的天然产物，具有盐水虾的杀伤力。

N-Acetyl-Ser-Asp-Lys-Pro 通过酶促处理胸腺素 β4 在骨髓细胞中形成。 它抑制多能造血干细胞进入细胞周期的 S 期，并防止小鼠中的 Ara-C 致死性。