hep3b

Triglycidyl isocyanurate (Teroxirone) 是一种三氮烯三环氧化合物，可通过 p53的激活抑制非小细胞肺癌细胞的生长。它诱导细胞凋亡，具有抗血管生成和抗肿瘤活性，用于癌症研究。

Roblitinib (FGF-401) 是一种口服有效的，高选择性的FGFR4抑制剂(IC50:1.9 nM)，具有抗癌作用。

Mollugin (Rubimaillin) 是Rubia cordifolia L.中主要的生物活性成分。它能通过 p38-Smad 信号通路增强 BMP-2 的成骨作用。它通过抑制 TNF-α 诱导的 NF-κB 激活起抗癌疗效。

Regorafenib (BAY 73-4506) 是一种多靶点受体酪氨酸激酶抑制剂，抑制 RET、C-RAF、VEGFR2、c-Kit、VEGFR1 和 PDGFRβ (IC50=1.5 2.5 4.2 7 13 22 nM)，具有口服活性。Regorafenib 具有抗肿瘤和抗血管生成活性。

Regorafenib monohydrate 是一种新型口服多激酶抑制剂，对VEGFR1 2 3、PDGFRβ、Kit、RET 和Raf-1的IC50分别为 13、4.2、46、22、7、1.5 和 2.5 nM。

Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).

Sorafenib (Bay 43-9006) 是一种多激酶抑制剂，抑制 Raf-1、B-Raf、VEGFR2、VEGFR3、VEGFR4、PDGFRβ、FLT3、c-Kit 等 (IC50=6 22 90 15 20 20 57 58 nM)，具有口服活性。Sorafenib 具有抗肿瘤活性，可以诱导细胞自噬和凋亡，也可以激动铁死亡。

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。

Berberine (Umbellatine) 属于生物碱类天然产物，可以激活 AMPK、抑制 DNA 拓扑异构酶、诱导 ROS 生成。Berberine 具有抗肿瘤、抗菌、降血糖、降血脂等生物学活性。

Ribociclib (LEE011) 是一种细胞周期蛋白依赖性激酶 CDK4 6 抑制剂 (IC50=10 39 nM)，具有特异性和口服活性。Ribociclib 具有抗肿瘤活性，可以阻滞细胞周期，抑制肿瘤细胞增殖。

Irinotecan (CPT-11) 是喜树碱的衍生物，是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂。Irinotecan 通过与 Topo I 复合物结合来阻止 DNA 链的重新连接，并导致双链 DNA 断裂和细胞死亡，具有抗肿瘤活性。

Tirbanibulin (KX2-391) 是一种高度选择性的 Src 激酶抑制，靶向 Src 的多肽底物结合位点，对多种癌症有疗效。

Tirbanibulin Mesylate (KX01 Mesylate) 是一种 Src 抑制剂，靶向 Src 的肽底物位点。在肿瘤细胞中，GI50值为 9-60 nM。

PAT-505 是一种可口服且具有选择性和高效性的自体表皮生长因子抑制剂（在 Hep3B 细胞中的 IC50 为 2 nM，在人体血液中的 IC50 为 9.7 nM，在小鼠血浆中的 IC50 为 62 nM）。

DGAT1-IN-1是 DGAT1的高效抑制剂，在 Hep3B 细胞过表达 DGAT1裂解物中，测得IC50低于10nM。

Myceliothermophin E is a polyketide-amino acid hybrid fungal metabolite that has been found inT. thermophilusand has anticancer and antimicrobial activities.1,2It is cytotoxic to DLD-1, Hep3B, HepG2, and HGC-27 cancer cells (IC50s = 0.32, 0.42, 0.26, and 0.08 μg/ml, respectively).1Myceliothermophin E is active against methicillin-resistant, but not -sensitive,S. aureus(MICs = 15.8 and >100 μM, respectively).2 1.Gao, Y.-L., Zhang, M.-L., Wang, X., et al.Isolation and characterization of a new cytotoxic polyketide-amino acid hybrid from Thermothelomyces thermophilus ATCC 42464Nat. Prod. Res.Epub ahead of print(2019) 2.Wang, X., Zhao, L., Liu, C., et al.New tetramic acids comprising of decalin and pyridones from Chaetomium olivaceum SD-80A with antimicrobial activityFront. Microbiol.102958(2020)

Destruxin B2 is a cyclic hexadepsipeptide mycotoxin that has been found in M. anisopliae and has antiviral, insecticidal, and phytotoxic activities.1,2,3 It inhibits secretion of hepatitis B virus surface antigen (HBsAg) by Hep3B cells expressing hepatitis B virus (HBV) DNA (IC50 = 1.3 μM).1 Destruxin B2 is toxic to Sf9 insect cells in an electric cell-substrate impedance sensing (ECIS) test with a 50% inhibitory concentration (ECIS50) value of 92 μM.4 It is also phytotoxic to B. napus leaves.3 |1. Yeh, S.F., Pan, W., Ong, G.-T., et al. Study of structure-activity correlation in destruxins, a class of cyclodepsipeptides possessing suppressive effect on the generation of hepatitis B virus surface antigen in human hepatoma cells. Biochem. Biophys. Res. Commun. 229(1), 65-72 (1996).|2. Male, K.B., Tzeng, Y.-M., Montes, J., et al. Probing inhibitory effects of destruxins from Metarhizium anisopliae using insect cell based impedance spectroscopy: Inhibition vs chemical structure. Analyst 134(7), 1447-1452 (2009).|3. Buchwaldt, L., and Green, H. Phytotoxicity of destruxin B and its possible role in the pathogenesis of Alternaria brassicae. Plant Pathol. 41(1), 55-63 (1992).

Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the production of reactive oxygen species (ROS) in, Hep3B human hepatocellular carcinoma cells. It does not induce cytotoxicity in RBL-2H3 mast cells at concentrations up to 100 μM. Streptochlorin prevents degranulation in antigen-stimulated mast cells, as well as inhibits Syk kinase and the Src family kinases LYN and Fyn and reduces the secretion of TNF-α and IL-4 induced by dinitrophenyl-human serum album (DNP-HSA) in RBL-2H3 mast cells. It also decreases swelling and reduces scratching behavior in a mouse model of allergic dermatitis induced by dinitrofluorobenzene (DNFB).

Corilagin 是一种鞣酸，有抑制 RNA 肿瘤病毒逆转录酶的活性。它抑制金黄色葡萄球菌的生长，MIC 为 25 μg mL。它有抗肿瘤活性，可用于肝癌和卵巢癌。

PROTAC PD-1 PD-L1 degrader-1 是一种降解 PD-L1 的 PROTAC，抑制 PD-1 PD-L1 相互作用（IC50：39.2 nM）。PROTAC PD-1 PD-L1 degrader-1 可恢复 Hep3B OS-8 hPD-L1 和 CD3 T 细胞共培养模型中被抑制的免疫力，可通过溶酶体依赖性方式降低 PD-L1 的蛋白质含量。

Steviolbioside (CCRIS-6025) 是一种存在于甜菊叶中的罕见甜味剂。它对几种人类癌细胞有抑制作用，对乳腺癌具有潜在的研究价值。

Corylifol A (Corylinin) 是补骨脂中的一种天然产物，可抑制IL-6 诱导的STAT3激活和磷酸化，IC50值为0.81 μM。

PD-1 PD-L1-IN 6 (compound A13) 是有效的PD-1 PD-L1相互作用抑制剂（IC50为 132.8 nM）。PD-1 PD-L1-IN 6 显示出显著的免疫调节活性。 在 Hep3B OS-8 hPD-L1 与 CD3 T 细胞共培养模型中，PD-1 PD-L1-IN 6显著提高干扰素 -γ 分泌，且无明显毒性作用。 在 T 细胞-肿瘤共培养模型中，PD-1 PD-L1-IN 6恢复免疫应答。

Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells. It increases levels of secreted erythropoietin in Hep3B cells in a concentration-dependent manner and increases erythropoiesis in rats when administered at doses of 25 and 50 mg kg. Roxadustat reverses anemia in a rat model of chronic inflammation induced by peptidoglycan-polysaccharide, as well as a rat model of chronic kidney disease induced by 5 6 nephrectomy. It reduces tumor growth and increases survival in a murine Lewis lung carcin......