u937

RIPK1-IN-9是是一种强效且具有选择性的 RIPK1抑制剂，是一种二氢萘酮化合物。RIPK1-IN-9对 U937细胞和 L929细胞具有抑制作用，IC50分别为2 nM 和1.3 nM。

GSK481 (GSK'481) 是一种选择性，特异性RIP1抑制剂，其IC50值为 1.3 nM，可抑制野生型人RIP1中的 Ser166磷酸化，IC50值为 2.8 nM。它对 U937 细胞的IC50值为 10 nM。

BC-1215 是一种 F-box protein 3 抑制剂。它能够稳定 TRAF1-TRAF6 来抑制 Fbxo3-TRAF 激活途径。它与 ApaG 相互作用，阻碍来自人 PBMC 广谱 TH1 细胞因子的分泌。

Solasodine (Purapuridine) 是存在于茄科植物中的一种类固醇生物碱。它具有神经保护、降压、抗真菌、抗癌、抗动脉粥样硬化、抗雄激素和抗炎活性。

AI-10-47 (1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47) 是 CBFβ-RUNX 结合的小分子抑制剂(IC50:3.2 μM)。

MK2-IN-3 (MK2 Inhibitor III) 是选择性的 MAPKAP-K2 (MK-2)抑制剂(IC50:8.5 nM)，能够抑制 U937 细胞及体内 TNFα 的生成。

NIBR189是 EBI2（GPR183）小分子拮抗剂(IC50:11 nM)。

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

6-OAU (GTPL5846) 是 GPR84 的替代激动剂，在 Gqi5 嵌合体存在的情况下，在 HEK293 细胞中激活人 GPR84，在 PI 测定中 EC50 为 105 nM。

Oxanosine is an analog of guanosine that has been found in S. capreolus and has diverse biological activities, including antibacterial, antiviral, and anticancer properties. It is active against a variety of bacteria, including S. flexneri, P. mirabilis, and E. coli (MICs = 6.25, 12.5, 25 µg/ml, respectively, on peptone, but not nutrient, agar). Oxanosine inhibits replication of the HIV-1 strain IIIb in infected CEM and U937, but not H9, cells (EC50s = 7, 27, and >500 µg/ml, respectively). It also inhibits the growth of HeLa human cervical cancer cells (IC50 = 32 µg/ml) and reduces tumor growth in a murine L1210 lymphocytic leukemia model.

Eicosapentaenoic Acid (EPA) sodium 为口服活性 ω-3 长链多不饱和脂肪酸 (ω-3 LC-PUFAs)。其通过DNA去甲基化，促进肿瘤抑制基因CCAAT 增强子结合蛋白δ (C EBPδ)的重新表达，并通过H-RAS内含子1 CpG岛的去甲基化，激活U937白血病细胞中RAS ERK C EBPβ途径。此外，该化合物能够促进血管平滑肌细胞松弛和血管舒张。

ML390 是二氢乳清酸脱氢酶抑制剂。他是骨髓分化的诱导剂，能够引起鼠 (ER-HoxA9) 以及人 (U937 and THP1) 急性髓细胞性白血病 (AML) 细胞发生骨髓分化。

C6 L-erythro Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is metabolized by ceramide glucosyltransferase to form C6 L-erythro glucosylceramide. C6 L-erythro Ceramide is cytotoxic to U937 cells (IC50 = 18 μM).

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.

Mahanine has effects on the activation of the apoptotic pathway in human leukemia U937 cells, causes the mitochondrial membranes to lose their permeability, resulting in caspase-3 activation and apoptosis. Mahanine can reverse an epigenetically silenced g

BML-278 是一种 SIRT1 激活剂 ，EC150 值为 1 μM。BML-278 增加父本和母本原核中的 H3K9 甲基化并抑制 H3K9 乙酰化，可用于改善早期胚胎发育。BML-278 促使原代人间充质细胞的细胞周期停止在 G1 S 期，可用于延缓衰老。BML-278 减少 U937 细胞中的微管蛋白乙酰化，增加小鼠 C2C12 成肌细胞的线粒体密度。

MOZ-IN-3 (Compound 6j) 是KAT6A (MOZ) 乙酰转移酶的抑制剂，IC50值为30 nM。该化合物在四种髓系白血病细胞系（HL-60、U937、SKNO-1、K562）上展现了抗肿瘤活性，并且显示出良好的代谢稳定性及药代动力学特性。

M50054 是一种有效的细胞凋亡抑制剂，可用于研究抗 Fas 抗体引起的肝炎和化疗引起的脱发。它抑制 Etoposide 诱导的 U937 细胞 caspase-3 活化，IC50为 79 μg mL。

C8 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 17 μM) and induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 ceramide . C8 D-threo Ceramide is a substrate for E. coli diacylglycerol kinase. It activates ceramide-activated protein kinase (CAPK) in U937 cells. C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein release, with a 50% release dose (RD50) value of ~5 μg ml.

Bepafant is a platelet activating factor (PAF) antagonist. Bepafant may produce significant anti-inflammatory effects. Bepafant triggered apoptosis in NB4, KG1, and NB4-MR4 cells where PTEN was expressed, but not in THP1 and U937 cells where PTEN was abse

Glutaminyl cyclases-IN-1 (IsoQC-IN-1) 是一种谷氨酰胺酰基环化酶 (glutaminyl cyclases, QC) 的有效抑制剂，作用于人 QC (IC50: 12 nM) 和 isoQC (IC50: 73 nM)。Glutaminyl cyclases-IN-1 能够抑制 isoQC，进而选择性的阻碍 CD47 SIRPα 的相互作用，也可以提高 THP-1 和 U937 巨噬细胞的吞噬作用。

MC4171 是一种选择性 KAT8 抑制剂 ，具有抗增殖活性，可用于研究癌症。

Anandamide (arachidonoyl ethanolamide; AEA) is an endogenous lipid with cannabinergic activity; along with 2-arachidonoyl glycerol, it forms part of the endocannabinoid system. AEA undergoes reuptake into neurons by a facilitated process. Controversy exists as to whether there is a specific AEA transporter, or instead the uptake process is simply driven by hydrolysis of AEA by intracellular fatty acyl amide hydrolase (FAAH). CAY10412 is an analog of AEA that has no intrinsic binding affinity for either CB1 or CB2 receptors. It is a potent inhibitor of AEA reuptake in U937 lymphoma cells, with an IC50 of 3 μM. CAY10412 could be a useful tool for distinguishing the competing transporter theories. The pharmacology of CAY10412 is largely unexplored; it may enhance endocannabinoid signalling by augmenting endocannabinoid concentrations.

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation.

C6 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 L-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 L-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 L-threo Ceramide enhances IL-4 production induced by phorbol 12-myristate 13-acetate in EL4 T cells when used at a concentration of 10 μM.

1alpha-Hydroxy VD4 can effectively induce the differentiation of monoblastic leukaemia U937, P39 TSU, and P31 FUJ cells.

2-Hydroxy-3-methylanthraquinone enhances apoptosis of U937 cells,in part,through activation of p-p38MAPK and downregulation of p-ERK1/2; triggers caspase-3 activation mediated apoptotic induction.

C6 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 D-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 D-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 D-threo Ceramide promotes survival of isolated rat spinal neurons when used at concentrations up to 2.5 μM but induces cell death at concentrations greater than 5 μM. It enhances IL-4 production induced by phorbol 12-myristate 13-acetate in EL4 T cells when used at a concentration of 10 μM.

Cathepsin C-IN-4 是一种组织蛋白酶 C (Cat C) 的有效抑制剂 (IC50: 65.6 nM)。Cathepsin C-IN-4 对 THP-1 (IC50: 203.4 nM)和 U937 (IC50: 177.6 nM) 细胞具有抑制作用。

KF38789 特异性的抑制P-selectin 与PSGL-1结合。它对 U937 细胞与 P-selectin 免疫球蛋白 G 嵌合蛋白 (P-selectin-Ig) 的结合具有抑制作用 (IC50:1.97 μM) 。

Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.

CAY10789 (化合物 6) 是有效的CysLT1R 拮抗剂 ，IC50值为2.80 μM。CAY10789 也是一种GPBAR1激动剂 ，EC50为3 μM。CAY10789 显著降低 U937 细胞对 HAEC 的粘附并降低 TNF-α 的表达。CAY10789 表现出有前途的代谢稳定性和出色的药代动力学。 CAY10789 可用于结肠炎、代谢综合征和其他 GPBAR1 CysLT1R 相关疾病的研究。

O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral administrationXenobiotica41(12)1063-1075(2011) 2.Lu, Y., Shen, X., Hang, T., et al.Identification and characterization of process-related substances and degradation products in apremilast: Process optimization and degradation pathway elucidationJ. Pharm. Biomed. Anal.14170-78(2017) 3.Bhole, R.P., Naksakhare, S.R., and Bonde, C.G.A stability indicating HPTLC method for apremilast and identification of degradation products using MS MSJ. Pharm. Sci. & Res.11(5)1861-1869(2019)

2-Desoxy-4-epi-pulchellin 是分离自 Polygonum hydropiper 的二氯甲烷可溶部分的一种化合物。

m-3M3FBS 是一种有效的磷脂酶C 激活剂，刺激人中性粒细胞产生超氧物，上调细胞内钙离子浓度，刺激多种细胞产生磷酸肌醇。它诱导单核细胞白血病细胞凋亡。

SLP7111228 is a potent, selective SPHK1 inhibitor with Ki values of 0.048 μM for SPHK1 and >10 μM for SPH2K, showing a concentration-dependent reduction of sphingosine-1-phosphate (S1P) in U937 cells without affecting sphingosine levels. In vivo, it dose-dependently lowers S1P blood levels in rats.

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and Bcl-x(L). CGP74514A treatment (5 microM; 18 hr) resulted in increased p21(CIP1) expression, p27(KIP1) degradation, diminished E2F1 expression, and dephosphorylation of p34(CDC2). It also induced early (i.e., within 2 hr) inhibition of CDK1 activity and dephosphorylation of pRb, followed by pRb degradation, but did not block pRb phosphorylation at CDK2- and CDK4- specific sites. These findings indicate that the selective CDK1 inhibitor, CGP74514A , induces complex changes in cell cycle......

4-Iodo-SAHA (1k) 是一种具有口服活性的I 类和II 类histone deacetylase (HDAC)抑制剂，对 Skbr3、 HT29、 U937、 JA16 和 HL60细胞的EC50值分别为1.1、0.95、0.12、0.24、0.85和1.3 μM。4-Iodo-SAHA (1k) 可用于癌症的研究。

Kaempferol tetraacetate is a potent antiplatelet agent. It exhibits significant cytotoxicity in vitro against three human cell lines HL-60, U937 and SK-MEL-1.

Schisandrin C (Wuweizisu-C) 是从五味子中分离得到的一种植物化学木脂素。它具有抗癌、抗炎和抗氧化等多种生物活性，可研究癌症、阿尔茨海默病、肝病。

4,5-Dimethoxycanthin-6-one 从 Picrasma quassioides BENNET (Simaroubaceae)是一种从 Picrasma quassioides BENNET (Simaroubaceae) 中分离得到生物碱。4,5-Dimethoxycanthin-6-one 是一种有效的、非竞争性的 CYP1A2 介导的 phenacetin O-deethylation 抑制剂（IC50 ： 1.7 μM, Ki ： 2.6 μM），对环磷酸腺苷（cAMP）磷酸二酯酶有很强的抑制作用。4,5-Dimethoxycanthin-6-one 具有抗菌活性，对金黄色葡萄球菌及其耐药菌株有抑制作用。4,5-Dimethoxycanthin-6-one 对肿瘤细胞株 U937 和 HepG2 具有细胞毒性。

Jolkinolide B 是一种从 Euphorbia fischeriana Steud 的根中分离出来的具有生物活性的二萜。 Jolkinolide B 诱导癌细胞凋亡。 Jolkinolide B 可用于预防和治疗骨溶解的研究。

HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng ml and human umbilical vein endothelial cells with an IC50value of 56.4 ng ml.1It induces oxidative stress, DNA damage, and autophagy in, as well as halts the development of, cultured mouse embryos when used at a concentration of 10 nM.3HT-2 toxin has been found in cereal grains and food products.4,5 1.Nielsen, C., Casteel, M., Didier, A., et al.Trichothecene-induced cytotoxicity on human cell linesMycotoxin Res.25(2)77-84(2009) 2.Nathanail, A.V., Varga, E., Meng-Reiterer, J., et al.Metabolism of the fusarium mycotoxins T-2 toxin and HT-2 toxin in wheatJ. Agric. Food Chem.63(35)7862-7872(2015) 3.Zhang, L., Li, L., Xu, J., et al.HT-2 toxin exposure induces mitochondria dysfunction and DNA damage during mouse early embryo developmentReprod. Toxicol.85104-109(2019) 4.Langseth, W., and Rundberget, T.The occurrence of HT-2 toxin and other trichothecenes in Norwegian cerealsMycopathologia147(3)157-165(1999) 5.Al-Taher, F., Cappozzo, J., Zweigenbaum, J., et al.Detection and quantitation of mycotoxins in infant cereals in the U.S. market by LC-MS MS using a stable isotope dilution assayFood Control72(Part A)27-35(2017)

C8 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 10 μM) and, like C8 D-threo ceramide , induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 L-erythro ceramide . C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein release, with a 50% release dose (RD50) value of ~30 μg ml.

RIPK1-IN-14 (Compound 41) 是一种 RIPK1 的有效抑制剂 (IC50: 92 nM)。RIPK1-IN-14 在 U937 细胞的坏死性凋亡模型中具有明显的抗坏死性凋亡效果。

BAY-218 (AHR antagonist 1) 是一种芳基烃受体(AHR)拮抗剂，在人细胞系中的IC50值为 39.9 nM。

Cathepsin C-IN-3 是组织蛋白酶 C (Cat C) 的有效抑制剂 (IC50: 61.79 nM)，也能抑制 THP-1 细胞 (IC50: 101.5 nM) 和 U937 细胞 (IC50: 86.5 nM)。