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T9616
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PD-1/PD-L1-IN-10
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PD-1/PD-L1 |
Apoptosis;
Cell Cycle/Checkpoint;
Immunology/Inflammation |
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PD-1/PD-L1-IN-10 是一种口服有效的PD-1/PD-L1抑制剂 (IC50of 2.7 nM)，显示出抗肿瘤活性。 |
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T7701
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Boc-NH-PEG3
PROTAC Linker 10,2-[2-(2-T-BOC-氨基乙氧基)乙氧基]乙醇
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Others;
PROTAC Linker |
Others;
PROTAC |
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Boc-NH-PEG3 (PROTAC Linker 10) 是一种属于 PEG 类的 PROTAC linker，可用于 PROTAC 的合成分子。 |
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T18366
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Ms-PEG10-t-butyl ester
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Others |
Others |
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Ms-PEG10-t-butyl ester is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells. |
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T30077
|
Anisperimus
LF 150195,LF-150195,LF 15-0195,LF-15-0195,LF15-0195
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Caspase |
Apoptosis;
Proteases/Proteasome |
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Anisperimus (LF 15-0195) 是一种免疫抑制剂，通过促进 DISC 水平的 caspase-8 和 caspase-10 激活来增强激活诱导的 T 细胞死亡，通过促进表达 Foxp3 的调节性 CD4 T 细胞的发育来预防中枢神经系统自身免疫。 |
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T28903
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T-3364366
T 3364366,T3364366
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Others |
Others |
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T-3364366 是一种噻吩并嘧啶酮 delta-5 去饱和酶 (Δ5D) 抑制剂，在 HepG2 和 RLN-10 细胞中的 IC50 分别为 1.9 nM 和 2.1 nM。 |
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T6120
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Pralatrexate
Folotyn,10-炔丙基-10-去氮杂氨基蝶呤,10-Propargyl-10-deazaaminopterin,普拉曲沙
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Apoptosis;
DHFR;
Antifolate;
TAM Receptor |
Apoptosis;
Cell Cycle/Checkpoint;
DNA Damage/DNA Repair;
Metabolism;
Tyrosine Kinase/Adaptors |
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Pralatrexate (10-Propargyl-10-deazaaminopterin) 是一种抗叶酸剂，也是二氢叶酸还原酶抑制剂，Ki 值为 13.4 pM。它具有抗肿瘤活性，可研究复发/难治性 T 细胞淋巴瘤。它是叶酰聚谷氨酸合成酶的底物，具有改善的细胞摄取和保留能力。 |
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T16832
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S18-000003
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ROR |
Metabolism |
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S18-000003 是口服有活性的维甲酸相关孤儿受体 (RORγt) 选择性抑制剂，在竞争性结合试验中，对 hRORγt 的 IC50值小于 30 nM。它对 RORγt 的选择性比其他 ROR 家族成员 (IC50>10 μM)更高。它可用于银屑病的研究，胸腺畸变风险较低。 |
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T35449
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α-(difluoromethyl)-DL-Arginine
DFMA,RMI 71897,α-(difluoromethyl)-DL-Arginine
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Others |
Others |
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α-(difluoromethyl)-DL-Arginine (RMI 71897) 是一种酶激活的、不可逆的大肠杆菌(Ki = 800 μM)、铜绿假单胞菌和肺炎克雷伯菌精氨酸脱羧酶抑制剂。在0.01 mM 时，它已被证明可以防止渗透胁迫诱导的燕麦叶片细胞精氨酸脱羧酶活性和腐胺合成的增加。当α-(difluoromethyl)-DL-Arginine 与多种多胺类似物联用时，能在10 mM 的最低浓度下抑制克氏锥虫在哺乳动物宿主细胞中的生长，并在T 细胞受体α缺陷小鼠模型中阻止小锥虫的生长。 |
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T4403
|
AX-024 hydrochloride
AX-024 HCl
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IL Receptor;
TNF;
COX;
IFNAR;
Interleukin |
Apoptosis;
Immunology/Inflammation;
Neuroscience |
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AX-024 hydrochloride (AX-024 HCl) 是一种细胞因子释放抑制剂，可强烈抑制 IL-6、TNFα、IFN-γ、IL-10 和 IL-17A 的产生。它是口服可利用的 TCR-Nck 相互作用抑制剂，可选择性地抑制 TCR 触发的 T 细胞活化。它通过靶向 SH3结构域调节细胞信号传导，具有低毒、高效和高选择性的特点。 |
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T14943
|
CGP60474
|
VEGFR;
CDK;
PKC |
Angiogenesis;
Cell Cycle/Checkpoint;
Chromatin/Epigenetic;
Cytoskeletal Signaling;
Tyrosine Kinase/Adaptors |
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CGP60474 是一种高效的抗内毒素药物，抑制细胞周期蛋白依赖激酶(CDK) ，抑制 CDK1/B、CDK2/E、CDK2/a、CDK4/D、CDK5/p25、CDK7/H 和 CDK9/T 的IC50分别为 26、3、4、216、10、200 和 13 nM。它是选择性和 ATP 竞争性PKC 抑制剂。 |
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T11846
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LHVS
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Cysteine Protease |
Proteases/Proteasome |
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LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion. LHVS is a potent, non-selective cysteine protease inhibitor. |
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T36331
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Z-AEVD-FMK
Z-AEVD-FMK,Z-Ala-Glu-Val-Asp-Fluoromethyl Ketone
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Z-AEVD-FMK is an irreversible inhibitor of caspase-10 and related caspases.[1] At 10 µM, it can prevent the initiation of Fas signaling by caspase-10 in Jurkat T lymphoma cells, preventing Bid cleavage into its active form, caspase cascade activation, and apoptosis.[2] |
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T77775
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TP-1454
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TP-1454是一种针对PKM2的激活剂，其生化测定的AC50为10 Nm。它可通过作用于T调节细胞来调控肿瘤的免疫反应。 |
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TP2101
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Z-VRPR-FMK trifluoroacetate salt
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Irreversible MALT1 inhibitor. Suppresses T cell activation-induced cleavage of Bcl-10 in a dose-dependent manor. Reduces Jurkat cell adhesion to fibronectin. Cell permeable. |
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T35912
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Pyrocoll
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Pyrocoll is a bacterial metabolite originally isolated from Streptomyces. It inhibits the growth of A. aurescens, A. globiformis, A. oxydans, A. pascens, and R. erythropolis bacteria (MICs = 10, 1, 10, 3, and 10 μg/ml, respectively) and HMO2, HepG2, and MCF-7 cancer cells (GI50s = 0.28, 0.42, and 2.2 μg/ml, respectively) in vitro. Pyrocoll is also active against P. falciparum and T. rhodesiense (IC50s = 1.19 and 1.97 μg/ml, respectively). |
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T36858
|
C12 Galactosylceramide (d18:1/12:0)
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C12 Galactosylceramide is a bioactive sphingolipid. It inhibits IL-4 production by 53.84% in EL4 T cells when used at a concentration of 10 μM. C12 Galactosylceramide reduces the growth of human papillomavirus type 16-associated tumors in mice and reduces tumor recurrence following surgical removal or chemotherapy. It also reduces natural killer T cell activity, delays the onset of proteinuria, and improves survival in a mouse model of systemic lupus. |
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T62927
|
HPK1-IN-22
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HPK1-IN-22 (compound ZYF0033) 是一种造血祖细胞激酶 1 (HPK1) 抑制剂，基于 MBP 蛋白的磷酸化抑制作用的 IC50小于 10 nM。HPK1-IN-22 能够减少 SLP76 (丝氨酸 376) 的磷酸化，促进抗癌免疫反应。HPK1-IN-22 可以抑制 4T-1 同基因小鼠模型中的肿瘤生长，增加 DC、NK 细胞和 CD107a+CD8+T 细胞的肿瘤内浸润，但会减少 T 细胞、PD-1+CD8+T 细胞、TIM-3+CD8+T 细胞和 LAG3+CD8+T 细胞的浸润。 |
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T40043
|
RORγt Inverse agonist 10
|
|
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RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R. |
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T79533
|
PDE5-IN-10
|
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PDE5-IN-10 (compound 4b)，一有效PDE5抑制剂，IC50值为20 nM。该化合物体外微粒体稳定性增强（t1/2= 44.6 分钟），在长期增强恢复方面效果显著，适用于阿尔茨海默病（AD）研究。 |
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T83874
|
S-72
|
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S-72是一种微管聚合抑制剂，以1, 3, 10 µM的浓度在无细胞测定中抑制微管聚合，并在MCF-7和耐紫杉醇的MCF-7/T乳腺癌细胞中降低细胞活性（IC50分别为15.64和26.32 nM）。50 nM浓度的S-72能抑制MCF-7和MCF-7/T细胞的迁移和侵袭，并减少划痕实验中的伤口闭合百分比。100 nM的S-72在MCF-7/T细胞中诱导G2/M期的细胞周期阻滞以及凋亡，并在同一浓度下抑制这些细胞中干扰素基因激活剂（STING）的激活。以每天15 mg/kg的剂量，S-72抑制了耐紫杉醇的MCF-7/T和MX-1/T小鼠异种移植模型中的肿瘤生长。 |
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T36254
|
dTAGV-1 hydrochloride
|
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Hydrochloride salt of dTAGV-1. Suitable for use in vivo. Following ip administration of 10 mg/kg in mice: T = 4.43 h; Cmax = 2123 ng mL-1; AUCinf = 18517 hr*ng mL-1 and CL = 9.05 mL min-1 kg-1 Negative control dTAGV-1-NEG also available. Important: It is recommended that DMSO stock solutions of this compound are made and used on the same day and are not subjected to freeze/thaw. |
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T35927
|
C2 L-threo Ceramide (d18:1/2:0)
C2 L-threo Ceramide (d18:1/2:0)
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C2 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide . C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1... |
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T38383
|
Altemicidin
|
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Altemicidin is a monoterpene alkaloid originally isolated fromS. sioyaensiswith acaricidal and anticancer activities.1It is acaricidal to two-spotted spider mites (T. urticae) in a greenhouse pot test at concentrations of 10 and 100 ppm. Altemicidin inhibits the growth of murine L1210 lymphocytic leukemia and IMC carcinoma cells (IC50s = 0.84 and 0.82 μg/ml, respectively). It is toxic to mice with an LD50value of 0.3 mg/kg.
1.Takahashi, A., Kurasawa, S., Ikeda, D., et al.Altemicidin, a new acari... |
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T38340
|
10-Norparvulenone
|
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10-Norparvulenone is a fungal metabolite originally isolated fromMicrosphaeropsis.1It decreases viral sialidase activity in, and increases survival of, MDCK cells infected with the mouse-adapted influenza virus A/PR/8/34 when used at a concentration of 1 μg/ml.
1.Fukami, A., Nakamura, T., Kim, Y.P., et al.A new anti-influenza virus antibiotic, 10-norparvulenone from Microsphaeropsis sp. FO-5050J. Antibiot. (Tokyo)53(10)1215-1218(2000) |
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T36982
|
CXCR3 Antagonist 6c
|
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CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50= 0.06 μM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 μM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50= ~100 nM).
1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial eva... |
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T36320
|
C6 L-threo Ceramide (d18:1/6:0)
C6 L-threo Ceramide (d18:1/6:0)
|
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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. |
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T36887
|
8(E),10(E),12(Z)-Octadecatrienoic Acid
|
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8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland... |
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T36323
|
C8 Galactosylceramide (d18:1/8:0)
C8 Galactosylceramide (d18:1/8:0)
|
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C8 Galactosylceramide is a synthetic C8 short-chain derivative of known membrane microdomain-forming sphingolipids. It increases the amount delivered and toxicity of doxorubicin in cancerous but not non-cancerous cells when incorporated into the nanoliposomal membrane of nanoliposomal-doxorubicin. C8 Galactosylceramide induces proliferation and cytokine production by splenocytes in vitro at concentrations ranging from 100-1,000 ng/ml but has no effect on natural killer T cell production in vivo.... |
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T72213
|
Efonidipine hydrochloride
NZ-105 hydrochloride
|
|
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Efonidipine(NZ-105)盐酸盐是T 型和L 型钙离子通道双重阻断剂。 |
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T61071
|
AX-024
|
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AX-024 is a novel chemical compound that acts as an orally available inhibitor of the TCR-Nck interaction. Its primary mechanism of action is the selective inhibition of T cell activation triggered by TCR stimulation. With an IC50 value of approximately 1 nM, AX-024 effectively modulates cell signaling by specifically targeting SH3 domains. Additionally, AX-024 demonstrates desirable characteristics such as low acute toxicity, high potency, and excellent selectivity. Notably, it exhibits strong ... |
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T37722
|
Diprovocim-1
|
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Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma mo... |
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T37564
|
C4 Ceramide (d18:1/4:0)
C4 Ceramide (d18:1/4:0),Cer(d18:1/4:0)
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C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7/Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing... |
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T37565
|
C6 D-threo Ceramide (d18:1/6:0)
C6 D-threo Ceramide (d18:1/6:0)
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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... |
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T35541
|
Lipoxygenin
|
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Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin... |
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T35918
|
N-Arachidonoyl Taurine
|
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N-Arachidonoyl taurine is an arachidonoyl amino acid. It is oxygenated by 12(S)- and 15(S)-lipoxygenase and is converted to 12-HETE-taurine (12-HETE-T) in murine resident peritoneal macrophages. N-Arachidonoyl taurine is an activator of the transient receptor potential vanilloid (TRPV) channels TRPV1 and TRPV4 (EC50s = 28 and 21 μM, respectively). It increases calcium flux in HIT-T15 pancreatic β-cells and INS-1 rat islet cells when used at a concentration of 10 μM and increases insulin secretio... |
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T37431
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ENPP1 Inhibitor C
ENPP1 Inhibitor C
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ENPP1 inhibitor C is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50 = 0.26 μM in a cell-free assay).1 It is selective for ENPP1 over ENPP2-7 at 10 μM. ENPP1 inhibitor C decreases ENPP1 activity in MDA-MB-231 human breast and C6 rat glioma cancer cells when used at a concentration of 10 μM.
|1. Kawaguchi, M., Han, X., Hisada, T., et al. Development of an ENPP1 fluorescence probe for inhibitor screening, cellular imaging, and prognostic assessment of malignant brea... |
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T35775
|
HT-2 Toxin-13C22
HT-2 Toxin-13C22
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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... |
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T35979
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Benastatin C
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Benastatin C is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2It inhibits glutathione S-transferase (GST; IC50= 24 μg/ml for the rat liver enzyme).2Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50= 10 μg/ml). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner.
1.Xu, Z., Schenk, A., and Hertweck, C.Molecul... |
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T83910
|
S1PL-IN-31
Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31
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S1PL-IN-31是一种鞘氨醇-1-磷酸(S1P)裂解酶的抑制剂(IC50 = 210 nM)，同时也是Smoothened(Smo)受体的对抗剂(IC50 = 440 nM)。在体内，S1PL-IN-31 (每天2 mg/kg)能够防止实验性自身免疫性脑炎(EAE)模型大鼠中，由髓鞘少突胶质细胞糖蛋白(MOG)肽段MOG29-152诱发的颈部及胸部淋巴细胞渗透和神经肌肉虚弱。该化合物降低了大鼠的淋巴细胞总数及CD4+ T细胞、CD8+ T细胞和B细胞的水平。S1PL-IN-31 (每天3及10 mg/kg剂量)在雄性和雌性大鼠心脏和淋巴结中增加了S1P水平，并且在雌性大鼠中降低了心率。 |
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T35829
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CC-90005
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CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1].
CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS... |
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T37329
|
PROTAC IDO1 Degrader-1
PROTAC IDO1 Degrader-1
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PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1].
PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24... |
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T36539
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Nocardamine
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Nocardamine is a ferrioxamine siderophore that has been found inStreptomycesand has diverse biological activities.1,2,3,4It chelates iron in a chrome azurol S assay (IC50= 9.9 μM).1Nocardamine inhibitsM. smegmatisandM. bovisbiofilm formation (MIC = 10 μM for both), an effect that can be reversed by iron.2It is cytotoxic to T47D, SK-MEL-5, SK-MEL-28, and RPMI-7951 cancer cells (IC50s = 6, 18, 12, and 14 μM, respectively).3Nocardamine also induces morphological changes in BM-N4 insect cells.4
1.Lo... |
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T37692
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Piericidin B
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Piericidin B is a bacterial metabolite that has been found inS. mobaraensisand has insecticidal and antimicrobial activities.1,2,3It inhibits NADH oxidase activity in isolated bovine heart mitochondria and inhibits respiration in isolated rat liver mitochondria and isolated cockroach (P. americana) muscle mitochondria.2,3Topical application of piericidin B (4 μg/insect) induces mortality in 87.5% of houseflies (M. domestica).1It induces 93.3, 100, and 100% mortality in rice stem borer (C. simple... |
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T35940
|
Darinaparsin
Dimethylarsinic glutathione,Darinaparsin
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Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2,... |
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T35451
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β-Defensin-2 (human) (trifluoroacetate salt)
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β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes whe... |
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T83779
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EP4 Antagonist 14
Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14
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EP4 antagonist 14是一种前列腺素E2（PGE2）受体亚型EP4的拮抗剂，其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募（IC50 = 0.9 nM）。EP4 antagonist 14（10 µM）能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达，这些mRNA编码Il-4、巨噬细胞甘露糖受体1（Mrc1）、几丁质酶样蛋白3（Chil3）、趋化因子（C-X-C）基序配体1（Cxcl1）、表达在髓样细胞上的触发受体2（Trem2）和精氨酸酶-1（Arg1）。在体内，EP4 antagonist 14（每天30 mg/kg），结合抗PD-1抗体，能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。 |
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T35504
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(±)10-HDHA
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(±)10-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro.[1][2] It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes.[3][4][5] (±)10-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid.
Reference：[1]. VanRollins, M., and Murphy, R.C. Autooxidation of docosahexaenoic acid: Analysis of ten isomers of hydroxydocosahexaenoate. J. Lipid Res. 25(5), 507-517 (1984).[2]. Reynaud, ... |
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T37723
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IT-143A
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IT-143A is a bacterial metabolite originally isolated fromStreptomycessp. IT-143.1It is active against the bacteriumM. luteus(MIC = 6.25 μg/ml) and the fungiA. fumigatusandT. rubrumin vitro(MICs = 12.5-25 μg/ml).
1.Urakawa, A., Sasaki, T., Yoshida, K., et al.IT-143-A and B, novel piericidin-group antibiotics produced by Streptomyces SpJ. Antibiot. (Tokyo)49(10)1052-1055(1996) |
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T38381
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CAY17c
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CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,... |
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T38309
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LL-37 amide (trifluoroacetate salt)
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LL-37 is a cationic and α-helical antimicrobial peptide expressed in human bone marrow, testis, granulocytes, and gingival epithelium and is upregulated in psoriatic lesions. It inhibits growth of Gram-positive E. coli D21 and Gram-negative B. megatarium in a concentration-dependent manner and LL-37 expression is induced in A549 epithelial cells, alveolar macrophages, neutrophils, and monocyte-derived macrophages following M. tuberculosis infection. LL-37 binds sheep erythrocytes coated with S. ... |
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