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13

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T10657 C75

C-75

Fatty Acid Synthase Metabolism
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)。
T10656 trans-C75

(±)-C75,反-4-羧基-5-辛基-3-甲基-丁内酯

Others; Fatty Acid Synthase Metabolism; Others
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。
T10801 CHMFL-ABL/KIT-155

CHMFL-ABL-KIT-155

c-Kit Tyrosine Kinase/Adaptors
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.
TF0100 C-HEGA-8

C-HEGA-8 是一种有用的有机化合物,可用于生命科学领域的相关研究。其产品编号为 TF0100,CAS号为 603111-75-7。
T76185 N-Myristoyl-Lys-Arg-Thr-Leu-Arg

N-Myristoyl-Lys-Arg-Thr-Leu-Arg 是一种蛋白激酶 C (PKC) 抑制剂,其 IC50值为 75 μM。N-Myristoyl-Lys-Arg-Thr-Leu-Arg 抑制人白血病细胞系 Jurkat 中 IL-2受体的诱导和 IL-2的产生。
T83847 SP-A (196-215) (human) TFA

Surfactant Protein A,SPA4

表面活性蛋白A(SP-A)(196-215)是一种合成肽,与人类SP-A的C末端碳水化合物识别域的196至215氨基酸序列相对应。当浓度为1和10 µM时,它能抑制JAWSII鼠树突细胞中由LPS诱导的TNF-α释放。SP-A(196-215)(75 µM)促使JAWSII细胞吞噬P. aeruginosa。通过气管内给药,SP-A(196-215)(50 µg/动物)降低了小鼠P. aeruginosa感染模型的疾病严重程度和肺部形成菌落数。
T71933 GNE-3500

GNE-3500 is a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist. Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory diseases such as psoriasis and rheumatoid arthritis. GNE-3500 poss...
T70538 PD-85639

PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membr...
T35855 AAA

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...
T36241 Arecaidine propargyl ester (hydrobromide)

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.2Arecai...
T83911 CYY292

CYY292是一种针对PDGFRα、PDGFRβ、FGFR1、-2和-3的抑制剂(IC50分别为5.35、4.6、28、28和78 nM)。该化合物对这些激酶的选择性高于FGFR4(IC50 > 1,000 nM),但也能抑制c-Kit、VEGFR2、VEGFR1和胰岛素样生长因子1受体(IGF-1R;IC50分别为67、33、36和75 nM),以及EGFR、布鲁顿酪氨酸激酶(BTK)、细胞周期依赖性激酶4(Cdk4)/cyclin D3和MET(IC50分别为128、198、214和396 nM)。CYY292抑制MG-63、U2OS、MNNG/HOS和Saos-2骨肉瘤细胞的增殖(IC50分别为0.84、0.76、1.36和0.72 µM)。在0.3和0.5 µM的浓度下,它抑制U87MG和LN-229胶质母细胞瘤细胞的迁移和侵袭。CYY292(30 mg/kg)在U87MG原位小鼠异种移植模型中降低肿瘤体积并增加生存率。
T35671 Salazinic Acid

Salazinic acid is a depsidone lichen metabolite that has been found in P. sulcata.1 It is active against B. cereus, B. subtilis, S. aureus, P. aeruginosa, S. typhimurium, C. albicans, and A. niger in vitro (MICs = 3.9-30.8 mM). Salazinic acid is cytotoxic to MM98, A431, and HaCaT cells in crystal violet (EC50s = 159, 2,870, and 48 μM, respectively) and neutral red uptake assays (EC50s = 1,925, 1,913, and 907 μM, respectively).2 It increases the wound closure rate in scratch-wounded HaCaT monolay...
T37187 D-erythro/L-threo Lysosphingomyelin (d18:1)

D-erythro/L-threo Lysosphingomyelin (d18:1)

Lysosphingomyelin is an endogenous bioactive sphingolipid and a constituent of lipoproteins.1,2It is produced by the removal of the acyl group from sphingomyelin by a deacylase and acts as a precursor in the biosynthesis of sphingosine-1-phosphate . D-erythroLysosphingomyelin is an agonist of the S1P receptors S1P1, S1P2, and S1P3(EC50s = 167.7, 368.1, and 482.6 nM, respectively, for the human receptors).3It is also an agonist of the orphan receptor ovarian cancer G protein-coupled receptor 1 (O...

化合物

C75
Cat.No: T10657
Synonym: C-75
Target: Fatty Acid Synthase
trans-C75
Cat.No: T10656
Synonym: (±)-C75,反-4-羧基-5-辛基-3-甲基-丁内酯
Target: Others, Fatty Acid Synthase
CHMFL-ABL/KIT-155
Cat.No: T10801
Synonym: CHMFL-ABL-KIT-155
Target: c-Kit
C-HEGA-8
Cat.No: TF0100
Synonym:
Target:
N-Myristoyl-Lys-Arg-Thr-Leu-Arg
Cat.No: T76185
Synonym:
Target:
SP-A (196-215) (human) TFA
Cat.No: T83847
Synonym: Surfactant Protein A,SPA4
Target:
GNE-3500
Cat.No: T71933
Synonym:
Target:
PD-85639
Cat.No: T70538
Synonym:
Target:
AAA
Cat.No: T35855
Synonym:
Target:
Arecaidine propargyl ester (hydrobromide)
Cat.No: T36241
Synonym:
Target:
CYY292
Cat.No: T83911
Synonym:
Target:
Salazinic Acid
Cat.No: T35671
Synonym:
Target:
D-erythro/L-threo Lysosphingomyelin (d18:1)
Cat.No: T37187
Synonym: D-erythro/L-threo Lysosphingomyelin (d18:1)
Target:
Cat. No. Product Name Target Signaling Pathways
TN2014 Ophiopogonanone C

Others Others
Ophiopogonanone C是一种天然产物,属于百合科沿阶草属,其产品编号为 TN2014,CAS号为 477336-75-7。Ophiopogonanone C可用作对照参考。
T35779 Oosporein

Oosporein is a mycotoxin that has been found inBeauveriaand has diverse biological activities.1,2It is cytotoxic to Sf9 and Sf21 insect cells with 50% cytotoxic concentration (CC50) values of 4.23 and 10.43 μM, respectively.3Oosporin induces lethality in day-old cockerels (LD50= 6.12 mg/kg).4It inhibits Na+/K+-, Ca2+-, and Mg2+-ATPase activities by 27, 52, and 100%, respectively, in equine erythrocyte ghosts when used at a concentration of 200 μg/ml.2Oosporein inhibits herpes simplex 1 (HSV-1), ...
T35624 Ajoene

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 &#181g/ml) and Gram-negative bacteria (MICs = 136-200 &#181g/ml), as well as yeasts (MICs = 10-20 &#181g/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 &#181M), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 &#181M).2It reduces...

天然产物

Ophiopogonanone C
Cat.No: TN2014
Synonym:
Target: Others
Oosporein
Cat.No: T35779
Synonym:
Target:
Ajoene
Cat.No: T35624
Synonym:
Target:
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