T83949
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DC 432是一种强效的N-terminal methyltransferase 1/2 (NTMT1/2) (IC50= 54 nM)肽模拟抑制剂,含有BM30肽和额外五个精氨酸残基。在HCT116细胞中,DC 432处理能够降低调节染色体凝缩1和SET蛋白的N端甲基化水平。该化合物具有细胞渗透性。 |
T68332
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AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular assays show that both Aurora A and Aurora B are inhibited at inhibitor concentrations sufficient to block proliferation. Importantly, the cellular activity translates to potent inhibition of tumor growth in vivo. An oral dose of 5 mg/kg QD is well tolerated and results in near stasis (92% TGI) in an HCT116 mouse xenograft model. |
T62331
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Autophagy-IN-1 是一种有效的细胞自噬 (autophagy) /线粒体自噬 (mitophagy) 抑制剂,能够阻断癌细胞内自噬体-溶酶体融合,并同时选择性地提高自噬通量发挥作用。Autophagy-IN-1 能够阻滞细胞周期,并诱导细胞凋亡 (apoptosis)。Autophagy-IN-1 在 HCT116 小鼠异种移植瘤模型中明显抑制肿瘤生长,且毒性低。Autophagy-IN-1 能够用于研究结直肠癌。 |
T79724
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IGF2BP1-IN-1(Compound A11)是一款高效的IGF2BP1抑制剂,对IGF2BP1蛋白有很强的结合能力,KD值仅为2.88 nM。该化合物能显著抑制A549和HCT116癌细胞株的增殖,IC50值分别为9 nM和34 nM,且能诱导癌细胞发生凋亡。此外,IGF2BP1-IN-1在A549异种移植小鼠模型中有效抑制了肿瘤生长。 |
T35668
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Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC50 = 13 μM) and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells (IC50 = 1.75 nM). Neoaureothin is cytotoxic to A549, HCT116, and HepG2 cells (IC50s = 34.3, 47, and 37.2 μg/ml, respectively). It also has nematocidal activity against the pine wood nematode B. xylophilus (LC50 = 0.84 μg/ml) and increases survival of P. densiflora trees inoculated with B. xylophilus. |
T83713
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DC432是一种细胞内可渗透的肽类抑制剂,针对N-末端Xaa-Pro-Lys N-甲基转移酶1 (NTMT1; IC50 = 0.054 µM)。该化合物与NTMT1和NTMT2有结合作用(Kds分别为0.3和1 µM),并在10和50 µM的浓度下,通过细胞外实验抑制NTMT1对调节染色体凝缩1 (RCC1) N-末端二甲基化。DC432(100 µM)在HCT116细胞中减少了RCC1 SPKRIA基序的三甲基化。 |
T36815
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Chevalone C is a meroterpenoid fungal metabolite originally isolated from E. chevalieri. It is active against M. tuberculosis H37Ra (MIC = 6.3 μg/ml) and is cytotoxic to BC1 human breast cancer cells (IC50 = 8.7 μg/ml). Chevalone C inhibits the growth of multidrug-resistant isolates of E. coli, S. aureus, and E. faecium in a disc diffusion assay when used at a concentration of 15 μg/disc. It also induces cell death in HCT116 colorectal carcinoma cells. |
T83855
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TG2-179-1是BRCA1相关蛋白1(BAP1)的抑制剂。它在25 µM至1.5 mM的浓度范围内,通过无细胞测定法抑制BAP1的去泛素化活性。TG2-179-1对八种结肠癌细胞系表现出细胞毒性(IC50s = 4.48-7.52 µM)。在体内,TG2-179-1(10和30 mg/kg)能够减少HCT116结肠癌小鼠异种移植模型中的肿瘤体积。 |
T83881
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4-(3,4-Difluorobenzo)curcumin(CDF)是一种具有抗寄生虫和抗癌活性的半合成香豆素。它能减少被T. gondii持鞭毛体和无鞭毛体感染的Vero细胞的数量(EC50s分别为0.8和0.37 µM)。CDF(4和8 µM)通过增强5-氟尿嘧啶和奥沙利铂对化药抵抗性HCT116细胞主要和次要结肠球形成的抑制作用。 |
T36471
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Ternatin is a cyclic heptapeptide first isolated from the mushroom C. versicolor that has been shown to have cytotoxic and anti-adipogenic effects in vitro. It inhibits adipogenesis with an IC50 value of 27 nM and becomes cytotoxic to 3T3-L1 mouse adipocytes at 10-fold higher concentrations. Ternatin is reported to inhibit HCT116 cell proliferation with an IC50 value of 71 nM. Note that this metabolite should not be confused with the plant flavonoid of the same name. |