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|---|---|---|---|---|---|---|---|
| {[ item.pr_size ]} |
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{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} |
{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} | 现货 | 1周 咨询 | - + |
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| 产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBI-0206965 |
+++
ULK2, IC50: 711 nM ULK1, IC50: 108 nM |
95% | |||||||||||||||||
| Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
| Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
| PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
| MRT68921 HCl |
++++
ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM |
99%+ | |||||||||||||||||
| ROC-325 | ✔ | 99%+ | |||||||||||||||||
| Autophinib |
+++
Autophagy, IC50: 40 nM |
99% | |||||||||||||||||
| Lys05 | ✔ | 99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Autophagy is an evolutionarily conserved mechanism of lysosomal proteolysis that is used for the turnover of organelles and proteins with long half-lives and also functions to generate alternative sources of metabolic fuel via nutrient recycling under stress conditions[3]. ROC-325 is a novel inhibitor of autophagy. Treatment with ROC-325 results in a significant loss of acridine orange fluorescence. ROC-325 triggers a highly significant increase in cathepsin D (CTSD) levels. ROC-325 treatment yields pharmacodynamic effects that are consistent with inhibition of autophagy. Treatment with 5 μM ROC-325 for 24 hours leads to the formation of LC3B punctae and a robust increase in LC3B levels in both A498 and 786-0 RCC cells. Immunoblotting analysis conducted in both A498 and 786-0 cells demonstrates that ROC-325 promotes a dose-dependent increase in LC3B expression in a manner that correlated with a corresponding increase in the levels of p62 and cathepsin D[3]. ROC-325 is well tolerated and no notable toxicities are observed other than a very modest, nonsignificant reduction in mean body weight at the highest dose. Immunohistochemical analysis of specimens collected from animals treated with ROC-325 demonstrates significant, dose-dependent increases in the autophagic markers LC3B and p62 and increases apoptosis[3]. |
| Dose | Mice: 25 mg/kg - 50 mg/kg[1] (p.o.) |
| Administration | p.o. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.94mL 1.99mL 0.99mL |
19.88mL 3.98mL 1.99mL |
|
| CAS号 | 1859141-26-6 |
| 分子式 | C28H27ClN4OS |
| 分子量 | 503.06 |
| SMILES Code | O=C1C2=C(SC3=C1C=CC=C3)C(C)=CC=C2NCCN(CCNC4=CC=NC5=CC(Cl)=CC=C45)C |
| MDL No. | MFCD31619252 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | HXUYKEGAEIYPKY-UHFFFAOYSA-N |
| Pubchem ID | 129626603 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 4 mg/mL(7.95 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
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