上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
OTS964
OTS964 是一种口服有效的，高亲和力和选择性的 TOPK 抑制剂，IC50 为 28 nM。OTS964 也是一种有效的细胞周期蛋白依赖激酶 CDK11 抑制剂，结合 CDK11B 的 Kd 值为 40 nM。
OTS964 Chemical Structure
CAS No. : 1338542-14-5
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
OTS964 的其他形式现货产品:
OTS964 hydrochloride
| 生物活性 |
OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM[1]. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM[2].
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| IC50 & Target[1][2] |
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CDK11B
40 nM (Kd)
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TOPK
28 nM (IC50)
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体外研究
(In Vitro) |
OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation[1].
OTS964 (10 nM; 48 hours) increases cancer cell death[1].
OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
| Cell Line: |
LU-99 cells |
| Concentration: |
10 nM |
| Incubation Time: |
48 hours |
| Result: |
Suppressed cancer cell proliferation. |
Apoptosis Analysis[1]
| Cell Line: |
LU-99 cells |
| Concentration: |
10 nM |
| Incubation Time: |
48 hours |
| Result: |
Increased cancer cell death. |
Western Blot Analysis[3]
| Cell Line: |
Hs683 cells, H4 cells |
| Concentration: |
0.1, 1, 2 μM |
| Incubation Time: |
24 and 48 hours |
| Result: |
Increased the expression of LC3-II and decreased the expression of P62, both in a dose-dependent manner. |
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体内研究
(In Vivo) |
OTS964 (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression[1].
OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Nude mice bearing LU-99 lung cancer cells[1] |
| Dosage: |
40 mg/kg |
| Administration: |
Intravenously; on days 1, 4, 8, 11, 15, and 18 |
| Result: |
The tumors continued shrinking even after the treatment and finally revealed complete regression. |
| Animal Model: |
Nude mice bearing LU-99 lung cancer cells[1] |
| Dosage: |
50 or 100 mg/kg |
| Administration: |
Oral administration; once every day for 2 weeks |
| Result: |
Achieved complete tumor regression. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Matsuo Y , et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancerthrough inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145.
[2]. Lin A, et al. Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials. Sci Transl Med. 2019 Sep 11;11(509).
[3]. Lu H, et al. TOPK inhibits autophagy by phosphorylating ULK1 and promotes glioma resistance to TMZ. Cell Death Dis. 2019 Aug 5;10(8):583.
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