1. Cell Cycle/DNA Damage Apoptosis
  2. TOPK Apoptosis
  3. OTS514 hydrochloride

OTS5144 hydrochloride 是一种高效的 TOPK 抑制剂,IC50 为 2.6 nM。OTS514 hydrochloride 强效抑制 TOPK 阳性的肿瘤细胞生长。OTS514 hydrochloride 诱导细胞周期停滞和凋亡 (apoptosis)。

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OTS514 hydrochloride Chemical Structure

OTS514 hydrochloride Chemical Structure

CAS No. : 2319647-76-0

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OTS514 hydrochloride 的其他形式现货产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells[1]. OTS514 hydrochloride induces cell cycle arrest and apoptosis[2].

IC50 & Target

IC50: 2.6 nM (TOPK)[1]

体外研究
(In Vitro)

OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138+ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1)
Concentration: 1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM
Incubation Time: 72 hours
Result: IC50 values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, was resistant.
体内研究
(In Vivo)

OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells[1]
Dosage: 1, 2.5, and 5 mg/kg
Administration: Intravenously treated; once every day for 2 weeks
Result: Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.
分子量

400.92

Formula

C21H21ClN2O2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
OTS514 hydrochloride
目录号:
HY-18621A
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