2. Metabolic Enzyme/Protease Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. E1/E2/E3 Enzyme Microtubule/Tubulin Apoptosis Caspase
  4. BKT300

BKT300 是一种强效且选择性的胞质分裂蛋白调节因子 1 (PRC1) 抑制剂。BKT300 可抑制 PRC1 在 T481 位点的去磷酸化，破坏肌动蛋白与微管 (microtubule) 的形成，诱导 G2/M 期细胞周期阻滞，引发有丝分裂灾难，并促进细胞凋亡 (apoptosis)，从而抑制急性髓系白血病 (AML) 细胞的增殖与迁移，同时对正常细胞无明显影响。BKT300 可抑制小鼠异种移植 AML 模型中的肿瘤生长。BKT300 可用于 AML 的相关研究[1]。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

BKT300

BKT300 Chemical Structure

CAS No. : 2551033-16-8

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

BKT300 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BKT300 is a potent and selective protein regulator of cytokinesis 1 (PRC1) inhibitor. BKT300 inhibits PRC1 dephosphorylation at T481, disrupts actin and microtubule formation, induces G2/M cell cycle arrest, triggers mitotic catastrophe, and promotes apoptosis, thereby inhibiting proliferation and migration of acute myeloid leukemia (AML) cells while sparing normal cells. BKT300 inhibits tumor growth in mouse xenograft AML models. BKT300 can be used for the research of AML[1].

IC50 & Target[1]

PRC1

 

Caspase-3

 

体外研究
(In Vitro)

BKT300 与重组 PRC1 结合，其 Kd 值在 SPR 分析中为 28.3 nM，在 MST 分析中 Kd 值为 104 nM[1]。
BKT300 (31.25-5000 nM；3 h) 可抑制 U937 和 Jurkat 细胞向 CXCL12 的迁移，以及 THP-1 细胞向 MCP-1 的迁移[1]。
BKT300 (62.5-500 nM；24 h) 可剂量依赖性地抑制 U937 细胞中的肌动蛋白丝形成，但对正常外周血单个核细胞 (PBMCs) 无此作用[1]。
BKT300 (1 µM; 24 h) 可破坏 U937 细胞中的微管组织与形成[1]。
BKT300 (7.8-5000 nM；2-24 h) 在 U937、MV4-11、OCI-AML-2、OCI-AML-3、Molm14 和 Marimo 急性髓系白血病 (AML) 细胞中诱导 G2/M 期阻滞和细胞死亡[1]。
BKT300 (3.9-1000 nM；24 h) 可在 U937 细胞中诱导剂量依赖性凋亡，并伴随活化型 caspase-3 表达水平升高[1]。
BKT300 (50-1000 nM；24 h) 可在 U937 和 MV4-11 细胞中下调 CDC25C、上调 p21，并以剂量/时间依赖性方式诱导 PRC1 在 T481 位点的磷酸化[1]。
BKT300 (31.2-500 nM；24 h) 可上调 U937 细胞中 pPRC1 (T481) 的水平，但对正常 PBMCs 无此作用[1]。
BKT300 (24 h) 可抑制 OCI-AML-3、Marimo、OCI-AML-2、MOLM-14、U937、K562、MV4-11 和 HL-60 细胞增殖，其 IC50 值分别为 107、135、120、122、27、98、98 和 110 nM[1]。

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

BKT300 相关抗体:

Cell Cycle Analysis[1]

Cell Line: U937 cells
Concentration: 19.5, 39, 62.5, 78, 156, 313, 625, 1250, 2500, 5000 nM
Incubation Time: 24 h; 2, 4, 6, 8, 24 h (at 62.5 nM)
Result: Induced G2/M cell cycle arrest in U937 cells, in a dose- and time-dependent manner.
Induced cell death in U937 cells at 62.5 nM.

Cell Cycle Analysis[1]

Cell Line: OCI-AML-2, OCIAML-3, Molm14, Marimo
Concentration: 250 nM
Incubation Time: 24 h
Result: Induced G2/M cell cycle arrest in all tested cells.

Apoptosis Analysis[1]

Cell Line: U937 cells
Concentration: 3.9, 7.8, 15.6, 31.25, 62.5, 125, 250, 500, 1000 nM
Incubation Time: 24 h
Result: Increased apoptotic cells in U937 cells in a dose-dependent manner.

Cell Migration Assay [1]

Cell Line: U937, Jurkat, and THP-1 leukemic cells
Concentration: 31.25, 62.5, 125, 250, 500, 1000 nM (U937 and THP1 cells); 125, 250, 500, 1000, 5000 nM (Jurkat cells)
Incubation Time: 3 h
Result: Significantly inhibited the migration of U937 cells and Jurkat cells toward CXCL12 in a dose-dependent manner.
Inhibited the migration of AML THP-1 cells toward monocyte chemotactic protein-1 (MCP-1) in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: U937, REH, NB4, MV4-11cells
Concentration: 50, 100, 1000 nM (U937 cells); 1000 nM (REH, NB4, MV4-11cells)
Incubation Time: 24 h
Result: Increased cleaved caspase-3 levels in U937 cells in a dose-dependent manner.
Increased cleaved caspase-3 levels in U937, REH, NB4, MV4-11cells at 1000 nM.

Western Blot Analysis[1]

Cell Line: U937, MV4-11 leukemic cell lines
Concentration: 50 nM, 100 nM, 1000 nM (24 h CDC25C/p21); 100 nM, 500 nM, 1000 nM (24 h pPRC1); 1000 nM (pPRC1 time course)
Incubation Time: 24 h (CDC25C/p21, pPRC1 dose-response); 4 h, 24 h (pPRC1 time course)
Result: Downregulated CDC25C and upregulated p21 in U937/MV4-11 cells without affecting CDC2/cyclin B1.
Induced a dose-dependent increase in PRC1 phosphorylation at T481 within 4 h, peaking at 24 h, without altering total PRC1 levels.

Immunofluorescence[1]

Cell Line: U937 cells, normal PBMCs
Concentration: 31.2, 62.5, 125, 250, 500 nM
Incubation Time: 24 h
Result: Induced a dose-dependent increase in pPRC1 (T481) levels in U937 cells.
Had no effect on pPRC1 or total PRC1 levels in normal PBMCs.
体内研究
(In Vivo)

BKT300 (1-2.5 mg/只小鼠；皮下注射；第 3 天至第 7 天每日 1 次) 在 U937 异种移植小鼠模型中抑制肿瘤生长[1]。
BKT300 (2.5 mg/只小鼠；皮下注射；第 10 天至第 12 天每日 2 次) 在 U937 异种移植小鼠模型中可抑制肿瘤生长并诱导肿瘤消退[1]。
BKT300 (2.5 mg/只小鼠；皮下注射；第 12 至 16 天及第 19 至 20 天给药) 可降低 MV4-11 静脉异种移植小鼠模型血液和骨髓中的 AML 细胞水平[1]。

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

Animal Model: NOD scid gamma (NSG) mice (6-8-week-old) subcutaneously injected with U937 cells[1]
Dosage: 1, 1.5, 2, 2.5 mg/mouse
Administration: s.c.; once daily from day 3 to day 7
Result: Achieved 98% tumor growth inhibition, with 6/7 treated mice exhibiting complete tumor growth inhibition by day 11.
Induced apoptosis of tumor cells.
Decreased CDC25C and increased pPRC1 T481 expression in the tumors.
Animal Model: NOD scid gamma (NSG) mice (6-8-week-old) subcutaneously injected with U937 cells[1]
Dosage: 2.5 mg/mouse
Administration: s.c.; twice daily from day 10 to day 12
Result: Reached 95.9% tumor growth inhibition and 89.4% tumor regression by day 17.
Showed no effect on body weight.
Animal Model: NOD scid gamma (NSG) mice (6-8-week-old) intravenously injected with MV4-11 cells[1]
Dosage: 2.5 mg/mouse
Administration: s.c.; on day 12 to day 16 and day 19 to day 20
Result: Reduced the percentage of AML cells in the blood by 74.8% and in bone marrow by 72%.
Increased the number of normal mouse cells in the bone marrow by 2-fold and in blood by 7-fold compared to control mice.
分子量

399.44

Formula

C22H25NO6
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

BKT300 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

BKT3002551033-16-8BKT 300BKT-300E1/E2/E3 EnzymeMicrotubule/TubulinApoptosisCaspaseE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseProtein regulator of cytokinesis 1actinapoptosisAML cellsmitotic catastrophecaspase-3 pathwaymouse xenograft AML modelsmicrotubulePRC1G2/M cell cycle arrestInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
BKT300
目录号：
HY-179466
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z