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BI 2536 {[allProObj[0].p_purity_real_show]}

货号：A203461

BI 2536是一种PLK1和BRD4的双重抑制剂，对它们的IC50分别为0.83 nM和25 nM。BI-2536还抑制IFNB基因转录。

BI 2536 化学结构 CAS号：755038-02-9
BI 2536 化学结构
CAS号：755038-02-9
BI 2536 3D分子结构
CAS号：755038-02-9
BI 2536 化学结构 CAS号：755038-02-9
BI 2536 3D分子结构 CAS号：755038-02-9
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BI 2536 纯度/质量文件 产品仅供科研

货号：A203461 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 BET ↓ bromodomain ↓ BRPF ↓ CBP/beta-catenin ↓ p300/CBP ↓ 其他靶点 纯度
MS436 ++

BRD4 (2), Ki: 0.34 μM

BRD4 (1), Ki: <0.085 μM

 		99%+
CPI-203 +++

BRD4, IC50: 37 nM

 		99+%
GSK1324726A +++

BRD2, IC50: 31 nM

BRD4, IC50: 22 nM

 		99%+
PFI-1 ++

BRD2, IC50: 98 nM

BRD4, IC50: 0.22 μM

 		98%
Apabetalone +

BD2, IC50: 0.51 μM

 		99%
(+)-JQ1 +++

BRD4 (2), IC50: 33 nM

BRD4 (1), IC50: 77 nM

 		98%
I-BET151 +

BRD4, IC50: 0.5 μM

BRD3, IC50: 0.25 μM

 		98%
Molibresib +++

BET proteins, IC50: 35 nM

 		99%+
I-BRD9 +++

BRD9, pIC50: 7.3

BRD4, pIC50: 5.3

 		99%+
BI-7273 ++++

BRD7, IC50: 117 nM

BRD9, IC50: 19 nM

 		99+%
Pelabresib +++

BRD4-BD1, IC50: 39 nM

 		98%
ARV-825 +++

BRD4 BD2, Kd: 28 nM

BRD4 BD1, Kd: 90 nM

 		99%+
Birabresib 99%+
BI 2536 +++

BRD4, Kd: 37 nM

 		c-Myc 99%+
Bromosporine ++

BRD2, IC50: 0.29 μM

BRD9, IC50: 0.122 μM

 		++++

CECR2, IC50: 17 nM

 		99%+
XMD8-92 ++

BRD4 (1), Kd: 170 nM

 		99%+
Mivebresib ✔ 99%+
BI-9564 ++++

BRD7, Kd: 73 nM

BRD9, Kd: 5.9 nM

 		++

CECR2, Kd: 77 nM

 		98%
AZD5153 6-Hydroxy-2-naphthoic acid ++++

FL-BRD4, IC50: 5 nM

 		99%+
PLX51107 ++++

BRD4 BD2, Kd: 1.7 nM

BRD3 BD1, Kd: 2.1 nM

 		99%+
FL-411 +

BRD4(1), IC50: 0.43 μM

 		99%+
ABBV-744 ✔ 99%+
dBET6 ++++

BRD4, IC50: 14 nM

 		99%+
dBET1 ++++

BRD4, IC50: 20 nM

 		99%+
MZ1 ++++

Brd3(BD2), Kd: 13 nM

Brd2(BD2), Kd: 62 nM

 		99%+
dBET57 +

BRD4BD1, DC50: 500 nM

 		99%+
SF2523 +

BRD4, IC50: 241 nM

 		DNA-PK 99%+
INCB054329 ++++

BRD3-BD1, IC50: 9 nM

BRD4-BD1, IC50: 119 nM

 		99%
INCB-057643 ✔ 99%+
(E/Z)-ZL0420 +++

BRD4 BD1, IC50: 27 nM

BRD4 BD2, IC50: 32 nM

 		99%+
BMS-986158 ✔ 99%+
BRD4 Inhibitor-10 ++++

BRD4-BD2, IC50: 41 nM

BRD4-BD1, IC50: 5 nM

 		97%
A1874 ✔ 99%+
Y06036 ++

BRD4 (1), Kd: 82 nM

 		99%+
Alobresib ✔ NF-κB 98%
ODM-207 ✔ 99%
GSK778 +++

BRD2-BD1, IC50: 75nM

BRD4-BD1, IC50: 143 nM

 		97%
SRX3207 +

BRD41, IC50: 3070 nM

BRD42, IC50: 3070 nM

 		Syk 98%
GSK046 +++

BRD3BD2, IC50: 98 nM

BRD4BD2, IC50: 214 nM

 		98%
GSK620 ✔ 97%
Thalidomide-NH-C4-NH-Boc ✔ 98%
Trotabresib ✔ 99%
NHWD-870 ✔ 98%
CFT8634 ++++

BRD9, DC50: 3 nM

 		98%
GSK2801 ++

BAZ2B, Kd: 136 nM

BAZ2A, Kd: 257 nM

 		99%+
KG-501 ✔ 99%+
UNC 669 +

L3MBTL4, IC50: 6 μM

L3MBTL3, IC50: 35 μM

 		98%
PFI-3 +++

SMARCA4, Kd: 55 nM

SMARCA2A, Kd: 72 nM

 		99%+
UNC1215 +++

L3MBTL3- D274A, IC50: 3.5 μM

L3MBTL3, IC50: 120 nM

 		99%+
EED226 ++

EED, Kd: 82 nM

PRC2, Kd: 114 nM

 		99%+
BRD9539 ✔ 98%
UNC926 +

L3MBTL1, Kd: 3.9 μM

 		99%
666-15 ++

CREB, IC50: 81 nM

 		99%+
UNC6852 +

EED, IC50: 247 nM

 		98%
BAZ1A-IN-1 +

BAZ1A, Kd: 0.52 μM

 		99%+
PFI-4 ++

BRPF1, IC50: 80 nM

BRPF2, IC50: 7.9 μM

 		99%+
OF-1 ++

BRPF2, Kd: 500 nM

BRPF1B, Kd: 100 nM

 		99%+
GSK-5959 ++

BRPF2, pIC50: 5.2

BRPF3, pIC50: 7.1

 		99%
GSK6853 ++++

BRPF1, pIC50: 8.1

 		99%+
NI-42 ++++

BRPF3, IC50: 260 nM

BRPF1, IC50: 48 nM

 		99%+
E-7386 +++

CBP/beta-catenin, IC50: 0.0484 μM

 		97%
I-CBP112 ++

p300, Kd: 167 nM

CBP, Kd: 151 nM

 		98+%
Histone Acetyltransferase Inhibitor II +

p300, IC50: 5 μM

 		98%
C646 +

p300/CBP, Ki: 400 nM

 		99%+
Anacardic Acid +

PCAF, IC50: 5 μM

p300/CBP, IC50: 8.5 μM

 		99%+
SGC-CBP30 ++++

EP300, IC50: 38 nM

CREBBP, IC50: 21 nM

 		99%+
Nordihydroguaiaretic acid ✔ HER2,IGF-1R 99%+
Curcumin +

p300, IC50: ~25 μM

 		Nrf2,Ferroptosis,NF-κB 98%
PF-CBP1 HCl ++

CREBBP, IC50: 125nM

p300/CBP, IC50: 363nM

 		97%
CPI-637 +++

EP300, IC50: 0.051 μM

CBP, IC50: 0.03 μM

 		99%+
Foscenvivint ✔ β-catenin 99%+
A-485 ++

p300 HAT, IC50: 0.06 μM

 		99%+
GNE-781 +

BRD4(1), IC50: 5100 nM

 		++++

CBP, IC50: 0.94 nM

 		98%
NEO2734 +++

BET, IC50: <30 nM

 		+++

p300/CBP, IC50: <30 nM

 		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。
产品名称 PLK1 ↓ PLK2 ↓ PLK3 ↓ PLK4 ↓ 其他靶点 纯度
HMN-214 ✔ 99%+
SBE13 HCl ++++

PLK1, IC50: 200 pM

 		98%
Onvansertib +++

PLK1, IC50: 2 nM

 		99%+
Volasertib ++++

PLK1, IC50: 0.87 nM

 		97%
GSK461364 +++

PLK1, Ki: 2.2 nM

 		99%+
MLN0905 +++

PLK1, IC50: 2 nM

 		99%+
Ro3280 ++

PLK1, IC50: 3 nM

 		99%
(E/Z)-Rigosertib sodium +

PLK1, IC50: 9 nM

 		+

PLK2, IC50: 260 nM

 		Bcr-Abl 99%+
BI 2536 ++++

PLK1, IC50: 0.83 nM

 		++

PLK2, IC50: 3.5 nM

 		+

PLK3, IC50: 9.0 nM

 		99%+
CFI-400945 ++

PLK4, IC50: 2.8 nM

 		Tie-2 98%
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。

BI 2536 生物活性

靶点

  • BET

    BRD4, Kd:37 nM

  • PLK2

    PLK2, IC50:3.5 nM

  • PLK3

    PLK3, IC50:9.0 nM

  • PLK1

    PLK1, IC50:0.83 nM
描述 Polo-like kinase 1 (Plk1) is a serine/theonin-specific kinase that regulates multiple stages during mitotic progression and acts as a negative prognostic marker in different types of human cancers. BI-2536 is a Plk1 inhibitor that blocks human Plk1 with an IC50 value of 0.83 nM. It also inhibits the activities of Plk2 and Plk3 with IC50 values of 3.5 nM and 9.0 nM, respectively. Accumulated 4N DNA content was observed in HeLa-S3 cells treated by BI-2536 (10 nM – 1 μM) for 24 hours, indicating a blockage of cell-cycle. When HeLa cells synchronized at the G1/S transition were treated with 60 nM BI-2536, cells released into median progressed through S phase normally followed by the G2/M arrest. In hTERT-RPE1 cells treated by BI-2536 (100 nM), nearly 70% of mitotic cells demonstrated a typical “Polo” phenotype. Intravenous injection of BI-2536 (40 – 50 mg/kg, once or twice/week) for 20 - 30 days inhibited the growth of HCT 116 tumor xenografts in immunodeficient, nu/nu mice. In a more rigorous xenograft model of larger HCT 116 tumors, 5 cycles of BI-2536 (50 mg/kg, twice weekly on two consecutive days) efficiently induced tumor regressions compared to control mice. In addition, four to seven cycles of BI-2536 (50 mg/kg, twice weekly on two consecutive days) also inhibited tumor growth in BxPC-3 and A549 xenograft models with T/C values of 5% and 14%, respectively. BI-2536 also inhibited the growth of NCI-H460 lung carcinomas, increased mitotic index and histone H3 phosphorylation in nu/nu mice)[3].
作用机制 BI-2536 is derived from a chemical series, the dihydro-pteridinones, and functions as an ATP-competitive inhibitor for Plk1[3].

BI 2536 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
5637 Growth Inhibition Assay IC50=45.47 nM 23792639
697 Growth Inhibition Assay IC50=0.01668 μM SANGER
697 Growth Inhibition Assay 24 h IC50=2107.1 nM 24519995
697 Growth Inhibition Assay 48 h IC50=305.3 nM 24519995

BI 2536 动物研究

Dose Nude Mice: 40 mg/kg - 50 mg/kg[3] (i.v.); 10 mg/kg, 20 mg/kg[4] (i.p.)
Administration i.v., i.p.

BI 2536 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00526149 Breast Cancer ... 展开 >> Endometrial Cancer Head and Neck Cancer Melanoma (Skin) Ovarian Cancer Sarcoma 收起 << Phase 2 Completed - Belgium ... 展开 >> U.Z. Gasthuisberg Leuven, Belgium, B-3000 收起 <<
NCT00710710 Pancreatic Neoplasms Phase 2 Completed - Austria ... 展开 >> 1216.10.43001 Boehringer Ingelheim Investigational Site Wien, Austria Germany 1216.10.49013 Boehringer Ingelheim Investigational Site Celle, Germany 1216.10.49009 Boehringer Ingelheim Investigational Site Düsseldorf, Germany 1216.10.49007 Boehringer Ingelheim Investigational Site Essen, Germany 1216.10.49001 Boehringer Ingelheim Investigational Site Freiburg/Breisgau, Germany 1216.10.49005 Boehringer Ingelheim Investigational Site Hamburg, Germany 1216.10.49010 Boehringer Ingelheim Investigational Site Herne, Germany 1216.10.49008 Boehringer Ingelheim Investigational Site München, Germany 1216.10.49003 Boehringer Ingelheim Investigational Site Stuttgart, Germany 1216.10.49002 Boehringer Ingelheim Investigational Site Ulm, Germany 收起 <<
NCT00412880 Carcinoma, Small Cell Phase 2 Completed - United States, Arkansas ... 展开 >> 1216.11.007 Boehringer Ingelheim Investigational Site Fayetteville, Arkansas, United States United States, Illinois 1216.11.003 Boehringer Ingelheim Investigational Site Chicago, Illinois, United States 1216.11.006 Boehringer Ingelheim Investigational Site Evanston, Illinois, United States United States, Massachusetts 1216.11.002 Boehringer Ingelheim Investigational Site Boston, Massachusetts, United States United States, Missouri 1216.11.005 Boehringer Ingelheim Investigational Site St. Louis, Missouri, United States United States, North Carolina 1216.11.001 Boehringer Ingelheim Investigational Site Chapel Hill, North Carolina, United States United States, South Carolina 1216.11.011 Boehringer Ingelheim Investigational Site Charleston, South Carolina, United States 1216.11.010 Boehringer Ingelheim Investigational Site Greenville, South Carolina, United States United States, Washington 1216.11.012 Boehringer Ingelheim Investigational Site Seattle, Washington, United States Canada, Alberta 1216.11.009 Alberta Cancer Board Edmonton, Alberta, Canada 收起 <<

BI 2536 参考文献

[1]17(4):316-22.

BI 2536 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.92mL

0.38mL

0.19mL

9.58mL

1.92mL

0.96mL

19.17mL

3.83mL

1.92mL

BI 2536 技术信息

CAS号755038-02-9
分子式C28H39N7O3
分子量 521.654
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 65 mg/mL(124.6 mM)，配合低频超声助溶，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

0.1 M HCL: 25 mg/mL(47.92 mM)，配合低频超声，并调节pH至4
动物实验配方

5%DMSO+40%PEG300+5%Tween80+50%water 12.5 mg/mL

Tags: BI 2536 | 755038-02-9 | BI2536 | BI-2536 | PLK1 Inhibitor | Cell Cycle/DNA Damage | Epigenetics | Apoptosis | Polo-like Kinase (PLK) | Epigenetic Reader Domain | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | BI 2536 纯度/质量文件 | BI 2536 亚型比较 | BI 2536 生物活性 | BI 2536 细胞研究 | BI 2536 动物研究 | BI 2536 临床数据 | BI 2536 参考文献 | BI 2536 实验方案 | BI 2536 技术信息

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