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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:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
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

 		98+%
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 +

BRD3, IC50: 0.25 μM

BRD4, IC50: 0.5 μM

 		98%
Molibresib +++

BET proteins, IC50: 35 nM

 		99%+
I-BRD9 +++

BRD4, pIC50: 5.3

BRD9, pIC50: 7.3

 		99%+
BI-7273 ++++

BRD7, IC50: 117 nM

BRD9, IC50: 19 nM

 		97%
Pelabresib +++

BRD4-BD1, IC50: 39 nM

 		98%
ARV-825 +++

BRD4 BD1, Kd: 90 nM

BRD4 BD2, Kd: 28 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 ++++

BRD9, Kd: 5.9 nM

BRD7, Kd: 73 nM

 		++

CECR2, Kd: 77 nM

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

FL-BRD4, IC50: 5 nM

 		99%+
PLX51107 ++++

BRD3 BD1, Kd: 2.1 nM

BRD4 BD2, Kd: 1.7 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 ++++

Brd2(BD2), Kd: 62 nM

Brd3(BD2), Kd: 13 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 BD2, IC50: 32 nM

BRD4 BD1, IC50: 27 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 95%
ODM-207 ✔ 98%
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%
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 +

L3MBTL3, IC50: 35 μM

L3MBTL4, IC50: 6 μM

 		99%
PFI-3 +++

SMARCA2A, Kd: 72 nM

SMARCA4, Kd: 55 nM

 		99%+
UNC1215 +++

L3MBTL3, IC50: 120 nM

L3MBTL3- D274A, IC50: 3.5 μM

 		99%+
EED226 ++

PRC2, Kd: 114 nM

EED, Kd: 82 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 ++

BRPF2, IC50: 7.9 μM

BRPF1, IC50: 80 nM

 		99%+
OF-1 ++

BRPF1B, Kd: 100 nM

BRPF2, Kd: 500 nM

 		99%+
GSK-5959 ++

BRPF3, pIC50: 7.1

BRPF2, pIC50: 5.2

 		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

 		99%
I-CBP112 ++

CBP, Kd: 151 nM

p300, Kd: 167 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 ✔ IGF-1R,HER2 99%+
Curcumin +

p300, IC50: ~25 μM

 		NF-κB,Nrf2,Ferroptosis 98%
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

 		99%
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 细胞实验

Cell Line
Concentration Treated Time Description References
Patched mutant tumor cells 0.15 nM - 1.5 µM 48 hours To evaluate the inhibitory effect of CCT129202 on tumor cell proliferation, results showed significant inhibition of tumor cell proliferation. Cancer Res. 2013 Oct 15;73(20):6310-22.
SUM-149 cells 25 nM 7 days Inhibited PLK1 activity, significantly reduced cell viability Mol Oncol. 2015 Feb;9(2):527-43.
HeLa cells 1 µM 2 h Inhibit PLK1 activity and observe cell behavior in prometaphase Sci Signal. 2011 Nov 8;4(198):rs12.
HeLa cells 0.1 μM 45 min To study the effect of PLK1 inhibitor on HeLa cells, observed downregulation of PLK1 substrates and upregulation of ATM and ATR substrates. Nature. 2023 Jan;613(7945):759-766.
hESPL1flox/Δ cells 25 or 200 nM 3 h To test the critical role of Plk1 in the cell cycle, it was found that Plk1 activity in late G2 or early M phase is essential for centriole disengagement and duplication Dev Cell. 2009 Sep;17(3):344-54.
SUM-149 cells 25 nM 7 days To evaluate the inhibitory effect of BI 2536 on PLK1 and its impact on cell growth, results showed that SUM-149 cells were more sensitive to BI 2536 than MCF-10A cells. Mol Oncol. 2015 Feb;9(2):527-43.
bone marrow-derived dendritic cells (BMDCs) 1 µM 2 or 4 h BI 2536 specifically abrogates transcription of antiviral genes without affecting inflammatory genes following stimulation with LPS, poly(I:C), or Pam3CSK4. Cell. 2011 Nov 11;147(4):853-67.
Human pulmonary arterial smooth muscle cells (hPASMCs) 50 nM 24 h To investigate the effect of BI 2536 on apoptosis in hPASMCs, results showed that BI 2536 significantly induced apoptosis in hPASMCs. Respir Res. 2023 Aug 19;24(1):204.
LNCaP cells 10 nM - 100 nM 24 h To investigate the effects of BI 2536 on LNCaP cells, results showed that Pim1-overexpressing cells were more sensitive to the inhibitory effects of BI 2536, exhibiting more mitotic arrest and apoptosis. Clin Cancer Res. 2014 Jun 15;20(12):3211-21.

BI 2536 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice LS174T colon cancer cell xenograft model Gavage 30 mg/kg twice a week Twice a week, for 11 days Synergistically inhibited tumor growth Mol Cancer Ther. 2021 Oct;20(10):1893-1903
Mice VSV infection model Intravenously 500 µg 3 hours before and 2 hours after infection BI 2536 inhibits antiviral cytokine mRNA production, while increasing viral replication during in vivo VSV infection. Cell. 2011 Nov 11;147(4):853-67.
Mice Hypoxia-induced pulmonary hypertension model Tail vein injection 50 mg/kg Once per week for 4 weeks To investigate the therapeutic effect of BI 2536 on hypoxia-induced pulmonary hypertension, results showed that BI 2536 significantly reduced right ventricular systolic pressure (RVSP) and right ventricular hypertrophy (RV/LV + S). Respir Res. 2023 Aug 19;24(1):204.
Nude mice Pim1-overexpressing prostate cancer xenograft model Intravenous injection 25 mg/kg Twice a week for three weeks To investigate the effects of BI 2536 on Pim1-overexpressing prostate cancer xenograft models, results showed that BI 2536 dramatically inhibited the growth of Pim1-overexpressing tumors and induced more mitotic arrest and apoptosis. Clin Cancer Res. 2014 Jun 15;20(12):3211-21.

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 521.65
SMILES Code O=C(NC1CCN(C)CC1)C2=CC=C(NC(N=C3N(C4CCCC4)[C@@H]5CC)=NC=C3N(C)C5=O)C(OC)=C2
MDL No. MFCD10565924
别名
运输蓝冰
InChI Key XQVVPGYIWAGRNI-JOCHJYFZSA-N
Pubchem ID 11364421
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

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 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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