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BI 2536

Catalog No.: A10134

PLK inhibitor

BI 2536

BI 2536 Chemical Structure

CAS NO. 755038-02-9

BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.

Availability: In stock

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5 mg
10 mg
50 mg
100 mg
10mM * 1mL in DMSO
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Warning Products are for laboratory research use only. Not for human use. We do not sell to patients.
  • Kei K Ito, .et al. Cep57 and Cep57L1 maintain centriole engagement in interphase to ensure centriole duplication cycle, J Cell Biol, 2021, Mar 1;220(3):e202005153 PMID: 33492359
  • Ryuzaburo Yuki, .et al. The tyrosine kinase v-Src modifies cytotoxicities of anticancer drugs targeting cell division, J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
  • Yamagishi A, .et al. Targeting Insulin-Like Growth Factor 1 Receptor Delays M-Phase Progression and Synergizes with Aurora B Inhibition to Suppress Cell Proliferation, Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
  • Bucko PJ, .et al. Subcellular drug targeting illuminates local kinase action, Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
  • Watanabe K, .et al. The Cep57-pericentrin module organizes PCM expansion and centriole engagement, Nat Commun, 2019, Feb 25;10(1):931 PMID: 30804344
  • Valérian Pasche, .et al. Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni, Parasit Vectors, 2018, 11: 298 PMID: 29764454
  • Takeshi Wakida, .et al. The CDK-PLK1 axis targets the DNA damage checkpoint sensor protein RAD9 to promote cell proliferation and tolerance to genotoxic stress, eLife, 2017, 6: e29953 PMID: 29254517
  • Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
  • Ifuji A, .et al. A novel immunofluorescence method to visualize microtubules in the antiparallel overlaps of microtubule-plus ends in the anaphase and telophase midzone, Exp Cell Res, 2017, Nov 15;360(2):347-357 PMID: 28942021

Biological Activity

BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.
Target Value
PLK1IC50: 0.83nM
PLK2IC50: 3.5nM
PLK3IC50: 9.0nM
PI3KαIC50: 2.407μM
MetIC50: 4.754μM
Tie-2IC50: 6.549μM
HGFRIC50: 9.5μM
ErbB4IC50: 9.908μM
AblIC50: >10μM
AxlIC50: >10μM
AMPKIC50: >10μM
AuroraAIC50: >10μM
AuroraBIC50: >10μM
βIRKIC50: >10μM
B-RafIC50: >10μM
BTKIC50: >10μM
CDK1/CyclinB1IC50: >10μM
CDK2/CyclinEIC50: >10μM
Chk1IC50: >10μM
CK1IC50: >10μM
CK2IC50: >10μM
C-RafIC50: >10μM
CSKIC50: >10μM
DYRK1AIC50: >10μM
ECKIC50: >10μM
ERK2IC50: >10μM
FGFR1IC50: >10μM
FGFR3IC50: >10μM
FLT1IC50: >10μM
FLT3IC50: >10μM
GSK-3βIC50: >10μM
HekIC50: >10μM
HER2IC50: >10μM
ITKIC50: >10μM
JAK2IC50: >10μM
JAK3IC50: >10μM
JNK1IC50: >10μM
LCKIC50: >10μM
LynIC50: >10μM
MEK1IC50: >10μM
MSK1IC50: >10μM
MKK1IC50: >10μM
NEK6IC50: >10μM
p38αIC50: >10μM
p38βIC50: >10μM
p38γIC50: >10μM
p38δIC50: >10μM
PAK2IC50: >10μM
PDGFRαIC50: >10μM
PDGFRβIC50: >10μM
PDK-1IC50: >10μM
PKAIC50: >10μM
PKBαIC50: >10μM
PKBβIC50: >10μM
PKCαIC50: >10μM
PRAKIC50: >10μM
RETIC50: >10μM
ROCK2IC50: >10μM
RONIC50: >10μM
S6KIC50: >10μM
SGKIC50: >10μM
SrcIC50: >10μM
SykIC50: >10μM
In vitro (25°C) DMSO 21 mg/mL (40.25 mM)
Water Insoluble
Ethanol 98 mg/mL (187.86 mM)
In vivo 30% PEG 400+0.5% Tween 80+5% Propylene glycol 14 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 19.17 mL 95.84 mL 191.68 mL
0.5 mM 3.83 mL 19.17 mL 38.34 mL
1 mM 1.92 mL 9.58 mL 19.17 mL
5 mM 0.38 mL 1.92 mL 3.83 mL

*The above data is based on the productmolecular weight 521.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A10134
Actions Inhibitor
CAS No. 755038-02-9
Formula C28H39N7O3
M. Wt 521.7
Purity >98%
Synonyms BI2536, BI-2536
SMILES CC[[email protected]@H]1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C

Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for 36 months.
In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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