Research Area
Product Type
United States ( Change Country )
BI 2536 Chemical Structure
TAK-960
TAK-960 is a novel, potent and selective PLK1 inhibitor with a minimal IC50 of 8 nM.
ON-01910
ON-01910 (Estybon, Novonex, Rigosertib) is a non-ATP-competitive inhibitor to Polo-like kinase 1 (PLK1) with IC50 of 9 nM.
HMN-214
HMN-214 is a potent PLK1 inhibitor an average IC50 of 0.12 μM.
BI6727 (Volasertib)
BI 6727 is a highly potent Polo-like kinase inhibitor with an IC50 of 0 .87 nM.
ABT-888 (Veliparib)
ABT-888 (Veliparib) is a potent poly (ADP-ribose) polymerase (PARP) inhibitor of PARP-1 and PARP-2 with Ki of 5.2 nM and 2.9 nM, respectively.
Olaparib (AZD2281)
Olaparib(AZD2281, KU0059436) is a selective inhibitor of PARP-1 and PARP-2 enzymes with IC50 of 5 nM and 1 nM, respectively.
Y-27632 2HCl
Y-27632 2HCl is ROCK inhibitor, as a novel bronchodilator. Y27632 is available with IC50 of 3.3±0.25 μM and 2.8±0.2 μM in human and rabbit tissues, respectively.
Rucaparib (AG-014699 , PF-01367338)
AG-014699 (Rucaparib, PF-01367338) is an inhibitor of PARP with a Ki of 1.4 nM.
PD 0332991 HCl
PD 0332991 is a highly selective inhibitor of Cdk4/cyclin D1 and Cdk6/cyclin D2 with IC50 of 11 nM and 16 nM, respectively.
Biological Activity
BI 2536 is a small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1, derived from human, mouse and rat) (with IC50of 0.83 nM), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible tumor cell populations.[1] Plk1, a serine/threonine-protein kinase, is a key regulator of multiple processes fundamental to mitosis and cell division.
This compound showed a more than 1000-fold selectivity relative to a panel of 63 other protein kinases, but it also affected the activities of Plk2 at an IC50 of 3.5 nM and, to a slightly lesser extent, the activity of Plk3 (IC50 9.0 nM).[1]
The half-maximal effective concentration (EC50) values in a panel of 32 human cancer cell lines ranged 2–25 nM.[1]
BI 2536 inhibits growth of human tumor xenografts in nude mice and induces regression of large tumors with well-tolerated intravenous dose regimens.[1]
References on BI 2536
- [1] Current Biology February 20, 2007;17：316–322
Product Information
| Molecular Weight (WM): | 521.66 |
|---|---|
| Formula: | C28H39N7O3 |
| CAS No.: | 755038-02-9 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥104mg/mL |
| Water <1mg/mL | |
| Ethanol ≥104mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
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Selleck's high quality products have been used in several published research findings, including the following:
Formation of stable attachments between kinetochores and microtubules depends on the B56-PP2A phosphatase
Polo-Like Kinase 1 Is a Potential Therapeutic Target in Human Melanoma
Small Molecule Kinase Inhibitor Screen Identifies Polo-Like Kinase 1 as a Target for Neuroblastoma Tumor-Initiating Cells.
Targeting Mitotic Exit Leads to Tumor Regression In Vivo: Modulation by Cdk1, Mastl, and the PP2A/B55α,δ Phosphatase.
Integrative mRNA profiling comparing cultured primary cells with clinical samples reveals PLK1 and C20orf20 as therapeutic targets in cutaneous squamous cell carcinoma
Small RNA Sequencing and Functional Characterization Reveals MicroRNA-143 Tumor Suppressor Activity in Liposarcoma
SLAIN2 links microtubule plus end-tracking proteins and controls microtubule growth in interphase.
Systematic discovery of TLR signaling components delineates viral-sensing circuits.
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Plk-1 knockdown and inhibition by BI 2536 and viability of human melanoma cell lines M14 and WM-115 as demonstrated by MTT assay. Experiments were performed in triplicate. One representative experiment is shown. *Po0.001, ANOVA test with Tukey’s post-test. ANOVA, analysis of variance; MTT, 3-(4,5 dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; Plk-1, polo-like kinase 1; siRNA, small-interfering RNA; WB, western blot. - Plk-1 knockdown and inhibition by BI 2536 and viability of human melanoma cell lines M14 and WM-115 as demonstrated by MTT assay. Experiments were performed in triplicate. One representative experiment is shown. *Po0.001, ANOVA test with Tukey’s post-test. ANOVA, analysis of variance; MTT, 3-(4,5 dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; Plk-1, polo-like kinase 1; siRNA, small-interfering RNA; WB, western blot.
Data from [J Invest Dermatol 2011 September;131:1886–1895] BI 2536 purchased from Selleck
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(a,b) RPE1 cells transfected with control or either of two B56-PP2A siRNA pools (1, 2) were incubated in MG132 (10 M, 15 min), followed by the addition of BI2536 (40 nM) or DMSO for 45 min. (a) The frequency of mitotic cells with few or absent cold-stable K-bres . (b) Maximum-intensity projection of tubulin (green) and an overlay with kinetochores (CREST, red) in B56-PP2A-siRNA (pool 2) cells treated with DMSO or BI2536 (40 nM). Insets are 3 enlargement of the optical sections spanning the outlined centromeres. - (a,b) RPE1 cells transfected with control or either of two B56-PP2A siRNA pools (1, 2) were incubated in MG132 (10 M, 15 min), followed by the addition of BI2536 (40 nM) or DMSO for 45 min. (a) The frequency of mitotic cells with few or absent cold-stable K-bres . (b) Maximum-intensity projection of tubulin (green) and an overlay with kinetochores (CREST, red) in B56-PP2A-siRNA (pool 2) cells treated with DMSO or BI2536 (40 nM). Insets are 3 enlargement of the optical sections spanning the outlined centromeres.
Data from [Nat Cell Biol 2011 August;13:1265-71] BI 2536 purchased from Selleck
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Comparison between Genetic Ablation of Cdc20 and Current Mitotic Drugs (C) Transformed Cdc20(lox/lox); RERT(+/Cre) MEFs were subcutaneously injected into the two flanks of SCID mice, and tumors were scored every 2–3 days.These mice were injected i.p. (three injections per week) with 4-OHT or mitotic drugs (taxol, vincristine, and BI2536) when tumors reached about 200 mm3 of volume (day 11; arrow) (n = 8 mice per group). (D) Representative images of these fibrosarcomas 3 days after injection with 4-OHT (to generate Cdc20(D/D) cells), BI2536, or taxol. These mice were injected with 10 mM BrdU to score DNA replication. CA3, immunodetection of active caspase 3. Scale bars, 50 or 10 mM (insets).
Comparison between Genetic Ablation of Cdc20 and Current Mitotic Drugs (C) Transformed Cdc20(lox/lox); RERT(+/Cre) MEFs were subcutaneously injected into the two flanks of SCID mice, and tumors were scored every 2–3 days.These mice were injected i.p. (three injections per week) with 4-OHT or mitotic drugs (taxol, vincristine, and BI2536) when tumors reached about 200 mm3 of volume (day 11; arrow) (n = 8 mice per group). (D) Representative images of these fibrosarcomas 3 days after injection with 4-OHT (to generate Cdc20(D/D) cells), BI2536, or taxol. These mice were injected with 10 mM BrdU to score DNA replication. CA3, immunodetection of active caspase 3. Scale bars, 50 or 10 mM (insets).
Data from [Cancer Cell 2010.December;18:641–654] BI 2536 purchased from Selleck
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Treatment with BI 2536 induces cell-cycle arrest in NB TICs and aberrant accumulation of cyclin B1 and p21. C, expression of cyclin B1 and p21 was assessed in NB88R2 following 16 and 24-hour treatment with different doses of BI 2536 (10, 30, and 100 nmol/L). ERK1 (extracellular signal regulated kinase 1) was used as the loading control. D, inhibition of PLK1 was assessed by in vitro kinase assay following treatment of NB88R2 for 3 hours with BI 2536.
Treatment with BI 2536 induces cell-cycle arrest in NB TICs and aberrant accumulation of cyclin B1 and p21. C, expression of cyclin B1 and p21 was assessed in NB88R2 following 16 and 24-hour treatment with different doses of BI 2536 (10, 30, and 100 nmol/L). ERK1 (extracellular signal regulated kinase 1) was used as the loading control. D, inhibition of PLK1 was assessed by in vitro kinase assay following treatment of NB88R2 for 3 hours with BI 2536.
Data from [Cancer Res 2011.February;71:1385-1395] BI 2536 purchased from Selleck
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Treatment with BI 2536 induces cell death via apoptosis. A,treatment with BI 2536 (10, 30, and 100 nmol/L) reduces viable cell numbers as assessed by trypan blue exclusion. B, representative Western blot demonstrating accumulation of cleaved PARP following treatment with 10 nmol/L BI 2536 .
Treatment with BI 2536 induces cell death via apoptosis. A,treatment with BI 2536 (10, 30, and 100 nmol/L) reduces viable cell numbers as assessed by trypan blue exclusion. B, representative Western blot demonstrating accumulation of cleaved PARP following treatment with 10 nmol/L BI 2536 .
Data from [Cancer Res 2011 February;71:1385-1395] BI 2536 purchased from Selleck
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BI 2536 inhibits NB tumor growth in vivo. A and B, NOD/SCID mice bearing 50- to100-mm3 tumors were injected intravenously with either vehicle (0.1N HCl per saline) or 12.5 to 25mg/kg BI 2536 for 2 consecutive days a week, for a total of 3 cycles.Two independent experiments were performed in each case with 5 animals per group. Representative tumor growth data are shown.
BI 2536 inhibits NB tumor growth in vivo. A and B, NOD/SCID mice bearing 50- to100-mm3 tumors were injected intravenously with either vehicle (0.1N HCl per saline) or 12.5 to 25mg/kg BI 2536 for 2 consecutive days a week, for a total of 3 cycles.Two independent experiments were performed in each case with 5 animals per group. Representative tumor growth data are shown.
Data from [Cancer Res 2011 February;71:1385-1395] BI 2536 purchased from Selleck
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animals with 50- to 100-mm3 tumors were randomized into 4 groups: group 1 injected intravenously with vehicle (0.1N HCl per saline), group 2 injected intravenously with 12.5 mg/kg of BI 2536 (2 consecutive days, 3 cycles), group 3 injected i.p. with 10 mg/kg of irinotecan (3 doses total, 3 days apart), and group 4 injected with BI 2536 and irinotecan. Both representative tumor growth data and a Kaplan–Meyer survival plot are shown.
animals with 50- to 100-mm3 tumors were randomized into 4 groups: group 1 injected intravenously with vehicle (0.1N HCl per saline), group 2 injected intravenously with 12.5 mg/kg of BI 2536 (2 consecutive days, 3 cycles), group 3 injected i.p. with 10 mg/kg of irinotecan (3 doses total, 3 days apart), and group 4 injected with BI 2536 and irinotecan. Both representative tumor growth data and a Kaplan–Meyer survival plot are shown.
Data from [Cancer Res 2011.February;71:1385-1395] BI 2536 purchased from Selleck
- I am very appreciating Selleck chem for providing reliable chemicals such as HDAC inhibitor LBH589 and PLK1 inhibitor BI2536. They worked well in my project.
Meng, XiangbingThe University of Iowa
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| Plk-1 knockdown and inhibition by BI 2536 and viability of human melanoma cell lines M14 and WM-115 as demonstrated by MTT assay. Experiments were performed in triplicate. One representative experiment is shown. *Po0.001, ANOVA test with Tukey’s post-test. ANOVA, analysis of variance; MTT, 3-(4,5 dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; Plk-1, polo-like kinase 1; siRNA, small-interfering RNA; WB, western blot. |
Data from [J Invest Dermatol 2011 September;131:1886–1895]
| (a,b) RPE1 cells transfected with control or either of two B56-PP2A siRNA pools (1, 2) were incubated in MG132 (10 M, 15 min), followed by the addition of BI2536 (40 nM) or DMSO for 45 min. (a) The frequency of mitotic cells with few or absent cold-stable K-bres . (b) Maximum-intensity projection of tubulin (green) and an overlay with kinetochores (CREST, red) in B56-PP2A-siRNA (pool 2) cells treated with DMSO or BI2536 (40 nM). Insets are 3 enlargement of the optical sections spanning the outlined centromeres. |
Data from [Nat Cell Biol 2011 August;13:1265-71]
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