SBE-13 | CAS#1052532-15-6 | PLK1 inhibitor

MedKoo Cat#: 406445 | Name: SBE-13 HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

SBE-13 is a potent and selective inhibitor of PLK1 and CDK1.

Chemical Structure

SBE-13 HCl

CAS#1052532-15-6

Theoretical Analysis

MedKoo Cat#: 406445

Name: SBE-13 HCl

CAS#: 1052532-15-6

Chemical Formula: C24H28Cl2N2O4

Exact Mass: 0.0000

Molecular Weight: 479.40

Elemental Analysis: C, 60.13; H, 5.89; Cl, 14.79; N, 5.84; O, 13.35

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 850.00	2 Weeks
200mg	USD 1,450.00	2 Weeks
500mg	USD 1,950.00	2 Weeks

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Related CAS #

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Synonym

SBE13; SBE 13; SBE13; SBE-13 HCl.

IUPAC/Chemical Name

N-(4-((6-chloropyridin-3-yl)methoxy)-3-methoxybenzyl)-2-(3,4-dimethoxyphenyl)ethanamine hydrochloride

InChi Key

QBGSVDJLQQXEGG-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H27ClN2O4.ClH/c1-28-20-7-4-17(12-22(20)29-2)10-11-26-14-18-5-8-21(23(13-18)30-3)31-16-19-6-9-24(25)27-15-19;/h4-9,12-13,15,26H,10-11,14,16H2,1-3H3;1H

SMILES Code

COC1=CC=C(CCNCC2=CC=C(OCC3=CC=C(Cl)N=C3)C(OC)=C2)C=C1OC.[H]Cl

Appearance

white solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

SBE-13 is an inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μ M for PLK1, PLK3 and PLK2 respectively).

In vitro activity:

SBE-13 effectively inhibited Plk1 activity without affecting other kinases such as Plk2, Plk3, and Aurora A. There was decreased cell proliferation, delayed progression through the cell cycle in lower SBE13 concentrations, a G(2)/M arrest using higher SBE-13 concentrations followed by apoptosis, and abnormal mitotic figures. Reference: Cell Cycle. 2010 Feb 15;9(4):761-73. https://pubmed.ncbi.nlm.nih.gov/20139717/

In vivo activity:

SBE-13 significantly reduced prostate smooth muscle contractions triggered by alpha-1 adrenergic stimulation in human prostate tissues. However, SBE-13 did not influence contractions induced by non-adrenergic agents such as endothelin-1 and U46619. Reference: Front Physiol. 2018 Jun 15;9:734. https://pubmed.ncbi.nlm.nih.gov/29962965/

	Solvent	mg/mL	mM
Solubility
	Water	5.0	10.43

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 479.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Lange L, Hemmerich P, Spänkuch B. Survival of primary, but not of cancer cells after combined Plk1-HDAC inhibition. Oncotarget. 2015 Sep 22;6(28):25801-14. doi: 10.18632/oncotarget.4445. PMID: 26317649; PMCID: PMC4694867. 2. Keppner S, Proschak E, Kaufmann M, Strebhardt K, Schneider G, Spänkuch B. Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010 Feb 15;9(4):761-73. doi: 10.4161/cc.9.4.10644. Epub 2010 Feb 16. PMID: 20139717. 3. Wang PC, Chen ST, Yang ZM. Effects of Aurora kinase A on mouse decidualization via Stat3-plk1-cdk1 pathway. Reprod Biol Endocrinol. 2021 Oct 29;19(1):162. doi: 10.1186/s12958-021-00847-5. PMID: 34715887; PMCID: PMC8557062. 4. Hennenberg M, Kuppermann P, Yu Q, Herlemann A, Tamalunas A, Wang Y, Rutz B, Ciotkowska A, Strittmatter F, Stief CG, Gratzke C. Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734. doi: 10.3389/fphys.2018.00734. PMID: 29962965; PMCID: PMC6013909.

In vitro protocol:

In vivo protocol:

1. Wang PC, Chen ST, Yang ZM. Effects of Aurora kinase A on mouse decidualization via Stat3-plk1-cdk1 pathway. Reprod Biol Endocrinol. 2021 Oct 29;19(1):162. doi: 10.1186/s12958-021-00847-5. PMID: 34715887; PMCID: PMC8557062. 2. Hennenberg M, Kuppermann P, Yu Q, Herlemann A, Tamalunas A, Wang Y, Rutz B, Ciotkowska A, Strittmatter F, Stief CG, Gratzke C. Inhibition of Prostate Smooth Muscle Contraction by Inhibitors of Polo-Like Kinases. Front Physiol. 2018 Jun 15;9:734. doi: 10.3389/fphys.2018.00734. PMID: 29962965; PMCID: PMC6013909.

1: Eckerdt F. Polo-like kinase 1 inhibitors SBE13 and BI 2536 induce different responses in primary cells. Cell Cycle. 2011 Apr 1;10(7):1027-8. Epub 2011 Apr 1. PubMed PMID: 21415595. 2: Posern G. Should I stall or should I cycle? An inhibitor for Polo-like Kinase 1 with distinct roles in primary cells. Cell Cycle. 2011 Apr 1;10(7):1029-30. Epub 2011 Apr 1. PubMed PMID: 21412046. 3: Keppner S, Proschak E, Schneider G, SpÃ¤nkuch B. Fate of primary cells at the G1/S boundary after polo-like kinase 1 inhibition by SBE13. Cell Cycle. 2011 Feb 15;10(4):708-20. Epub 2011 Feb 15. PubMed PMID: 21301227. 4: Eckerdt F. Freezing Polo in its sleep: targeting the inactive conformation of Polo-like kinase 1 in cancer cells. Cell Cycle. 2010 Mar 1;9(5):862. Epub 2010 Mar 1. PubMed PMID: 20348843. 5: Keppner S, Proschak E, Kaufmann M, Strebhardt K, Schneider G, SpÃ¤nkuch B. Biological impact of freezing Plk1 in its inactive conformation in cancer cells. Cell Cycle. 2010 Feb 15;9(4):761-73. Epub 2010 Feb 16. PubMed PMID: 20139717. 6: Liu X. SBE13 joins the family of Polo-like kinase 1 (Plk1) inhibitors. Cell Cycle. 2010 Feb 1;9(3):445-6. Epub 2010 Feb 1. PubMed PMID: 20130451. 7: Keppner S, Proschak E, Schneider G, SpÃ¤nkuch B. Identification and validation of a potent type II inhibitor of inactive polo-like kinase 1. ChemMedChem. 2009 Nov;4(11):1806-9. doi: 10.1002/cmdc.200900338. PubMed PMID: 19746360.