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MedKoo Cat#: 463481 | Name: PLHSpT

Description:

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

PLHSpT is a Plk1 PBD-specific phosphopeptide inhibitor, effectively inhibiting mitotic progression and cell proliferation.

Chemical Structure

PLHSpT
PLHSpT
CAS#1186496-84-3

Theoretical Analysis

MedKoo Cat#: 463481

Name: PLHSpT

CAS#: 1186496-84-3

Chemical Formula: C24H40N7O11P

Exact Mass: 633.2523

Molecular Weight: 633.60

Elemental Analysis: C, 45.50; H, 6.36; N, 15.48; O, 27.78; P, 4.89

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
PLHSpT;
IUPAC/Chemical Name
N-L-prolyl-L-leucyl-L-histidyl-L-seryl-O-phosphono-L-threonine
InChi Key
WXGBWHLFXXMZRD-PFFQMSPKSA-N
InChi Code
InChI=1S/C24H40N7O11P/c1-12(2)7-16(28-20(33)15-5-4-6-26-15)21(34)29-17(8-14-9-25-11-27-14)22(35)30-18(10-32)23(36)31-19(24(37)38)13(3)42-43(39,40)41/h9,11-13,15-19,26,32H,4-8,10H2,1-3H3,(H,25,27)(H,28,33)(H,29,34)(H,30,35)(H,31,36)(H,37,38)(H2,39,40,41)/t13-,15+,16+,17+,18+,19+/m1/s1
SMILES Code
[C@@H](CC1=CN=CN1)(NC([C@@H](NC(=O)[C@@H]2CCCN2)CC(C)C)=O)C(N[C@H](C(N[C@@H]([C@H](OP(=O)(O)O)C)C(O)=O)=O)CO)=O
Appearance
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 DMSO
Shelf Life
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 633.60 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.

Recalculate based on batch purity %
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
1: Alverez CN, Park JE, Toti KS, Xia Y, Krausz KW, Rai G, Bang JK, Gonzalez FJ, Jacobson KA, Lee KS. Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1. J Med Chem. 2020 Nov 25;63(22):14087-14117. doi: 10.1021/acs.jmedchem.0c01669. Epub 2020 Nov 11. PMID: 33175530. 2: Li Z, Zhang Z, Sun H, Xu L, Jiang C. Identification of novel peptidomimetics targeting the polo-box domain of polo-like kinase 1. Bioorg Chem. 2019 Oct;91:103148. doi: 10.1016/j.bioorg.2019.103148. Epub 2019 Jul 27. PMID: 31376784. 3: Zhao XZ, Tsuji K, Hymel D, Burke TR Jr. Development of Highly Selective 1,2,3-Triazole-containing Peptidic Polo-like Kinase 1 Polo-box Domain-binding Inhibitors. Molecules. 2019 Apr 16;24(8):1488. doi: 10.3390/molecules24081488. PMID: 31014020; PMCID: PMC6515314. 4: Kim KU, Lee JH, Lee MY, Chae CH, Lee JH, Lee BH, Oh KS. DITMD-induced mitotic defects and apoptosis in tumor cells by blocking the polo-box domain-dependent functions of polo-like kinase 1. Eur J Pharmacol. 2019 Mar 15;847:113-122. doi: 10.1016/j.ejphar.2019.01.032. Epub 2019 Jan 25. PMID: 30689997. 5: Hymel D, Grant RA, Tsuji K, Yaffe MB, Burke TR Jr. Histidine N(τ)-cyclized macrocycles as a new genre of polo-like kinase 1 polo-box domain-binding inhibitors. Bioorg Med Chem Lett. 2018 Oct 15;28(19):3202-3205. doi: 10.1016/j.bmcl.2018.08.018. Epub 2018 Aug 19. PMID: 30174151; PMCID: PMC6287497. 6: Abdullah M, Guruprasad L. Structural insights into the inhibitor binding and new inhibitor design to Polo-like kinase-1 Polo-box domain using computational studies. J Biomol Struct Dyn. 2019 Aug;37(13):3410-3421. doi: 10.1080/07391102.2018.1515663. Epub 2018 Nov 1. PMID: 30146942. 7: Chan CF , Lan R , Tsang MK , Zhou D , Lear S , Chan WL , Cobb SL , Wong WK , Hao J , Wong WT , Wong KL . Directional Plk1 inhibition-driven cell cycle interruption using amphiphilic thin-coated peptide-lanthanide upconversion nanomaterials as in vivo tumor suppressors. J Mater Chem B. 2015 Apr 7;3(13):2624-2634. doi: 10.1039/c4tb02104e. Epub 2015 Feb 25. PMID: 32262910. 8: Kim SM, Chae MK, Lee C, Yim MS, Bang JK, Ryu EK. Enhanced cellular uptake of a TAT-conjugated peptide inhibitor targeting the polo-box domain of polo-like kinase 1. Amino Acids. 2014 Nov;46(11):2595-603. doi: 10.1007/s00726-014-1798-8. Epub 2014 Aug 24. PMID: 25151148. 9: Kim SM, Yoon SM, Yim MS, Cho G, Ryu EK. Targeted delivery of a phosphopeptide prodrug inhibits the proliferation of a human glioma cell line. Amino Acids. 2013 Nov;45(5):1149-56. doi: 10.1007/s00726-013-1570-5. Epub 2013 Aug 2. PMID: 23907439. 10: Murugan RN, Park JE, Lim D, Ahn M, Cheong C, Kwon T, Nam KY, Choi SH, Kim BY, Yoon DY, Yaffe MB, Yu DY, Lee KS, Bang JK. Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1. Bioorg Med Chem. 2013 May 1;21(9):2623-34. doi: 10.1016/j.bmc.2013.02.020. Epub 2013 Feb 27. PMID: 23498919; PMCID: PMC7561269. 11: Qian WJ, Park JE, Lee KS, Burke TR Jr. Non-proteinogenic amino acids in the pThr-2 position of a pentamer peptide that confer high binding affinity for the polo box domain (PBD) of polo-like kinase 1 (Plk1). Bioorg Med Chem Lett. 2012 Dec 15;22(24):7306-8. doi: 10.1016/j.bmcl.2012.10.093. Epub 2012 Oct 27. PMID: 23159568; PMCID: PMC3530200. 12: Leung K. 68Ga-1,4,7-Triazacyclononane-1,4,7-triacetic acid-c(RGDyK)-S-S-CPLHSpT. 2012 Aug 14 [updated 2012 Oct 25]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 23115806. 13: Kim SM, Yoon S, Choi N, Hong KS, Murugan RN, Cho G, Ryu EK. In vivo tumor imaging using polo-box domain of polo-like kinase 1 targeted peptide. Biomaterials. 2012 Oct;33(29):6915-25. doi: 10.1016/j.biomaterials.2012.06.046. Epub 2012 Jul 15. PMID: 22795848. 14: Liu F, Park JE, Qian WJ, Lim D, Scharow A, Berg T, Yaffe MB, Lee KS, Burke TR Jr. Peptoid-Peptide hybrid ligands targeting the polo box domain of polo-like kinase 1. Chembiochem. 2012 Jun 18;13(9):1291-6. doi: 10.1002/cbic.201200206. Epub 2012 May 8. PMID: 22570300; PMCID: PMC4536914. 15: Liu F, Park JE, Qian WJ, Lim D, Scharow A, Berg T, Yaffe MB, Lee KS, Burke TR Jr. Identification of high affinity polo-like kinase 1 (Plk1) polo-box domain binding peptides using oxime-based diversification. ACS Chem Biol. 2012 May 18;7(5):805-10. doi: 10.1021/cb200469a. Epub 2012 Feb 14. PMID: 22292814; PMCID: PMC3355227. 16: Liu F, Park JE, Qian WJ, Lim D, Gräber M, Berg T, Yaffe MB, Lee KS, Burke TR Jr. Serendipitous alkylation of a Plk1 ligand uncovers a new binding channel. Nat Chem Biol. 2011 Jul 17;7(9):595-601. doi: 10.1038/nchembio.614. PMID: 21765407; PMCID: PMC3158281.