5-FAM-PMDM6

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5-FAM-PMDM6
Details
5-carboxyfluorescein-labeled PMDM6 functional
peptide; HPLC ≥95%.
Related Documents: COA/MS/HPLC
report; fluorescent-peptide handling guide.
Category
Drug Peptides
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Description

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Description 5-FAM-PMDM6 is a 5-carboxyfluorescein conjugate of the PMDM6 functional peptide. 5-FAM (Ex/Em ~492/517 nm) suits fluorescence-polarization, confocal imaging or flow cytometry for target-affinity measurement and cellular-uptake/localization studies.
Structure type Linear peptide (PMDM6 backbone, 5-FAM-labeled)
Solubility Readily soluble in water/PBS; minor DMSO acceptable
Storage Powder, −20°C, dry, light-protected

 

Product Basic Information Table

 

Product Standard English Name Product Abbreviation / Alias Function Tags (comma-separated) Core Structure Molecular Formula Exact Mass (Da) Average MW (Da) Salt Form Length (aa)
5-FAM-PMDM6 (PMDM6-F), N-terminally 5-Carboxyfluorescein-Labeled MDM2-Binding Peptide 5-FAM-PMDM6; PMDM6-F; FAM-betaAla-betaAla-FM-Aib-pY-(6-Cl-W)-E-Ac3c-LN-NH2; 5-carboxyfluorescein-labeled MDM2-binding probe; p53-MDM2 interaction fluorescent probe fluorescent-labeled peptide, FAM label, MDM2-p53 interaction probe, p53 helix mimetic, competitive binding assay, anticancer drug screening, light-sensitive, non-natural residues Linear 11-residue backbone (with two beta-Ala linkers plus Aib, pTyr, 6-Cl-Trp, Ac3c and other non-coded residues); N-terminally conjugated to 5-FAM (5-carboxyfluorescein) via an amide bond to the first beta-Ala amine; C-terminal Asn amidated (-NH2); sequence: 5-FAM-betaAla-betaAla-Phe-Met-Aib-pTyr-(6-Cl-L-Trp)-Glu-Ac3c-Leu-Asn-NH2. PMDM6 is an MDM2-binding peptide mimetic designed from the p53 alpha-helical hot-spot (Phe19/Trp23/Leu26); side-chain modifications (6-Cl-Trp, Ac3c, Aib) stabilize the helix and enhance affinity; pTyr carries a phosphate group (P, O); contains 1 Met (oxidation-prone); 5-FAM is a green fluorophore (lambda_ex~492 nm/lambda_em~518 nm) and is light-sensitive. C84H96ClN14O24PS 1782.59 1784.23 Free peptide (C-terminal Asn-NH2 amidated); N-terminal 5-FAM label; contains phosphotyrosine; CAS not publicly listed 11

 

Physicochemical Solubility & Storage Parameters

 

Product Code Appearance Long-term Storage Short-term Storage Solution Stability Solid Powder Stability
PEP-FAMPMDM6-01 Light yellow to yellow solid (FAM fluorescein pigment) Store at -80°C, sealed, desiccated, protected from light (amber tube / aluminum foil wrap), ~2 years; at -20°C ~1 year; strongly recommend aliquoting to avoid repeated freeze-thaw. Contains Met (oxidation-prone) and FAM (light-sensitive)-must be kept dry, dark, and under inert gas. 2-8°C, protected from light, for ~1-2 weeks; working aliquots at -80°C, protected from light; ship on dry ice, protected from light. Recommended to prepare stock in fresh DMSO (100 mg/mL ~ 56 mM; sonicate to aid dissolution; hygroscopic DMSO significantly impacts solubility-use freshly opened DMSO), then dilute into neutral buffer (PBS/HEPES pH 7.4) to working concentration. In solution: -80°C protected from light for 6 months; -20°C protected from light for 1 month; prepare fresh, aliquot, and avoid repeated freeze-thaw. Protect FAM fluorescence from light throughout (aluminum foil wrap); Met is oxidation-prone-avoid air/strong oxidants; pTyr may dephosphorylate under strong acid/base. Uses: MDM2 competitive fluorescence-binding assays (FAM channel tracing); IC50/Ki determination of MDM2-p53 interaction inhibitors (Nutlin-class small molecules, stapled peptides, SAR405838, idasanutlin); HTS screening by fluorescence polarization (FP) or time-resolved FRET. solid stable ~2 years at -80°C, sealed, desiccated, protected from light; contains FAM (light-sensitive), Met (oxidizable), and pTyr (phosphate ester)-must be stored dark, dry, under argon/nitrogen; aliquot immediately upon receipt into single-use portions to avoid moisture uptake and oxidation.

 

Functional Description

 

Product Code Frontend Short Summary Detailed Biological Function Description Applicable Research Areas (comma-separated) Targets / Pathways
PEP-FAMPMDM6-01 N-terminally 5-FAM fluorescent-labeled MDM2-binding peptide probe (a p53 helix mimetic with betaAla-betaAla linker, Aib, pTyr, 6-Cl-Trp, Ac3c non-natural residues and C-terminal Asn-NH2); used for MDM2-p53 interaction competitive fluorescence-binding / FP / FRET assays and MDM2 antagonist screening; light-sensitive, store at -80°C. MDM2 (mouse double minute 2 homolog; HDM2 in human) is an E3 ubiquitin ligase that directly binds the N-terminal transactivation domain of the tumor suppressor p53, inhibiting p53 transcriptional activity and mediating its ubiquitin-dependent degradation. In approximately 50% of human tumors, MDM2 is overexpressed, leading to functional p53 inactivation-making MDM2 a classic anti-cancer drug target. Native p53 inserts an amphipathic alpha-helix (residues 17-29; hot-spot residues Phe19-Trp23-Leu26) into a deep hydrophobic pocket of MDM2. PMDM6 is a non-natural-amino-acid-modified peptide mimetic designed from the p53 helical hot-spot: a betaAla-betaAla hydrophilic N-terminal linker, backbone Aib (alpha-aminoisobutyric acid, a helix promoter) and Ac3c (1-aminocyclopropane-1-carboxylic acid, a conformational constraint) stabilize the helical conformation, while Phe, Met, pTyr, (6-Cl)-Trp and Leu reproduce the p53 Phe19/Trp23/Leu26 hot-spot; Glu and Leu-Asn-NH2 form the C-terminus. N-terminal 5-FAM (5-carboxyfluorescein, lambda_ex~492 nm/lambda_em~518 nm) labeling yields PMDM6-F (i.e., 5-FAM-PMDM6), which retains nanomolar MDM2 binding and serves as a highly sensitive fluorescent tracer for MDM2-binding studies. Main applications: (1) saturation binding of MDM2 protein by fluorescence polarization (FP) or time-resolved FRET (TR-FRET); (2) competitive binding assays with unlabeled PMDM6 or native p53 peptide (p53 17-29) to determine Ki/IC50 of small-molecule MDM2 antagonists (Nutlin-3a, RG7112, SAR405838/MI-888, idasanutlin, etc.); (3) HTS screening of MDM2-p53 interaction inhibitors; (4) validation of stapled peptides (e.g., ATSP-7041/ALRN-6924A) for dual MDM2/MDMX binding. **Critical notes**: the peptide contains the light-sensitive FAM group, oxidation-prone Met, and acid/base-labile pTyr phosphate-must be handled under reduced light, stored at -80°C sealed/dry/inert gas, dissolved in fresh DMSO, aliquoted, and kept away from repeated freeze-thaw, strong reductants and oxidants. MDM2-p53 interaction, p53 helix-mimetic peptide, anti-cancer drug screening, MDM2 antagonists (Nutlin-class / stapled peptides), fluorescence polarization (FP) / TR-FRET binding assays, HTS fluorescent probes, protein-protein interaction (PPI) research MDM2 (HDM2) hydrophobic groove (p53-binding pocket; hot-spot Phe19/Trp23/Leu26); homologous MDMX (MDM4) pocket (partial cross-binding); FAM fluorescence channel lambda_ex/em ~ 492/518 nm

 

 

 

 

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