PTBP1-RNA-binding inhibitor P6 TFA
Based on 1 Customer Validation
PTBP1-RNA-binding inhibitor (PTBP1 α3-helix derived peptide) P6 TFA is a cell-permeable PTBP1 inhibitor. PTBP1-RNA-binding inhibitor P6 TFA binds to the α3 helix binding site of the PTBP1 RRM1 domain, and disrupts the synergistic RNA-binding effect of the RRM1 and RRM2 domains of PTBP1. PTBP1-RNA-binding inhibitor P6 (TFA) regulates the regulatory pattern of PTBP1-related alternative splicing events, and thus exhibits anticancer potential.
For research use only. We do not sell to patients.
- Purity: 98.59%
- Formula: C73H122N22O19.xC2HF3O2
- Molecular Weight:1597.86 (free base)
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Storage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All DNA/RNA Synthesis Isoforms
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Biological Activity
PTBP1[1]
PTBP1-RNA-binding inhibitor P6 (TFA) potently inhibits PTBP1 RRM12-RNA-2 binding with a Ki of 9.3 μM, shows no activity against single-domain PTBP1 constructs, helix-disrupted PTBP1 mutants, or non-target RRM-containing proteins hnRNP A2/B1 and SRSF1[1].
PTBP1-RNA-binding inhibitor P6 (TFA) binds directly to PTBP1 RRM1 with a Kd of 18.6 μM, and binds PTBP1 RRM12-L151G with similar affinity[1].
PTBP1-RNA-binding inhibitor P6 (TFA) binds PTBP1 RRM1 with a Kd of 98.1 μM and PTBP1 RRM12-L151G with a Kd of 44.5 μM[1].
PTBP1-RNA-binding inhibitor P6 (TFA) (20 hours) exhibits high cell permeability in HEK293T cells with an EC50 of 35 nM, exceeding the permeability of a positive control cell-penetrating peptide[1].
PTBP1-RNA-binding inhibitor P6 (TFA) (up to 24 hours) is stable in HEK293T cell lysate, with 43% remaining intact after 24 hours, showing greater stability than linear and monocyclic analogs[1].
PTBP1-RNA-binding inhibitor P6 (TFA) (100-300 μM) significantly increases PTBP2 exon 10 inclusion in HEK293T cells at concentrations of 100 μM and 300 μM, without affecting cell viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 1597.86 (free base)
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Formula C73H122N22O19.xC2HF3O2
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Color White to off-white
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Synonyms
PTBP1 α3-helix derived peptide P6 TFA
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Sequence
Ac-Asn-Gln-{S5}-Arg-Ala-Gln-{B5}-Ala-Leu-Gln-{R5}-Val-Asn-NH2
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Sequence Shortening
Ac-NQ-{S5}-RAQ-{B5}-ALQ-{R5}-VN-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL
* "≥" means soluble, but saturation unknown.
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PTBP1-RNA-binding inhibitor P6 TFA Related Classifications
HY-P5960 Related Classifications
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