2. Epigenetics PROTAC
  3. Epigenetic Reader Domain PROTACs
  4. TAT-PiET-PROTAC

TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

TAT-PiET-PROTAC

TAT-PiET-PROTAC Chemical Structure

CAS No. : 3036046-04-2

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Based on 1 publication(s) in Google Scholar

TAT-PiET-PROTAC Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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  • Purity & Documentation

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Description

TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer[1].

IC50 & Target[1]

BRD4

 

VHL

 

In Vitro

TAT-PiET-PROTAC (2.5-10 μM, 6-24 h) reduces BRD4 and JMJD6 levels in MCF7 cells[1].
TAT-PiET-PROTAC inhibits proliferation in MCF7, T47D, MDA-MB231, and BT549 cells with EC50 values of 13.2, 6.16, 43.88 and 36.3 μM[1].
TAT-PiET-PROTAC (10 μM) inhibits colony formations in MCF7 and MDA-MB231 cells[1].
TAT-PiET-PROTAC (10 μM) inhibits migration in MCF7 and MDA-MB231 cells[1].
TAT-PiET-PROTAC (10 μM, 6 h) decreases expression of c-Myc, N-myc, and CCND1 in MCF7 and MDA-MB-231 cells[1].
TAT-PiET-PROTAC (10 μM) increases sensitivities in Tamoxifen (HY-13757A) -resistant MCF7 and T47Dcells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TAT-PiET-PROTAC Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF7 cells
Concentration: 2.5, 5 and 10 μM
Incubation Time: 6, 12 and 24 h
Result: Reduced BRD4 and JMJD6 levels.

Western Blot Analysis[1]

Cell Line: MCF7 and MDA-MB-231 cells
Concentration: 10 μM
Incubation Time: 6 h
Result: Decreased expression of c-Myc, N-myc, and CCND1.
In Vivo

TAT-PiET-PROTAC (25 mg/kg, i.p., every 2 days) inhibits tumor growth in MCF7/ MDA-MB231 tumor mice models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MCF7/MDA-MB231 tumor mice models[1]
Dosage: 25 mg/kg
Administration: Intraperitoneally injection, every 2 days
Result: Reduced tumor volume and weight.
Reduced BRD4 and JMJD6 levels.
Reduced c-Myc, N-myc, and CCND1 levels.
Molecular Weight

3430.01

Formula

C151H250N54O36S
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Arg-Asn-Gln-Lys-Phe-Lys-Cys-Gly-Glu-{Ahx}-Ile-Tyr-{Hyp}-Tyr-Ile
Sequence Shortening

YGRKKRRQRRRRNQKFKCGE-{AHX}-IY-{Hyp}-YI
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (1.46 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2915 mL 1.4577 mL 2.9154 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.2915 mL 1.4577 mL 2.9154 mL 7.2886 mL
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TAT-PiET-PROTAC Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAT-PiET-PROTAC3036046-04-2Epigenetic Reader DomainPROTACsPROTACBRD4JMJD6Breast cancerMCF7MDA-MB231Inhibitorinhibitorinhibit

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