TAT-PiET-PROTAC
Based on 1 Customer Validation
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.
- Purity: 98.04%
- CAS No.: 3036046-04-2
- Formula: C151H250N54O36S
- Molecular Weight:3430.01
-
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)
All PROTACs Isoforms
More
Biological Activity
|
BRD4 |
VHL |
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.
-
Cell Line:MCF7 cells
-
Concentration:2.5, 5 and 10 μM
-
Incubation Time:6, 12 and 24 h
-
Result:Reduced BRD4 and JMJD6 levels.
-
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.
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.
Chemical Information
-
CAS No. 3036046-04-2
-
Appearance Solid
-
Molecular Weight 3430.01
-
Formula C151H250N54O36S
-
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
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (281 KB)
-
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)
-
Handling Instructions (2659 KB)
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 |