TRAP-1
Based on 1 Customer Validation
TRAP-1 (XJZ-06-462) is a transcriptional activator of p53 (TRAP) with JQ-1 carboxylic acid (HY-78695) as its target protein ligand. TRAP-1 forms a ternary complex with p53Y220C and BRD4, potently activates p53 transcription, and inhibits the growth and proliferation of tumor cells. TRAP-1 upregulates p21 and other p53 target genes in pancreatic cell lines carrying p53Y220C, and induces cellular senescence and apoptosis. TRAP-1 can be used in cancer research involving p53Y220C-carrying tumors.
(Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand; Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.69%
- CAS No.: 3109600-48-5
- 화학식: C57H66ClF3N11O3PS
- 분자량:1108.69
-
보관:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
Biological Activity
TRAP-1 (0.1 nM-10 μM; 15 min) potently and specifically induces proximity between purified p53Y220C DNA binding domain and BRD4BD1, with no activity toward wild-type p53[1].
TRAP-1 (0.1-10 μM; 24 h) induces potent, dose-dependent p53-mediated transcriptional activation in p53Y220C-expressing BxPC-3 cells[1].
TRAP-1 (1-10 μM; 4 h) induces a stable interaction between BRD4 and p53Y220C in transfected HEK293T cells[1].
TRAP-1 (1, 3 μM; 2-24 h) induces robust, time-dependent upregulation of p53 target genes (MDM2, CDKN1A, BBC3) in p53Y220C-expressing BxPC-3 cells; induces rapid and robust upregulation of p21 and MDM2 protein levels in p53Y220C-expressing BxPC-3 cells[1].
TRAP-1 (2 μM; 2 h pulse, 72 h compound-free) is sufficient to induce persistent inhibition of cell proliferation in p53Y220C-expressing BxPC-3 cells[1].
TRAP-1 (0.001-10 μM; 72, 120 h) exhibits potent, mutant-selective antiproliferative activity against p53Y220C-expressing cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:BxPC-3 cells (p53Y220C expressing)
-
Concentration:3 μM
-
Incubation Time:2, 4, 8, 16, 24 h; 8 h
-
Result:Upregulated MDM2 and CDKN1A mRNA in a time-dependent manner as early as 2 h post-treatment, with maximum levels at 8 h.
Induced an ~10-fold increase in BBC3 mRNA after 8 h of treatment, while TP53 mRNA levels remained unchanged.
-
Cell Line:BxPC-3 cells (p53Y220C expressing)
-
Concentration:1, 3 μM
-
Incubation Time:2, 16 h
-
Result:Caused robust upregulation of p21 and MDM2 protein levels when treated with 1 or 3 μM for 16 h.
Induced potent upregulation of p21 protein when treated with 3 μM for 2 h, with no significant changes in p53, PUMA, or BAX protein levels detected at either time point.
-
Cell Line:BxPC-3 cells (p53Y220C expressing)
-
Concentration:2 μM
-
Incubation Time:2 h (pulse treatment), followed by 72 h compound-free incubation
-
Result:Inhibited cell proliferation, with a significant reduction in luminescence-based cell proliferation signal relative to DMSO and B-1 linker-treated cells.
-
Cell Line:BxPC-3 cells (p53Y220C expressing), A549 cells (p53WT), CCD 841 CoN cells (p53WT), isogenic A549-p53Y220C cells, A549-p53-/- cells, A549-p53WT cells
-
Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM
-
Incubation Time:72 h (BxPC-3, A549, isogenic A549 cells); 120 h (BxPC-3, CCD 841 CoN cells)
-
Result:Inhibited the viability of BxPC-3, A549, and CCD 841 CoN cells, with IC50 values of 0.531 μM (72 h)/0.314 μM (120 h), 3.94 μM (72 h), and 6.47 μM (120 h), respectively.
Inhibited isogenic A549-p53Y220C cell viability with an IC50 of 1.03 μM at 72 h, showing enhanced activity compared to A549-p53-/- (3.83 μM) and A549-p53WT (3.45 μM) cells.
Chemical Information
-
CAS No. 3109600-48-5
-
Appearance Solid
-
분자량 1108.69
-
화학식 C57H66ClF3N11O3PS
-
Color Off-white to light yellow
-
SMILES
CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(N4CCN(CC4)CC5CCN(CC5)C(CN6CCC(CC6)NC7=C8C(N(C(C#CCNC9=CC=C(C=C9)P(C)(C)=O)=C8)CC(F)(F)F)=CC=C7)=O)=O)C%10=NN=C(C)N2%10
-
Synonyms
XJZ-06-462
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 100 mg/mL (90.20 mM; Need ultrasonic; 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 (protect from light). 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 (protect from light). 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)
순도&문서
-
Data Sheet (277 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 (protect from light). 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 | 0.9020 mL | 4.5098 mL | 9.0197 mL | 22.5491 mL |
| 5 mM | 0.1804 mL | 0.9020 mL | 1.8039 mL | 4.5098 mL | |
| 10 mM | 0.0902 mL | 0.4510 mL | 0.9020 mL | 2.2549 mL | |
| 15 mM | 0.0601 mL | 0.3007 mL | 0.6013 mL | 1.5033 mL | |
| 20 mM | 0.0451 mL | 0.2255 mL | 0.4510 mL | 1.1275 mL | |
| 25 mM | 0.0361 mL | 0.1804 mL | 0.3608 mL | 0.9020 mL | |
| 30 mM | 0.0301 mL | 0.1503 mL | 0.3007 mL | 0.7516 mL | |
| 40 mM | 0.0225 mL | 0.1127 mL | 0.2255 mL | 0.5637 mL | |
| 50 mM | 0.0180 mL | 0.0902 mL | 0.1804 mL | 0.4510 mL | |
| 60 mM | 0.0150 mL | 0.0752 mL | 0.1503 mL | 0.3758 mL | |
| 80 mM | 0.0113 mL | 0.0564 mL | 0.1127 mL | 0.2819 mL |
TRAP-1 Related Classifications
HY-169369 Related Classifications
Powered by Bioz