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Art. -Nr.: HY-169369

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TRAP-1

(Synonyms: XJZ-06-462)

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Based on 1 Customer Validation

TRAP-1 (XJZ-06-462) is a non-covalent regulated induced proximity targeting chimera (RIPTAC) with JQ-1 carboxylic acid (HY-78695) as its target protein ligand. TRAP-1 forms a ternary complex with p53^Y220C 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 p53^Y220C, and induces cellular senescence and apoptosis. TRAP-1 can be used in cancer research involving p53^Y220C-carrying tumors.
(Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand; Black: linker).

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Reinheit: 99.69%
CAS. Nr.: 3109600-48-5
Formel: C₅₇H₆₆ClF₃N₁₁O₃PS
Molecular Weight:1108.69

Speicherung:

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

TRAP-1 Chemical Structure

CAS. Nr.: 3109600-48-5

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Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

TRAP-1 (XJZ-06-462) is a non-covalent regulated induced proximity targeting chimera (RIPTAC) with JQ-1 carboxylic acid (HY-78695) as its target protein ligand. TRAP-1 forms a ternary complex with p53^Y220C 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 p53^Y220C, and induces cellular senescence and apoptosis. TRAP-1 can be used in cancer research involving p53^Y220C-carrying tumors^[1]. (Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand; Black: linker).

In Vitro

TRAP-1 (0.1 nM-10 μM; 15 min) potently and specifically induces proximity between purified p53^Y220C DNA binding domain and BRD4_BD1, 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 p53^Y220C-expressing BxPC-3 cells^[1].
TRAP-1 (1-10 μM; 4 h) induces a stable interaction between BRD4 and p53^Y220C 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 p53^Y220C-expressing BxPC-3 cells; induces rapid and robust upregulation of p21 and MDM2 protein levels in p53^Y220C-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 p53^Y220C-expressing BxPC-3 cells^[1].
TRAP-1 (0.001-10 μM; 72, 120 h) exhibits potent, mutant-selective antiproliferative activity against p53^Y220C-expressing cells^[1].

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

Real Time qPCR^[1]

Cell Line:

BxPC-3 cells (p53^Y220Cexpressing)
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.

Western Blot Analysis^[1]

Cell Line:

BxPC-3 cells (p53^Y220Cexpressing)
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 Proliferation Assay^[1]

Cell Line:

BxPC-3 cells (p53^Y220Cexpressing)
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 Viability Assay^[1]

Cell Line:

BxPC-3 cells (p53^Y220Cexpressing), A549 cells (p53^WT), CCD 841 CoN cells (p53^WT), isogenic A549-p53^Y220C cells, A549-p53^-/- cells, A549-p53^WT 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-p53^Y220C cell viability with an IC₅₀ of 1.03 μM at 72 h, showing enhanced activity compared to A549-p53^-/- (3.83 μM) and A549-p53^WT (3.45 μM) cells.

Chemical Information

CAS. Nr. 3109600-48-5
Appearance Solid
Molecular Weight 1108.69
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9020 mL

4.5098 mL

9.0197 mL

5 mM

0.1804 mL

0.9020 mL

1.8039 mL

10 mM

0.0902 mL

0.4510 mL

0.9020 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhu X, et al. Activating p53Y220C with a mutant-specific small molecule. Nat Commun. 2026.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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TRAP-1

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TRAP-1 Related Classifications

HY-169369 Related Classifications