1. Cell Cycle/DNA Damage
    MAPK/ERK Pathway
  2. DNA/RNA Synthesis
    JNK
  3. DTP3 TFA

DTP3 TFA 

Cat. No.: HY-100538A Purity: 98.75%
Handling Instructions

DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.

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

Custom Peptide Synthesis

DTP3 TFA Chemical Structure

DTP3 TFA Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 225 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
25 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway[1].

IC50 & Target

GADD45β/MKK7[1]

In Vitro

DTP3 (10 μM; 1-21 days) causes the potent and tumor-selective induction of JNK activation and apoptosis, as shown by the appearance of phosphorylated JNK, as early as 24 hours[2].

Western Blot Analysis[2]

Cell Line: Multiple myeloma (MM) cell lines
Concentration: 10 μM
Incubation Time: 1, 3, 5, 14, 21 days
Result: Caused the appearance of phosphorylated JNK, as early as 24 hours.
In Vivo

DTP3 TFA (s.c.; 14.5 mg/kg/day; 28 days) has shown a dramatic shrinkage of the tumors, and virtually eradicates established subcutaneous myeloma xenografts in mice[2].
DTP3 TFA (intravenous injection; 10 mg/kg/day) has t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg[2].

Animal Model: 6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River)[2]
Dosage: 14.5 mg/kg
Administration: S.c.; daily; 28 days
Result: Had shown a dramatic shrinkage of the tumors.
Animal Model: CD1 male mice of 25-30 g[2]
Dosage: 10 mg/kg (Pharmacokinetic Study)
Administration: Intravenous injection
Result: Had t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg.
Molecular Weight

639.62

Formula

C₂₈H₃₆F₃N₇O₇

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

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

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (156.34 mM; Need ultrasonic)

DMSO : 50 mg/mL (78.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5634 mL 7.8171 mL 15.6343 mL
5 mM 0.3127 mL 1.5634 mL 3.1269 mL
10 mM 0.1563 mL 0.7817 mL 1.5634 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DTP3DTP 3DTP-3DNA/RNA SynthesisJNKc-Jun N-terminal kinaseInhibitorinhibitorinhibit

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DTP3 TFA
Cat. No.:
HY-100538A
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