DTP3 |
Catalog No.GC13244
One-Click Copy Product Info
|
inhibitor of GADD45β/MKK7 complex
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1809784-29-9
Sample solution is provided at 25 µL, 10mM.
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DTP3 is an inhibitor of GADD45β/MKK7 complex [1].
GADD45β is an antiapoptotic factor regulated by NF-kB. MAP kinase kinase 7 (MKK7) is a JNK kinase. GADD45β/MKK7 complex is the downstream module of NF-κB and becomes a therapeutic target in multiple myeloma (MM) [1].
DTP3 is an inhibitor of GADD45β/MKK7 complex. DTP3 interacted with and caused a significant conformational change of GADD45β/MKK7 complex in a dose dependent way, as well as of the isolated MKK7 protein. DTP3 bound to MKK7 with KD value of 64.81 nM. By binding to MKK7, DTP3 dissociated the GADD45b/MKK7 complex through an allosteric mechanism and caused conformational rearrangement of the kinase. In both MM and non-MM cell lines with high expression of GADD45B, DTP3 inhibited cell growth and displayed potent and selective activity and was completely inactive in tumor cell lines with low GADD45B expression. Also, DTP3 effectively activated tumor necrosis factor α (TNFα, a potent inducer of JNK) and JNK [1].
In mice bearing myeloma xenografts, DTP3 (14.5 mg/kg/day) significantly inhibited tumor growth through induction of JNK activation and apoptosis [1].
Reference:
[1]. Tornatore L, Sandomenico A, Raimondo D, et al. Cancer-Selective Targeting of the NF-kB
Survival Pathway with GADD45b/MKK7 Inhibitors. Cancer Cell, 2014, 26(4): 495-508.
| Cas No. | 1809784-29-9 | SDF | |
| Chemical Name | (R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide | ||
| Canonical SMILES | CC(N[C@H](CC1=CC=C(O)C=C1)C(N[C@H](CCCNC(N)=N)C(N[C@H](CC2=CC=CC=C2)C(N)=O)=O)=O)=O | ||
| Formula | C26H35N7O5 | M.Wt | 525.6 |
| Solubility | Soluble in DMSO | Storage | -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9026 mL | 9.5129 mL | 19.0259 mL |
| 5 mM | 380.5 μL | 1.9026 mL | 3.8052 mL |
| 10 mM | 190.3 μL | 951.3 μL | 1.9026 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)