| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg |
|
||
| 1g | |||
| Other Sizes |
| Targets |
PDCD4-IN-1 targets PDCD4 (Programmed Cell Death 4). PDCD4 is a protein involved in regulating cell growth, apoptosis, and tumor suppression. PDCD4-IN-1 functions as a PDCD4 inhibitor, promoting BDNF expression in neuronal cells. Inhibition of PDCD4 relieves its suppressive effects on neurotrophic signaling.
|
|---|---|
| ln Vitro |
In vitro, PDCD4-IN-1 is a PDCD4 inhibitor with a Kd of 350 nM. It promotes the expression of BDNF in hippocampal neuron cell HT-22. This demonstrates its potential for modulating neurotrophic signaling and promoting neuronal survival and plasticity.
|
| ln Vivo |
Specific in vivo activity data for PDCD4-IN-1 are not extensively reported. As a PDCD4 inhibitor that promotes BDNF expression, it would be expected to have neuroprotective effects in vivo. Further studies would be required to evaluate its efficacy in animal models of neurological disorders.
|
| Enzyme Assay |
The binding of PDCD4-IN-1 to PDCD4 is measured using binding assays with recombinant PDCD4 protein. Kd values are determined from binding curves using techniques such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC).
|
| Cell Assay |
The cellular activity of PDCD4-IN-1 is evaluated in hippocampal neuron cell HT-22. Cells are treated with the compound, and BDNF expression is measured by qRT-PCR or ELISA. Cell viability and neuroprotection are assessed using MTT assays or by measuring protection against glutamate-induced excitotoxicity.
|
| Animal Protocol |
In vivo efficacy of PDCD4-IN-1 would typically be evaluated in animal models of neurological disorders such as Alzheimer's disease, Parkinson's disease, or depression. Animals would be administered the compound, and BDNF levels and behavioral outcomes would be assessed.
|
| ADME/Pharmacokinetics |
PDCD4-IN-1 has a molecular formula of C12H9BrClN3O and a molecular weight of 326.58 g/mol. It is soluble in DMSO (250 mg/mL). The compound is stored at -20°C.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicological data for PDCD4-IN-1 are limited. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
|
| Additional Infomation |
PDCD4-IN-1 (compound 20031600) is a PDCD4 inhibitor with a Kd of 350 nM. It promotes BDNF expression in hippocampal neuron cells. The compound is a valuable tool for studying PDCD4 function, neurotrophic signaling, and potential therapeutic applications in neurological disorders.
|
| Molecular Formula |
C12H9BRCLN3O
|
|---|---|
| Molecular Weight |
326.576360464096
|
| Exact Mass |
324.96
|
| Elemental Analysis |
C, 44.13; H, 2.78; Br, 24.47; Cl, 10.85; N, 12.87; O, 4.90
|
| CAS # |
494763-64-3
|
| PubChem CID |
16654126
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
3.3
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
18
|
| Complexity |
293
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC(=CC(=C1)Cl)NNC(=O)C2=CC(=CN=C2)Br
|
| InChi Key |
VYRKESGWNTVDIT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H9BrClN3O/c13-9-4-8(6-15-7-9)12(18)17-16-11-3-1-2-10(14)5-11/h1-7,16H,(H,17,18)
|
| Chemical Name |
5-bromo-N'-(3-chlorophenyl)nicotinohydrazide
|
| Synonyms |
Compound 20031600; PDCD4-IN-1; PDCD-4-IN-1; PDCD 4-IN-1
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~765.51 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0620 mL | 15.3102 mL | 30.6204 mL | |
| 5 mM | 0.6124 mL | 3.0620 mL | 6.1241 mL | |
| 10 mM | 0.3062 mL | 1.5310 mL | 3.0620 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.