| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Targets |
Pit-1 targets the pleckstrin homology (PH) domains of several proteins, including Akt (PKB) and PDK1. It acts as a selective PIP3 antagonist, specifically disrupting the binding of PIP3 to these PH domains. Importantly, it does not affect interactions against PIP2-selective PH domains. By blocking this interaction, Pit-1 interferes with the activation of the PI3K/Akt signaling pathway.
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| ln Vitro |
Pit-1 is a selective PIP3 antagonist that specifically disrupts PIP3/Akt PH domain binding with an IC50 value of 31 μM. It suppresses PI3K-PDK1-Akt-dependent phosphorylation, including the phosphorylation of Akt-1, 2, and 3. In PTEN-deficient U87MG glioblastoma cells, Pit-1 reduces cell viability and induces apoptosis with an IC50 of 37 μM.
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| ln Vivo |
Pit-1 has been shown to exhibit antitumor activity in vivo. It inhibits cancer cell survival and induces apoptosis by inhibiting PIP3-dependent PI3K/Akt signaling. The compound also shows inhibitory effects on tumor angiogenesis and metastasis by interfering with the activation of Akt.
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| Enzyme Assay |
Pit-1's mechanism of action can be assessed using in vitro protein-lipid overlay assays or surface plasmon resonance (SPR). PH domains of target proteins (e.g., Akt, PDK1) are immobilized, and binding to PIP3-containing liposomes in the presence of varying concentrations of Pit-1 is measured. The ability of Pit-1 to compete with PIP3 for PH domain binding is determined, and IC50 values are calculated.
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| Cell Assay |
The cellular activity of Pit-1 is evaluated in cell-based assays measuring Akt phosphorylation. Cells (e.g., PTEN-deficient U87MG glioblastoma cells) are treated with increasing concentrations of Pit-1. Phosphorylation of Akt at Ser473 and Thr308 is measured by Western blot using phospho-specific antibodies. The inhibition of PIP3-mediated cell signaling can also be assessed by measuring downstream effects such as cell proliferation, migration, and survival.
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| Animal Protocol |
Specific in vivo animal experimental protocols for Pit-1 are not extensively detailed in standard reference sources. However, for evaluating its anti-tumor activity, Pit-1 would be administered to tumor-bearing mice (xenograft models) via intraperitoneal or oral routes. Tumor growth, angiogenesis markers, and metastatic spread would be monitored to assess efficacy.
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| ADME/Pharmacokinetics |
Pit-1 has a molecular formula of C14H10ClN3O4S and a molecular weight of 351.76 g/mol. It is soluble in DMSO at ≥14 mg/mL and is typically stored at 2-8°C. Its SMILES string is S=C(Nc2c(c(cc(c2)[N+](=O)[O-])Cl)O)NC(=O)c1ccccc1.
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| Toxicity/Toxicokinetics |
Pit-1 is classified as an acute toxicant (Acute Tox. 4 Oral) and is aquatic acute toxic (Aquatic Acute 1). It should be handled with care, and appropriate safety precautions should be taken. Specific LD50 values and organ-specific toxicity data are not extensively detailed in standard reference sources.
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| References | |
| Additional Infomation |
Pit-1 (CAS# 53501-41-0) is also known as PIT-1 and by its IUPAC name N-[(3-chloro-2-hydroxy-5-nitrophenyl)carbamothioyl]benzamide. It is a featured product for Kinase Phosphatase Biology research and is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. Pit-1 is used in PIP3-mediated cell signaling studies.
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| Molecular Formula |
C14H10CLN3O4S
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|---|---|
| Molecular Weight |
351.761
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| Exact Mass |
351.008
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| CAS # |
53501-41-0
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| PubChem CID |
3664359
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.747
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| LogP |
4.28
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
467
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RIGXBXPAOGDDIG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10ClN3O4S/c15-10-6-9(18(21)22)7-11(12(10)19)16-14(23)17-13(20)8-4-2-1-3-5-8/h1-7,19H,(H2,16,17,20,23)
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| Chemical Name |
N-[(3-chloro-2-hydroxy-5-nitrophenyl)carbamothioyl]benzamide
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| Synonyms |
Pit1; Pit 1; Pit-1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~177.68 mM)
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| 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 | 2.8428 mL | 14.2142 mL | 28.4285 mL | |
| 5 mM | 0.5686 mL | 2.8428 mL | 5.6857 mL | |
| 10 mM | 0.2843 mL | 1.4214 mL | 2.8428 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.
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