PIK-75
Based on 5 publication(s) in Google Scholar
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 372196-67-3
- Formula: C16H14BrN5O4S
- Molecular Weight:452.28
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Publications Citing Use of MedChemExpress (MCE) PIK-75
More
Biological Activity
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DNA-PK 2 nM (IC50) |
p110α 5.8 nM (IC50) |
p110γ 76 nM (IC50) |
p110δ 510 nM (IC50) |
p110β 1.3 μM (IC50) |
hsVPS34 2.6 μM (IC50) |
PI3KC2β 1 μM (IC50) |
PI3KC2α 10 μM (IC50) |
mTORC1 1 μM (IC50) |
mTORC2 10 μM (IC50) |
ATM 2.3 μM (IC50) |
ATR 21 μM (IC50) |
PI4KIIIβ 50 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | CC50 |
>100 μM
Compound: 12; PIK-75
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Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
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[PMID: 33539089] |
| HT-22 | IC50 |
0.16 μM
Compound: 24
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Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
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[PMID: 36876904] |
| MV4-11 | IC50 |
0.003 μM
Compound: 6, PIK-75
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Cytotoxicity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay
Cytotoxicity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 26349627] |
| OCI-AML-3 | IC50 |
220 nM
Compound: 74; PIK-75
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Antiproliferative activity against human OCI-AML-3 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
Antiproliferative activity against human OCI-AML-3 assessed as reduction in cell viability incubated for 48 hrs by CellTiter-Glo cell vaibility assay
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[PMID: 38564299] |
PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC50s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively[1].
PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC50 values of 1.2 and 1.3 μM, respectively[1].
PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC50 of 78 nM[2].
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death[3].
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1)
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Concentration:0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM
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Incubation Time:48 hours
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Result:Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment.
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Cell Line:Overnight-starved CHO-IR cells
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:5 minutes
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Result:Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner. PIK-75 potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice bearing tumors of MIA PaCa-2[3]
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Dosage:2 mg/kg; or combination with Gemcitabine (20 mg/kg)
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Administration:Administered injection; 5 times per week. 25 days
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Result:Reduced the tumor growth and enhanced the antitumor effect.
Chemical Information
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CAS No. 372196-67-3
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Appearance Solid
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Molecular Weight 452.28
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Formula C16H14BrN5O4S
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Color Light yellow to light brown
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SMILES
O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)/N=C/C2=CN=C3C=CC(Br)=CN32)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
TRIM24 Cooperates with Ras Mutation to Drive Glioma Progression through snoRNA Recruitment of PHAX and DNA-PKcs. [Abstract]2024 Jun 3:e2400023. PMID: 38828688 -
Clin Cancer Res
Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]2020 Apr 15;26(8):2011-2021. PMID: 31937620 -
Cell Rep
Meteorin-like alleviates hepatic steatosis by regulating hepatic triglyceride secretion and fatty acid oxidation. [Abstract]2025 Feb 5;44(2):115246. PMID: 39918960 -
Molecules
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]2020 Apr 23;25(8):1980. PMID: 32340370 -
Res Sq
Haploinsufficiency of ZNF251 causes DNA-PKcs-dependent resistance to PARP inhibitors in BRCA1-mutated cancer cells. [Abstract]2023 Apr 6:rs.3.rs-2688694. PMID: 37066268
Solvent & Solubility
DMSO : 13 mg/mL (28.74 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. [Content Brief]
[2]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. [Content Brief]
[3]. Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69. [Content Brief]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2110 mL | 11.0551 mL | 22.1102 mL | 55.2755 mL |
| 5 mM | 0.4422 mL | 2.2110 mL | 4.4220 mL | 11.0551 mL | |
| 10 mM | 0.2211 mL | 1.1055 mL | 2.2110 mL | 5.5275 mL | |
| 15 mM | 0.1474 mL | 0.7370 mL | 1.4740 mL | 3.6850 mL | |
| 20 mM | 0.1106 mL | 0.5528 mL | 1.1055 mL | 2.7638 mL | |
| 25 mM | 0.0884 mL | 0.4422 mL | 0.8844 mL | 2.2110 mL |
PIK-75 Related Classifications
HY-107834 Related Classifications
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