372196-67-3
372196-67-3 structure
- Name: PIK-75
- Chemical Name: 2-Methyl-5-nitro-1-benzenesulfonic acid 2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide
- CAS Number: 372196-67-3
- Molecular Formula: C16H14BrN5O4S
- Molecular Weight: 452.283
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-11-28 18:38:07
- Modify Date: 2025-08-20 05:02:25
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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)[1][2]. PIK-75 induces apoptosis[3].
| Name | 2-Methyl-5-nitro-1-benzenesulfonic acid 2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide |
|---|---|
| Synonyms |
2-methyl-5-nitro-2,3-dihydro-phthalazine-1,4-dione
N'-[(E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide Benzenesulfonic acid, 2-methyl-5-nitro-, 2-[(1E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide 2-Methyl-5-nitro-2,3-dihydro-phthalazin-1,4-dion 2-methyl-5-nitro-2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazidebenzenesulfonic acid 8-Nitro-3-methyl-2,3-dihydro-1,4-phthalazindion [2-methyl-5-nitro-1-benzenesulfonic acid 2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide] 1,4-Phthalazinedione,2,3-dihydro-2-methyl-5-nitro N'-[(E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylidene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide 2'-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylidene]-1',2-dimethyl-5-nitrobenzenesulfonohydrazide PIK-75 free base |
| Description | 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)[1][2]. PIK-75 induces apoptosis[3]. |
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| Related Catalog | |
| Target |
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) |
| In Vitro | 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]. Cell Viability Assay[3] Cell Line: Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1) Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM Incubation Time: 48 hours Result: Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment. Western Blot Analysis[2] Cell Line: Overnight-starved CHO-IR cells Concentration: 1, 10, 100, 1000 nM Incubation Time: 5 minutes 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]. |
| In Vivo | PIK-75 (2 mg/kg) 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]. Animal Model: Mice bearing tumors of MIA PaCa-2[3] Dosage: 2 mg/kg; or combination with Gemcitabine (20 mg/kg) Administration: Administered injection; 5 times per week. 25 days Result: Reduced the tumor growth and enhanced the antitumor effect. |
| References |
| Density | 1.7±0.1 g/cm3 |
|---|---|
| Molecular Formula | C16H14BrN5O4S |
| Molecular Weight | 452.283 |
| Exact Mass | 450.994965 |
| PSA | 121.24000 |
| LogP | 3.84 |
| Index of Refraction | 1.701 |