CEP-1347
Based on 1 Customer Validation
CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53.
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- 純度: 98.5%
- CAS 番号: 156177-65-0
- 分子式: C33H33N3O5S2
- 分子量:615.76
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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JNK1 |
MLK3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
72 nM
Compound: 1
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Inhibition of GST-fused human MLK1 expressed in CHO cells assessed as MKK4 phosphorylation
Inhibition of GST-fused human MLK1 expressed in CHO cells assessed as MKK4 phosphorylation
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[PMID: 18714982] |
| SH-SY5Y | IC50 |
5.3 nM
Compound: 1
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Neuroprotective activity against human SH-SY5Y cells assessed as inhibition of MPP+-induced cell death
Neuroprotective activity against human SH-SY5Y cells assessed as inhibition of MPP+-induced cell death
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[PMID: 18714982] |
CEP-1347 (0-500 nM; 3 days) decreases the expression of MDM4 and activates the p53 pathway in malignant meningioma cells with wild-type p53[4].
CEP-1347 (KT7515) promotes motor neuron survival by inhibiting JNK1 activity in rat embryonic motor neurons deficient in nutritional factors. The IC50 values of CP-1347 for JNK1 activation and EC50 values of motor neuron survival are both 20 nM[5].
CEP-1347 (0.2-20 μM; 2 h) dose-dependently inhibits pancresin-induced JNK activation in isolated pancreatic acinus, and is almost completely effective at a concentration of 2 μM[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:male white Sprague-Dawley rats[6]
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Dosage:Caerulein (HY-A0190): 10 μg/kg; CEP-1347: 0-60 mg/kg
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Administration:Caerulein: Intravenous injection (i.v.); CEP-1347: Subcutaneous injection (s.c.)
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Result:Caerulein-induced JNK activation was dose-dependent inhibited.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 156177-65-0
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性状 Solid
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分子量 615.76
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分子式 C33H33N3O5S2
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Color White to off-white
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SMILES
C[C@]12N3C4=C(C5=CC(CSCC)=CC=C53)C(CNC6=O)=C6C(C7=C8)=C4N([C@@H](C[C@]2(O)C(OC)=O)O1)C7=CC=C8CSCC
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別名
KT7515
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Saporito MS, Hudkins RL, Maroney AC. Discovery of CEP-1347/KT-7515, an inhibitor of the JNK/SAPK pathway for the treatment of neurodegenerative diseases. Prog Med Chem. 2002;40:23-62. [Content Brief]
[2]. Maroney AC, Finn JP, Connors TJ, et al. Cep-1347 (KT7515), a semisynthetic inhibitor of the mixed lineage kinase family. J Biol Chem. 2001;276(27):25302-25308. [Content Brief]
[3]. Mitobe Y, Nakagawa-Saito Y, Togashi K, et al. CEP-1347 Targets MDM4 Protein Expression to Activate p53 and Inhibit the Growth of Glioma Cells. Anticancer Res. 2022;42(10):4727-4733. [Content Brief]
[4]. Mitobe Y, Suzuki S, Nakagawa-Saito Y, et al. The Novel MDM4 Inhibitor CEP-1347 Activates the p53 Pathway and Blocks Malignant Meningioma Growth In Vitro and In Vivo. Biomedicines. 2023;11(7):1967. [Content Brief]
[5]. Maroney AC, et al. Motoneuron apoptosis is blocked by CEP-1347 (KT 7515), a novel inhibitor of the JNK signaling pathway. J Neurosci. 1998;18(1):104-111. [Content Brief]
[6]. Wagner AC, et al. EP-1347 inhibits caerulein-induced rat pancreatic JNK activation and ameliorates caerulein pancreatitis. Am J Physiol Gastrointest Liver Physiol. 2000;278(1):G165-G172. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CEP-1347 関連分類
HY-10412 関連分類
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