K-252a
Based on 27 publication(s) in Google Scholar
K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
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- 純度: 99.02%
- CAS 番号: 99533-80-9
- 分子式: C27H21N3O5
- 分子量:467.47
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 K-252a
More- Signal Transduct Target Ther. 2024 Jun 28;9(1):153. [Abstract]
- Adv Mater. 2025 May 28:e2419768. [Abstract]
- J Adv Res. 2025 Apr 19:S2090-1232(25)00273-5. [Abstract]
- Theranostics. 2024 Mar 25;14(6):2345-2366. [Abstract]
- Cancer Lett. 2022 Jun 1:535:215629. [Abstract]
- Journal of Future Foods. 2025 Nov 19.
- Mol Psychiatry. 2026 Mar 23. [Abstract]
- Mol Psychiatry. 2022 Feb;27(2):1047-1058. [Abstract]
- Mol Med. 2023 Dec 19;29(1):170. [Abstract]
- Stem Cell Res Ther. 2023 Sep 21;14(1):263. [Abstract]
- Transl Psychiatry. 2023 Nov 17;13(1):352. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- CNS Neurosci Ther. 2026 Feb;32(2):e70795. [Abstract]
- Biochem Pharmacol. 2021 Oct:192:114740. [Abstract]
- J Neuroimmune Pharmacol. 2025 Apr 3;20(1):31. [Abstract]
- J Neuroimmune Pharmacol. 2025 Feb 4;20(1):13. [Abstract]
- Cancer Biol Ther. 2026 Dec 31;27(1):2644788. [Abstract]
- Sci Rep. 2025 Jul 25;15(1):27107. [Abstract]
- Front Mol Neurosci. 2020 Jun 30;13:95. [Abstract]
- Mol Pain. 2025 Jan-Dec:21:17448069251376198. [Abstract]
- Exp Cell Res. 2025 May 5:114569. [Abstract]
- 3 Biotech. 2021 Sep;11(9):418. [Abstract]
- PeerJ. 2022 Feb 15:10:e12886. [Abstract]
- Clin Exp Pharmacol Physiol. 2021 May;48(5):757-769. [Abstract]
- BMC Ophthalmol. 2019 Jun 17;19(1):130. [Abstract]
- Biomed Pharmacother. 2025 Oct 23:192:118602. [Abstract]
- Research Square Preprint. 2022 May.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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IHC
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In Vivo Efficacy Study
生物活性
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CaMK II |
K-252a (3-100 nM, 8d) inhibits NGF-promoted neurite outgrowth[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LINC00641-overexpressed cell line.
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Concentration:1.7 nM (NGF (50 ng/mL)).
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Incubation Time:6 h.
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Result:Decreased p-Akt and p-TrkB levels.
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Cell Line:PC12 subclone h cells.
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Concentration:3 to 100 nM.
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Incubation Time:8 d.
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Result:Inhibited NGF-promoted neurite outgrowth.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[6].
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Dosage:20 mg/kg/day.
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Administration:Intraperitoneally, daily, for consecutive 5 days.
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Result:Dampened the neuroprotective effects induced by TH.
化学情報
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CAS 番号 99533-80-9
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性状 Solid
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分子量 467.47
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分子式 C27H21N3O5
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Color White to light yellow
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SMILES
O=C(NC1)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5[C@](C[C@]7(O)C(OC)=O)([H])O[C@]7(C)N4C8=C3C=CC=C8
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別名
SF2370; Antibiotic K 252a; Antibiotic SF 2370
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Structure Classification
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Initial Source
Nocardiopsis sp.
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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 2 years -20°C 1 year
Publications (27)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Clinical efficacy and identification of factors confer resistance to afatinib (tyrosine kinase inhibitor) in EGFR-overexpressing esophageal squamous cell carcinoma. [Abstract]2024 Jun 28;9(1):153. PMID: 38937446
K-252a purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jun 28;9(1):153. [Abstract]
The efficacy of the pan-Trk inhibitors K252a (0.5 mg/kg every other day by intraperitoneal injection, for 17 days) was assessed when administered alone or in combination with afatinib in an afatinib-resistant model (KYSE30) (n = 5 mice per group).
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Adv Mater
Noninvasive Optogenetics Realized by iPSC-Derived Tentacled Carrier in Alzheimer's Disease Treatment. [Abstract]2025 May 28:e2419768. PMID: 40434197 -
J Adv Res
Astragaloside II, a natural saponin, facilitates remyelination in demyelination neurological diseases via p75NTR receptor mediated β-catenin/Id2/MBP signaling axis in oligodendrocyte precursor cells. [Abstract]2025 Apr 19:S2090-1232(25)00273-5. PMID: 40258474
K-252a purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Apr 19:S2090-1232(25)00273-5. [Abstract]
Molecular docking results for p75NTR (PDB: 5ZGG) with AS-II, NSC49652, and K252a.
K-252a purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Apr 19:S2090-1232(25)00273-5. [Abstract]
Binding affinities of AS-II and K252a (at concentrations from 1.5625-100 μM), PD90780 (at concentrations from 1.5625-200 μM) to p75NTR were determined using SPR assay.
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Theranostics
HDAC6-dependent deacetylation of NGF dictates its ubiquitination and maintains primordial follicle dormancy. [Abstract]2024 Mar 25;14(6):2345-2366. PMID: 38646645
K-252a purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Mar 25;14(6):2345-2366. [Abstract]
Hematoxylin staining of the ovarian section with TubA and K252a treated ovary. The 2 dpp ovaries were cultured for 3 days.
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Cancer Lett
Rab8A promotes breast cancer progression by increasing surface expression of Tropomyosin-related kinase B. [Abstract]2022 Jun 1:535:215629. PMID: 35278612 -
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Mol Psychiatry
BDNF restores impaired long-term potentiation of GABAergic synapses induced by chronic ethanol exposure in the VTA and attenuates reward-seeking behavior. [Abstract]2026 Mar 23. PMID: 41872517 -
Mol Psychiatry
Anti-depressive-like behaviors of APN KO mice involve Trkb/BDNF signaling related neuroinflammatory changes. [Abstract]2022 Feb;27(2):1047-1058. PMID: 34642455 -
Mol Med
TIM-3 regulates the proliferation by BDNF-mediated PI3K/AKT axis in the process of endometriosis. [Abstract]2023 Dec 19;29(1):170. PMID: 38114892 -
Stem Cell Res Ther
Human umbilical cord-derived mesenchymal stem cells ameliorate perioperative neurocognitive disorder by inhibiting inflammatory responses and activating BDNF/TrkB/CREB signaling pathway in aged mice. [Abstract]2023 Sep 21;14(1):263. PMID: 37735415
K-252a purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2023 Sep 21;14(1):263. [Abstract]
Schematic illustrating the timeline used for K252a (an antagonist of the TrkB receptor) or DMSO, hUC-MSC treatment, isoflurane anesthesia and exploratory laparotomy, NOR and MWM tests in the second experiment.
K-252a purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2023 Sep 21;14(1):263. [Abstract]
K252a treatment reversed the protective effects of hUC-MSCs on neural progenitor cells and immature neurons.
K-252a purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2023 Sep 21;14(1):263. [Abstract]
hUC-MSC treatment significantly increased the density of dendritic spines as assessed by Golgi–Cox staining, and K252a blocked these alterations [F(3, 12) = 25.668, P < 0.0001].
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Transl Psychiatry
eIF4E phosphorylation mediated LPS induced depressive-like behaviors via ameliorated neuroinflammation and dendritic loss. [Abstract]2023 Nov 17;13(1):352. PMID: 37978167 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
CNS Neurosci Ther
KCC2 Dysfunction Mediated by Microglial BDNF/TrkB Signaling Exacerbates Early Post-Stroke Seizure Susceptibility. [Abstract]2026 Feb;32(2):e70795. PMID: 41689206 -
Biochem Pharmacol
Brain-derived neurotrophic factor upregulates synaptic GluA1 in the amygdala to promote depression in response to psychological stress. [Abstract]2021 Oct:192:114740. PMID: 34419429 -
J Neuroimmune Pharmacol
Pentoxifylline Prevents Neuroinflammation and Modifies PTEN/TrkB Signaling in an LPS-Induced Depression Model. [Abstract]2025 Apr 3;20(1):31. PMID: 40175765 -
J Neuroimmune Pharmacol
PKR Inhibition Prevents Neuroinflammation and Rescues Depressive-Like Behaviors via BDNF/TrkB Signaling. [Abstract]2025 Feb 4;20(1):13. PMID: 39903347 -
Cancer Biol Ther
Deguelin inhibits perineural invasion in esophageal squamous cell carcinoma via targeting BDNF/TrkB axis. [Abstract]2026 Dec 31;27(1):2644788. PMID: 41851958 -
Sci Rep
BDNF improves fracture healing through promoting osteoblasts proliferation and migration via trkb/akt regulated NUCKS1 expression. [Abstract]2025 Jul 25;15(1):27107. PMID: 40715274 -
Front Mol Neurosci
LncRNA LINC00641 Sponges miR-497-5p to Ameliorate Neural Injury Induced by Anesthesia via Up-Regulating BDNF. [Abstract]2020 Jun 30;13:95. PMID: 32714145 -
Mol Pain
Inhibition of mTOR/S6K1/Gli1 signaling alleviates morphine-induced thermal hyperalgesia and tolerance. [Abstract]2025 Jan-Dec:21:17448069251376198. PMID: 40968661 -
Exp Cell Res
Low concentration of quercetin promotes BDNF expression and osteoblast differentiation during fracture healing via TrkB-ERK1/2 signaling pathway. [Abstract]2025 May 5:114569. PMID: 40334810 -
3 Biotech
Functional investigation of AfsKRS regulatory system for pristinamycin biosynthesis in Streptomyces pristinaespiralis. [Abstract]2021 Sep;11(9):418. PMID: 34603918 -
PeerJ
7,8-Dihydroxyflavone protects neurons against oxygen-glucose deprivation induced apoptosis and activates the TrkB/Akt pathway. [Abstract]2022 Feb 15:10:e12886. PMID: 35186478 -
Clin Exp Pharmacol Physiol
Tenacissoside H promotes neurological recovery of cerebral ischaemia/reperfusion injury in mice by modulating inflammation and oxidative stress via TrkB pathway. [Abstract]2021 May;48(5):757-769. PMID: 32799328 -
BMC Ophthalmol
Nerve growth factor promotes the proliferation of Müller cells co-cultured with internal limiting membrane by regulating cell cycle via Trk-A/PI3K/Akt pathway. [Abstract]2019 Jun 17;19(1):130. PMID: 31208396 -
Biomed Pharmacother
Protective effects of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside against cadmium toxicity involve BDNF/TrkB and PI3K/Akt signaling pathways. [Abstract]2025 Oct 23:192:118602. PMID: 41135432 -
溶剤 & 溶解度
DMSO : 50 mg/mL (106.96 mM; Need ultrasonic and warming; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
純度とドキュメンテーション
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データシート (288 KB)
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- Korean - KR (419 KB)
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参考文献
[1]. Yasuzawa, T., et al. The structures of the novel protein kinase C inhibitors K-252a, b, c AND d Journal of Antibiotics 39(8), 1072-1078 (1986). [Content Brief]
[2]. Davis, P.D., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides Journal of Medicinal Chemistry 35, 177-184 (1992). [Content Brief]
[3]. Tapley P, et al. K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors. Oncogene. 1992 Feb;7(2):371-81. [Content Brief]
[4]. Qingxia Chen, et al. LncRNA LINC00641 Sponges miR-497-5p to Ameliorate Neural Injury Induced by Anesthesia via Up-Regulating BDNF. Front Mol Neurosci. 2020 Jun 30;13:95. [Content Brief]
[5]. S Hashimoto, et al. K-252a, a potent protein kinase inhibitor, blocks nerve growth factor-induced neurite outgrowth and changes in the phosphorylation of proteins in PC12h cells. J Cell Biol. 1988 Oct;107(4):1531-9. [Content Brief]
[6]. Rui Zhang, et al. Tenacissoside H promotes neurological recovery of cerebral ischaemia/reperfusion injury in mice by modulating inflammation and oxidative stress via TrkB pathway. Clin Exp Pharmacol Physiol. 2021 May;48(5):757-769. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1392 mL | 10.6959 mL | 21.3917 mL | 53.4794 mL |
| 5 mM | 0.4278 mL | 2.1392 mL | 4.2783 mL | 10.6959 mL | |
| 10 mM | 0.2139 mL | 1.0696 mL | 2.1392 mL | 5.3479 mL | |
| 15 mM | 0.1426 mL | 0.7131 mL | 1.4261 mL | 3.5653 mL | |
| 20 mM | 0.1070 mL | 0.5348 mL | 1.0696 mL | 2.6740 mL | |
| 25 mM | 0.0856 mL | 0.4278 mL | 0.8557 mL | 2.1392 mL | |
| 30 mM | 0.0713 mL | 0.3565 mL | 0.7131 mL | 1.7826 mL | |
| 40 mM | 0.0535 mL | 0.2674 mL | 0.5348 mL | 1.3370 mL | |
| 50 mM | 0.0428 mL | 0.2139 mL | 0.4278 mL | 1.0696 mL | |
| 60 mM | 0.0357 mL | 0.1783 mL | 0.3565 mL | 0.8913 mL | |
| 80 mM | 0.0267 mL | 0.1337 mL | 0.2674 mL | 0.6685 mL | |
| 100 mM | 0.0214 mL | 0.1070 mL | 0.2139 mL | 0.5348 mL |
K-252a 関連分類
HY-N6732 関連分類
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