Art. -Nr.: HY-N6732

K-252a

(Synonyms: SF2370; Antibiotic K 252a; Antibiotic SF 2370)

27 Cited Publications

Kundenbewertung

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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Reinheit: 99.02%
CAS. Nr.: 99533-80-9
Formel: C₂₇H₂₁N₃O₅
Molecular Weight:467.47

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year

K-252a Chemical Structure

CAS. Nr.: 99533-80-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (27)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1]^[2]. 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^[3].

IC₅₀ & Target

CaMK II

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Alle PKC Isoform-spezifische Produkte anzeigen :

Alle PKA Isoform-spezifische Produkte anzeigen :

Alle CaMK Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Western Blot Analysis^[4].

Cell Line:

LINC00641-overexpressed cell line.
Concentration:

1.7 nM (NGF (50 ng/mL)).
Incubation Time:

6 h.
Result:

Decreased p-Akt and p-TrkB levels.

Cell Viability Assay^[5].

Cell Line:

PC12 subclone h cells.
Concentration:

3 to 100 nM.
Incubation Time:

8 d.
Result:

Inhibited NGF-promoted neurite outgrowth.

In Vivo

K252a (20 mg/kg/day) inhibiting TrkB pathway dampens the neuroprotective effects induced by TH^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mice^[6].
Dosage:

20 mg/kg/day.
Administration:

Intraperitoneally, daily, for consecutive 5 days.
Result:

Dampened the neuroprotective effects induced by TH.

Chemical Information

CAS. Nr. 99533-80-9
Appearance Solid
Molecular Weight 467.47
Formel C₂₇H₂₁N₃O₅
Color White to light yellow
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
Synonyms

SF2370; Antibiotic K 252a; Antibiotic SF 2370
Structure Classification
- Alkaloids
- Indole Alkaloids
Initial Source
- Microorganisms
Nocardiopsis sp.
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (27)

All In Vivo Efficacy StudyIHCBio/Physico-chemical AssayHistological Imaging/Staining

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Journal Impact Factor

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).
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.
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.
Cancer Lett

Rab8A promotes breast cancer progression by increasing surface expression of Tropomyosin-related kinase B. [Abstract]

2022 Jun 1:535:215629. PMID: 35278612
Journal of Future Foods

2025 Nov 19.
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].
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
Research Square Preprint

2022 May.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1392 mL

10.6959 mL

21.3917 mL

5 mM

0.4278 mL

2.1392 mL

4.2783 mL

10 mM

0.2139 mL

1.0696 mL

2.1392 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

K-252a

27 Cited Publications

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K-252a

MCE Bioactive Compound Library

Natural Product Library Plus

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) K-252a

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Alle PKC Isoform-spezifische Produkte anzeigen

Alle PKA Isoform-spezifische Produkte anzeigen

Alle CaMK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (27)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

K-252a

MCE Bioactive Compound Library

Natural Product Library Plus

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) K-252a

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Alle PKC Isoform-spezifische Produkte anzeigen

Alle PKA Isoform-spezifische Produkte anzeigen

Alle CaMK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (27)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

K-252a Related Classifications

HY-N6732 Related Classifications