2. K-252a

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

Cat. No.: HY-N6732 Purity: 99.23%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

K-252a Chemical Structure

K-252a Chemical Structure

CAS No. : 99533-80-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 514 In-stock
Solution
10 mM * 1 mL in DMSO USD 514 In-stock
Solid
1 mg USD 140 In-stock
5 mg USD 500 In-stock
10 mg USD 850 In-stock
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Based on 13 publication(s) in Google Scholar

K-252a Related Antibodies

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Description

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

IC50: 470 nM (PKC), 140 nM (PKA), 270 nM (Ca2+/calmodulin-dependent kinase type II), 1.7 nM (phosphorylase kinase)[1][2].
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.

K-252a Related Antibodies

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.
Molecular Weight

467.47

Formula

C27H21N3O5
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1392 mL 10.6959 mL 21.3917 mL
5 mM 0.4278 mL 2.1392 mL 4.2783 mL
View the 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.

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  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.45%

COA (263 KB) HNMR (238 KB) RP-HPLC (228 KB)

Handling Instructions (2659 KB)

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

K-252a99533-80-9SF2370 Antibiotic K 252a Antibiotic SF 2370SF 2370SF-2370Antibiotic SF2370Antibiotic SF 2370Antibiotic SF-2370Inhibitorinhibitorinhibit

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