2. Apoptosis Metabolic Enzyme/Protease
  3. Apoptosis MDM-2/p53 Prolyl Endopeptidase (PREP)
  4. KYP-2047

KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation.

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KYP-2047

KYP-2047 構造式

CAS 番号 : 796874-99-2

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 84 在庫あり
Solution
10 mM * 1 mL in DMSO USD 84 在庫あり
Solid or liquid
5 mg $77 在庫あり
10 mg $113 在庫あり
25 mg $208 在庫あり
50 mg $308 在庫あり
100 mg $464 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Other Forms of KYP-2047:

KYP-2047 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation[1][2].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
>10 μM
Compound: 17, KYP-2047
Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique
Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique
[PMID: 23121075]
体外実験

KYP-2047 (0-100 μM) decreases U-87, U-138 and A-172 cell viability in a concentration-dependent manner[2].
KYP-2047 (0-100 μM) increases the pro-apoptotic protein Bax, p53 and caspase-3 expression whereas reduces Bcl-2 expression, and reduced significantly TGF-β expression[2].

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

KYP-2047 関連抗体

Cell Proliferation Assay

Cell Line: U-87, U-138 and A-172 cell[2]
Concentration: 0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 10 μM, 30 μM, 50 μM and 100 μM
Incubation Time: 24 h
Result: Decreased U-87, U-138 and A-172 cell viability in a concentration-dependent manner.

Western Blot Analysis

Cell Line: U-87 cell[2]
Concentration: 0, 50, 100 μM
Incubation Time: 24 h
Result: Increased the pro-apoptotic protein Bax, p53 and cleaved-caspase-3 expression, reduced significantly Bcl2 expression, reduced Ang1 and Ang2 expression, and decreased Ki-67 expression.
体内実験

KYP-2047 (1 or 5 mg/kg, 30 min before daily testing) dose-dependently improved the escape performance (i.e. latency to find the hidden platform and swimming path length) of the young but not the old rats in the water maze[1].
KYP-2047 (9 or 27 μmol/kg; IP; once, 1 or 3 h before decapitation; two daily doses for 10 days) increases neurotensin concentration in the hypothalamus[1].
KYP-2047 (0-5 mg/kg) significantly reduces tumor mass and neutrophil infiltration[2].
KYP-2047 (0-5 mg/kg) significantly reduces vascular endothelial-growth-factor (VEGF), CD34, angiopoietins (Ang) and endothelial-nitric-oxide synthase (eNOS) expression[2].

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

339.43

分子式

C20H25N3O2
CAS 番号
Appearance

Solid-Liquid Mixture

Color

Colorless to light yellow

SMILES

N#C[C@H]1N(C([C@H]2N(C(CCCC3=CC=CC=C3)=O)CCC2)=O)CCC1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (294.61 mM; Need ultrasonic; 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 2.9461 mL 14.7306 mL 29.4612 mL
5 mM 0.5892 mL 2.9461 mL 5.8922 mL
10 mM 0.2946 mL 1.4731 mL 2.9461 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (7.37 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.37 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
純度とドキュメンテーション

純度: 99.94%

COA (248 KB) HNMR (272 KB) RP-HPLC (254 KB) MS (198 KB)

取扱説明書 (2659 KB)
参考文献

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9461 mL 14.7306 mL 29.4612 mL 73.6529 mL
5 mM 0.5892 mL 2.9461 mL 5.8922 mL 14.7306 mL
10 mM 0.2946 mL 1.4731 mL 2.9461 mL 7.3653 mL
15 mM 0.1964 mL 0.9820 mL 1.9641 mL 4.9102 mL
20 mM 0.1473 mL 0.7365 mL 1.4731 mL 3.6826 mL
25 mM 0.1178 mL 0.5892 mL 1.1784 mL 2.9461 mL
30 mM 0.0982 mL 0.4910 mL 0.9820 mL 2.4551 mL
40 mM 0.0737 mL 0.3683 mL 0.7365 mL 1.8413 mL
50 mM 0.0589 mL 0.2946 mL 0.5892 mL 1.4731 mL
60 mM 0.0491 mL 0.2455 mL 0.4910 mL 1.2275 mL
80 mM 0.0368 mL 0.1841 mL 0.3683 mL 0.9207 mL
100 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7365 mL
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KYP-2047 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

KYP-2047796874-99-2KYP2047KYP 2047ApoptosisMDM-2/p53Prolyl Endopeptidase (PREP)prolyl oligopeptidasePOPGlioblastomaNeurotensinU-87 cellAngiopoietinseNOSVEGFInhibitorinhibitorinhibit

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製品名:
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製品番号:
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