2. PROTAC Metabolic Enzyme/Protease Immunology/Inflammation JAK/STAT Signaling Stem Cell/Wnt
  3. PROTACs Phosphatase IFNAR STAT
  4. PVD-06

PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). PVD-06 induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. PVD-06 can be used to further investigate PTPN2 in diseases such as leukemia and melanoma. (Pink: PTPN2 ligand (HY-168691), Black: linker (HY-B0236), Blue: VHL ligand (HY-112078)).

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PVD-06

PVD-06 構造式

CAS 番号 : 3032975-48-4

容量 価格（税別） 在庫状況 数量
1 mg $1120 在庫あり
5 mg $2800 在庫あり
10 mg $4200 在庫あり
25 mg $6300 在庫あり
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100 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

PVD-06 関連抗体

Top Publications Citing Use of Products

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

STAT アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
STAT3 STAT5 STAT6 STAT1

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製品説明

PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). PVD-06 induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. PVD-06 can be used to further investigate PTPN2 in diseases such as leukemia and melanoma[1]. (Pink: PTPN2 ligand (HY-168691), Black: linker (HY-B0236), Blue: VHL ligand (HY-112078)).

IC50 & Target

PTPN2[1]
体外実験

PVD-06 (0.1-10 μM, 1-48 h) induces PTPN2 degradation and reduces the PTPN2 protein levels through a VHL-, ubiquitin, and proteasome-dependent pathway[1].
PVD-06 (0.1-10 μM, 1-48 h) enhances the phosphorylation of STAT1 in Jurkat cells, a key downstream signaling node, confirming that the effect is dependent on selective PTPN2 degradation[1].
PVD-06 (1.25-5 μM, 3 days) promotes T cell proliferation under CD3/CD28 stimulation in a concentration-dependent manner[1].
PVD-06 (1.25-5 μM, 96 h) significantly amplifies B16F10 cell growth inhibition in a concentration-dependent manner in the presence of IFN-γ[1].

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

PVD-06 関連抗体

Western Blot Analysis[1]

Cell Line: Jurkat, B16F10, HepG2 and mouse spleen cells
Concentration: 0.1, 0.013, 0.04, 0.12, 0.37, 1, 1.1, 3.5, 5, 10 and 50 μM
Incubation Time: 24 h
Result: Induced PTPN2 degradation in a concentration-dependent manner without the hook effect.
Showed excellent PTPN2 subtype selectivity in B16F10 and mouse spleen cell models, consistent with the experimental results in the Jurkat cells.
Induced remarkable PTPN2 degradation without affecting the levels of PTP1B, SHP-1, and SHP-2.
Induced PTPN2 degradation on the HepG2 cell line, but it did not affect the PTP1B level.
Significantly reduced the PTPN2 level but not the PTP1B level in mouse spleen cells.
Significantly induced PTPN2 degradation in B16F10 cells, while the PTP1B level remained unchanged.
Dose dependently increased STAT1 phosphorylation after 24 h on the Jurkat cell line in the presence of 10 ng/mL IFN-γ.
Increased STAT1 phosphorylation by degrading PTPN2 selectively.

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 1 μM
Incubation Time: 1, 2, 3, 6, 9, 12, 24, 36, and 48 h
Result: Induced PTPN2 degradation in a time-dependent manner without affecting the PTP1B level at all time points.
The degradation induced was weakened by the addition of excessive PTPN2 ligand M8, proteasome inhibitor MG132 (HY-13259), NEDD8-activating enzyme inhibitor MLN4924 (HY-70062), or VHL E3 ligase ligand VM5.
Induced degradation through the PTPN2 ligand-dependent and VHL-dependent ubiquitin proteasomal degradation pathway.
分子量

1074.13

分子式

C48H55F4N9O11S2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

OC(C(F)(F)F)=O.O=C(CN1N=CC(C2=CC=C3C=C(C(N4CC(NS4(=O)=O)=O)=C(C3=C2)F)O)=C1)NCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -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 (93.10 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 0.9310 mL 4.6549 mL 9.3099 mL
5 mM 0.1862 mL 0.9310 mL 1.8620 mL
10 mM 0.0931 mL 0.4655 mL 0.9310 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.

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

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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）

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体積 （開始）

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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 (2.33 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.33 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 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:

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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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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.
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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 0.9310 mL 4.6549 mL 9.3099 mL 23.2747 mL
5 mM 0.1862 mL 0.9310 mL 1.8620 mL 4.6549 mL
10 mM 0.0931 mL 0.4655 mL 0.9310 mL 2.3275 mL
15 mM 0.0621 mL 0.3103 mL 0.6207 mL 1.5516 mL
20 mM 0.0465 mL 0.2327 mL 0.4655 mL 1.1637 mL
25 mM 0.0372 mL 0.1862 mL 0.3724 mL 0.9310 mL
30 mM 0.0310 mL 0.1552 mL 0.3103 mL 0.7758 mL
40 mM 0.0233 mL 0.1164 mL 0.2327 mL 0.5819 mL
50 mM 0.0186 mL 0.0931 mL 0.1862 mL 0.4655 mL
60 mM 0.0155 mL 0.0776 mL 0.1552 mL 0.3879 mL
80 mM 0.0116 mL 0.0582 mL 0.1164 mL 0.2909 mL
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PVD-06 Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

質量   濃度   体積   分子量 *
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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:

PVD-063032975-48-4PVD06PVD 06PROTACsPhosphataseIFNARSTATInterferon-α/β receptorInterferon-alpha/beta receptorPROTACPTPN2VHLubiquitinationproteasomeT cellIFN-γSTAT1JurkatB16F10HepG2mouse spleen cellsleukemiamelanomaInhibitorinhibitorinhibit

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製品名:
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製品番号:
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