1. PROTAC JAK/STAT Signaling Stem Cell/Wnt
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  3. DU-14 (PTP1B/TC-PTP PROTAC)

DU-14 (PTP1B/TC-PTP PROTAC) is a potent and selective PTP1B and TC-PTP dual PROTAC degrader. DU-14 (PTP1B/TC-PTP PROTAC) has the IC50 for PTP1B and TC-PTP phosphatase activity of 24.2 nM and 30.1 nM, respectively. DU-14 (PTP1B/TC-PTP PROTAC) enhances IFN-γ signaling, promotes T cell activation, and has anti-tumor activity. (Pink: PTP1B/TC-PTP inhibitor (HY-171027); Black: Linker (HY-W340290); Blue: E3 ligand (HY-112078)).

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

DU-14 (PTP1B/TC-PTP PROTAC)

DU-14 (PTP1B/TC-PTP PROTAC) Chemical Structure

CAS No. : 3053413-58-1

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Based on 1 publication(s) in Google Scholar

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Description

DU-14 (PTP1B/TC-PTP PROTAC) is a potent and selective PTP1B and TC-PTP dual PROTAC degrader. DU-14 (PTP1B/TC-PTP PROTAC) has the IC50 for PTP1B and TC-PTP phosphatase activity of 24.2 nM and 30.1 nM, respectively. DU-14 (PTP1B/TC-PTP PROTAC) enhances IFN-γ signaling, promotes T cell activation, and has anti-tumor activity. (Pink: PTP1B/TC-PTP inhibitor (HY-171027); Black: Linker (HY-W340290); Blue: E3 ligand (HY-112078))[1].

IC50 & Target

IC50: 24.2 nM (PTP1B); 30.1 nM (TC-PTP)[1]

In Vitro

DU-14 (PTP1B/TC-PTP PROTAC) (0-1000 nM; 16 h) causes PTP1B/TC-PTP degradation and promotes STAT1 phosphorylation in IFN-γ-treated MC38 cells[1].
DU-14 (PTP1B/TC-PTP PROTAC) (48 h) effectively degrades TC-PTP and PTP1B in T cells and promotes the activation of T cells[1].

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

Western Blot Analysis[1]

Cell Line: IFN-γ treated MC38 cells
Concentration: 0, 5, 25, 125, 250, 500 and 1000 nM
Incubation Time: 16 h
Result: Inhibited the levels of PTP1B and TC-PTP in a dose-dependent manner.
Increased the level of pSTAT1/Y701 in a dose-dependent manner.
In Vivo

DU-14 (PTP1B/TC-PTP PROTAC) (25-50 mg/kg; intraperitoneal injection; 10 days) has antitumor activity in a mouse model of colon cancer[1].

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

Animal Model: C57BL/6 mice bearing MC38 colorectal tumors in the flanks[1]
Dosage: 25 and 50 mg/kg
Administration: Intraperitoneal injection (i.p.); 10 days
Result: Effectively repressed MC38 tumor growth at dose of 25 mg/kg, and resulted in static tumor growth at dose of 50 mg/kg.
Did not produce significant toxicity.
Degraded nearly complete PTP1B and TC-PTP in whole tumor homogenates.
Increased CD8+ T cell infiltrates in MC38 tumors.
Molecular Weight

1505.46

Formula

C74H85BrF2N9O14PS

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=P(O)(O)C(F)(F)C(C=C1)=CC=C1C[C@H](NC([C@@H](NC(CC2=CC(OC)=C(C=C2)O)=O)CC3=CC=CC=C3)=O)C(N[C@@H](CCCCNC(C4=CC(Br)=C(C=C4)C)=O)C(NCC5=CC=CC(CC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(N[C@H](C7=CC=C(C8=C(N=CS8)C)C=C7)C)=O)=O)=O)=C5)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (66.42 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 0.6642 mL 3.3212 mL 6.6425 mL
5 mM 0.1328 mL 0.6642 mL 1.3285 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 (protect from light, stored under nitrogen). 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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Purity & Documentation
References

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 (protect from light, stored under nitrogen). 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 0.6642 mL 3.3212 mL 6.6425 mL 16.6062 mL
5 mM 0.1328 mL 0.6642 mL 1.3285 mL 3.3212 mL
10 mM 0.0664 mL 0.3321 mL 0.6642 mL 1.6606 mL
15 mM 0.0443 mL 0.2214 mL 0.4428 mL 1.1071 mL
20 mM 0.0332 mL 0.1661 mL 0.3321 mL 0.8303 mL
25 mM 0.0266 mL 0.1328 mL 0.2657 mL 0.6642 mL
30 mM 0.0221 mL 0.1107 mL 0.2214 mL 0.5535 mL
40 mM 0.0166 mL 0.0830 mL 0.1661 mL 0.4152 mL
50 mM 0.0133 mL 0.0664 mL 0.1328 mL 0.3321 mL
60 mM 0.0111 mL 0.0554 mL 0.1107 mL 0.2768 mL
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  • 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.

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Product Name:
DU-14 (PTP1B/TC-PTP PROTAC)
Cat. No.:
HY-164864
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