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)).

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

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

CAS No. : 3053413-58-1

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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.
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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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DU-14 (PTP1B/TC-PTP PROTAC)
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