Bioactivity | 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]. |
Target | IC50: 24.2 nM (PTP1B); 30.1 nM (TC-PTP) |
Invitro | DU-14 (PTP1B/TC-PTP PROTAC) (0-1000 nM;16 小时) 在 IFN-γ 处理的 MC38 细胞中,导致 PTP1B/TC-PTP 降解和促进 STAT1 的磷酸化[1]。DU-14 (PTP1B/TC-PTP PROTAC) (48 小时) 在 T 细胞中可有效降解 TC-PTP 和 PTP1B,以及促进 T 细胞的活化[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> DU-14 (PTP1B/TC-PTP PROTAC) 相关抗体: Western Blot Analysis[1] Cell Line: |
In Vivo | DU-14 (PTP1B/TC-PTP PROTAC) (25-50 mg/kg;腹腔注射;10 天) 在结肠癌小鼠模型中具有抗肿瘤的活性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 3053413-58-1 |
Formula | C74H85BrF2N9O14PS |
Molar Mass | 1505.46 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Dong J, et al. Small Molecule Degraders of Protein Tyrosine Phosphatase 1B and T-Cell Protein Tyrosine Phosphatase for Cancer Immunotherapy. Angew Chem Int Ed Engl. 2023 May 22;62(22):e202303818. |