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DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC). DT2216 targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
In vivo, DT2216 (i.p.; weekly for 60 days) of 15 mg/kg is more effective at suppressing the growth of MOLT-4 T-ALL xenografts in mice than 7.5 mg/kg.
Cell Death Differ. 2024 Dec 03.
HRK downregulation and augmented BCL-xL binding to BAK confer apoptotic protection to therapy-induced senescent melanoma cells
DT2216 purchased from AbMole
| Molecular Weight | 1542.36 |
| Formula | C77H96ClF3N10O10S4 |
| CAS Number | 2365172-42-3 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage | -20°C, sealed |
[1] Cancer Discov. The PROTAC DT2216 Targets Cancer by Promoting BCL-X L Degradation
| Related PROTAC Products |
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MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. |
| xStAx-VHLL TFA
xStAx-VHLL TFA, a PROTAC, sustains β-catenin degradation and manifested strong inhibition of Wnt signaling. xStAx-VHLL TFA promotes β-catenin ubiquitination. |
| (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. |
| MTX-23
MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis. |
| YD23
YD23 is a SMARCA2 PROTAC. |
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Products are for research use only. Not for human use. We do not sell to patients.
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