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SD-36 is a potent STAT3 PROTAC degradation agent (Kd=~50 nM) with a high selectivity compared to other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). Induction of STAT3 degradation resulted in strong inhibition of its transcriptional network in leukemia and lymphoma cells. SD-36 inhibited the growth of a subset of acute myeloid leukemia and anaplastic large cell lymphoma cell lines by inducing cell cycle arrest and/or apoptosis. SD-36 achieved complete and durable tumor regression in multiple xenograft mouse models with well-tolerated dosing schedules. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase.
| Molecular Weight | 1158.15 |
| Formula | C59H62F2N9O12P |
| CAS Number | 2429877-44-9 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage | -20°C, sealed |
| Related PROTAC Products |
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| GDC-2992
GDC-2992 is an orally active androgen receptor (AR) degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. |
| Setidegrasib
Setidegrasib is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib has antitumor effect. |
| PROTAC HK2 Degrader-1
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. |
| ZXH-4-130 TFA
ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). |
| MS4322
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