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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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| CR8
CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). |
| ARV-393
ARV-393 is an orally active PROTAC degrader targeting BCL6 for studies related to diffuse large B-cell lymphoma. ARV-393 utilizes the ubiquitin-proteasome system to target the degradation of BCL6. |
| ARV-766
ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations. ARV-766 has the potential to be first- and best-in class PROTAC AR degrader in mCRPC. |
| Indisulam
Indisulam is a carbonic anhydrase inibitor and antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition. |
| dBET6
dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity. |
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