1. PROTAC
    Stem Cell/Wnt
    JAK/STAT Signaling
    Apoptosis
  2. PROTAC
    STAT
    Apoptosis
  3. SD-36

SD-36 

Cat. No.: HY-129602
Handling Instructions

SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of CRBN ligand Lenalidomide for E3 ubiquitin ligase.

For research use only. We do not sell to patients.

SD-36 Chemical Structure

SD-36 Chemical Structure

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Description

SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of CRBN ligand Lenalidomide for E3 ubiquitin ligase[1].

IC50 & Target[1]

STAT3

50 nM (Kd)

Cereblon

 

In Vitro

SD-36 inhibits the growth of a subset of acute myeloid leukemia and anaplastic large-cell lymphoma cell lines by inducing cell-cycle arrest and/or apoptosis[1].
SD-36 (0.005-5 μM; 4 days) demonstrates potent activity (IC50<2 μM) in MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines[1].
SD-36 (1 μM; 5 hours) completely depletes both monomeric and dimeric STAT3 protein in MOLM-16 cells[1].

Cell Viability Assay[1]

Cell Line: MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines
Concentration: 0.005, 0.05, 0.5, 5 μM
Incubation Time: 4 days
Result: Demonstrated potent activity (IC50<2 μM) in those cell lines.

Western Blot Analysis[1]

Cell Line: MOLM-16 cells
Concentration: 1 μM
Incubation Time: 5 hours
Result: Completely depletes both monomeric and dimeric STAT3 protein.
In Vivo

SD-36 (25-100 mg/kg; i.v.; weekly dosing for 4 weeks) achieves complete and long-lasting tumor regression in mice[1].
SD-36 effectively inhibits tumor growth at 25 and 50 mg/kg administered on day 1, 3, and 5 per week and achieved complete tumor regression at 100 mg/kg with the same schedule in the SU-DHL-1 xenograft model[1].
SD-36 at 50 mg/kg 3 times per week completely inhibits tumor growth in the SUP-M2 tumor model[1].

Animal Model: SCID female mice (MOLM-16 xenograft model)[1]
Dosage: 25, 50, 100 mg/kg
Administration: i.v.; weekly dosing for 4 weeks
Result: At 25 and 50 mg/kg weekly dosing for 4 weeks effectively inhibited tumor growth. At either 100 mg/kg weekly or 50 mg/kg twice weekly for 4 weeks induced complete tumor regression.
Molecular Weight

1158.15

Formula

C₅₉H₆₂F₂N₉O₁₂P

SMILES

O=C([[email protected]@H](NC([[email protected]@H]1CC[[email protected]](CCN(C(CCCCCC#CC2=CC=CC3=C2CN(C4CCC(NC4=O)=O)C3=O)=O)C[[email protected]@H]5NC(C6=CC(C=C(C(F)(P(O)(O)=O)F)C=C7)=C7N6)=O)N1C5=O)=O)CCC(N)=O)NC(C8=CC=CC=C8)C9=CC=CC=C9

Shipping

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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Keywords:

SD-36SD36SD 36PROTACSTATApoptosisProteolysis-targeting chimeraSH2 domaindegraderleukemialymphomatranscriptionalfactorapoptosislong-lastingInhibitorinhibitorinhibit

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SD-36
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