1. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  2. PROTACs STAT
  3. SD-2301

SD-2301 is a selective STAT3 PROTAC degrader. SD-2301 induces STAT3 degradation without affecting the protein levels of other STAT family members (STAT1, STAT2, STAT4, STAT5, STAT6). SD-2301 exerts anti-tumor effects in B16F10-bearing mice. SD-2301 can be used for the study of cancer. (Pink: STAT3 ligand (HY-172947), Blue: VHL Ligand (HY-172948), Black: Linker (HY-W577012), VHL ligand-linker conjugate (HY-172949)).

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

SD-2301

SD-2301 Chemical Structure

CAS No. : 3054116-24-1

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Description

SD-2301 is a selective STAT3 PROTAC degrader. SD-2301 induces STAT3 degradation without affecting the protein levels of other STAT family members (STAT1, STAT2, STAT4, STAT5, STAT6). SD-2301 exerts anti-tumor effects in B16F10-bearing mice. SD-2301 can be used for the study of cancer. (Pink: STAT3 ligand (HY-172947), Blue: VHL Ligand (HY-172948), Black: Linker (HY-W577012), VHL ligand-linker conjugate (HY-172949))[1].

IC50 & Target[1]

STAT3

 

VHL

 

In Vitro

SD-2301 (50 nM, 24 h) effectively degrades STAT3 protein in mouse dendritic cells (DCs)[1].
SD-2301 (0.32-200 nM, 14 h) exhibits high potency and selectivity in inducing degradation of STAT3 over other STAT proteins (STAT1, STAT2, STAT4, STAT5, STAT6) in human peripheral blood mononuclear cells (PBMCs)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SD-2301 (5 mg/kg, i.v., once every 3 days, 4 weeks) shows potency in inhibiting B16F10 melanoma growth in mice[1].
SD-2301 (5 mg/kg, i.v., once every 3 days) increases the proportion of KSPWFTTL tetramer+CD8+ T cells in tumor-infiltrating lymphocytes of MC38-bearing C57BL/6J mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B16F10 cells (2 × 105) were subcutaneously implanted into the flanks of 6-8-week-old C57BL/6J mice[1]
Dosage: 5 mg/kg
Administration: i.v., once every 3 days, 4 weeks
Result: Exhibited potency in inhibiting tumor growth.
Increased the number of effector CD8+ T cells (IFNγ+, GZMB+) in tumors.
Showed no significant changes in body weight.
Degraded STAT3 protein.
Molecular Weight

1366.50

Formula

C64H80N13O15PS2

CAS No.
SMILES

O=C([C@@H](NC([C@@H]1CC[C@@H]2CCN(C[C@@H](C(N12)=O)NC(C3=CC4=C(N3)C=CC(C(P(O)(O)=O)=O)=C4)=O)C(CCCCC5=CN(N=N5)[C@@H](C(C)(C)C)C(N6C[C@@H](C[C@H]6C(N[C@H](C7=CC=C(C=C7)C8=C(N=CS8)C)C)=O)O)=O)=O)=O)CCC(N)=O)NCC(C=C9)=CC=C9S(=O)(CC)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SD-2301
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HY-172946
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