2. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  3. PROTACs STAT
  4. SD-965

SD-965 is a selective STAT3 PROTAC degrader with a DC50 of 0.14 μM. SD-965 promotes the ubiquitination and degradation of STAT3. SD-965 induces rapid, complete and persistent depletion of STAT3 protein. SD-965 induces tumor regression in mouse xenograft models of leukemia and lymphoma.
(Pink: STAT3 Target protein ligand; Blue: Cereblon ligand (HY-W1009348); Black: linker (HY-W017522)).

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

SD-965

SD-965 Chemical Structure

CAS No. : 3054394-56-5

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SD-965 Related Antibodies

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Description

SD-965 is a selective STAT3 PROTAC degrader with a DC50 of 0.14 μM. SD-965 promotes the ubiquitination and degradation of STAT3. SD-965 induces rapid, complete and persistent depletion of STAT3 protein. SD-965 induces tumor regression in mouse xenograft models of leukemia and lymphoma[1]. (Pink: STAT3 Target protein ligand; Blue: Cereblon ligand (HY-W1009348); Black: linker (HY-W017522)).

IC50 & Target[1]

STAT3

0.14 μM (DC50)

In Vitro

SD-965 (up to 5 μM; 24 h) potently degrades STAT3 in the STAT3 HiBiT assay with a DC50 of 0.14 μM and 85% maximal degradation after 24 h incubation[1].
SD-965 potently inhibits the growth of MOLM-16 leukemia cells (IC50 = 1.3 nM) and SU-DHL-1 lymphoma cells (IC50 = 260 nM)[1].
SD-965 (3.2-2000 nM; 14 h) selectively degrades STAT3 with >90% maximal degradation in human PBMCs after 14 h incubation, with no significant effect on other STAT family proteins up to 2 μM[1].
SD-965 exhibits excellent microsomal and plasma stability in mouse, rat, dog, monkey, and human, with a half-life of >120 min in all tested matrices[1].

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

SD-965 Related Antibodies

Western Blot Analysis[1]

Cell Line: SU-DHL-1 human anaplastic large cell lymphoma cells
Concentration: 3.2-2000 nM
Incubation Time: 14 h
Result: Degraded STAT3 with a DC50 of 80 nM and a Dₘₐₓ of >90%.
Showed no obvious effect on STAT1 or STAT6, modestly reduced STAT2 and STAT5 at 2 μM, and increased STAT4 levels in a dose-dependent manner.
In Vivo

SD-965 (25-50 mg/kg; i.v.; once weekly; for 3-4 consecutive weeks) effectively inhibits tumor growth in SU-DHL-1 lymphoma xenograft mouse models[1].

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

Animal Model: SU-DHL-1 lymphoma xenograft mouse model[1]
Dosage: 25-50 mg/kg
Administration: i.v.; once weekly; for 3-4 consecutive weeks
Result: Induced a maximum tumor regression by 58% at 25 mg/kg.
Reduced the tumor volume by 52% on day 5 after the first dose and by 96% on day 16, with 60% of mice without palpable tumors (50 mg/kg).
Molecular Weight

1213.21

Formula

C56H65N10O17PS
CAS No.
SMILES

O=C(P(O)(O)=O)C1=CC2=C(NC(C(N[C@H]3CN(C(CCCCC(N4C[C@@]5([H])N(C6=C(OC5)C7=C(C(N([C@@H](CC8)C(NC8=O)=O)C7)=O)C=C6)CC4)=O)=O)CC[C@](CC[C@H]9C(N[C@@H](CCC(N)=O)COC%10=CC=CC(S(=O)(C)=O)=C%10)=O)([H])N9C3=O)=O)=C2)C=C1
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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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References
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SD-965 Related Classifications

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Help & FAQs
  • 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.

Keywords:

SD-9653054394-56-5SD965SD 965PROTACsSTATleukemiaMOLM-16STAT3proteasomecereblonNEDD8-activating enzymemouse xenograft modelslymphomahuman PBMCsSU-DHL-1Inhibitorinhibitorinhibit

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