2. PROTAC JAK/STAT Signaling Stem Cell/Wnt
  3. PROTACs STAT
  4. SD-91

SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a Ki of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506).

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SD-91

SD-91 Estructura química

No. CAS : 2497583-03-4

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SD-91 Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas PROTACs:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Ver todos los productos específicos de isoformas STAT:

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STAT3 STAT5 STAT6 STAT1

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Descripciòn

SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a Ki of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506)[1][2].

IC50 & Target[2]

STAT3

5.5 nM (Ki)

STAT3

28 nM (Kd)

Cellular Effect
Cell Line Type Value Description References
SU-DHL-1 IC50
2.6 μM
Compound: SD-91; 2
Antiproliferative activity against human SU-DHL-1 cells assessed as cell growth inhibition incubated for 4 days by CellTiter-Glo asssay
Antiproliferative activity against human SU-DHL-1 cells assessed as cell growth inhibition incubated for 4 days by CellTiter-Glo asssay
[PMID: 34141084]
In Vitro

SD-91 (Compound 92) (0.2 μM, 1 μM, 30 nM, 100 nM, 300 nM; 3 h) decreased the level of total STAT3 protein in acute leukemia Molm-16 cells[1].
In the BLI assays, SD-91 binds to STAT3 with a Kd value of 28 nM, while it displays a very weak affinity (Kd >10 μM) to all other STAT proteins (STAT1, STAT2, STAT4, STAT5A, STAT5B, and STAT6)[2].
In the MOLM-16 acute leukemia, SU-DHL-1, and SUP-M2 lymphoma cell lines, SD-91 has IC50 values of 0.17, 2.6, and 0.46 μM, respectively[2].
SD-91 (1-10 μM; 4 h) effectively reduce the levels of STAT3 protein in a dose-dependent manner, with DC50 values of 0.38 μM, 0.061μM, and 2.5 μM for MOLM-16, SU-DHL-1, and SUP-M2 cells, respectively[2].

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

SD-91 Related Antibodies

Western Blot Analysis[1]

Cell Line: Acute leukemia Molm-16 cells
Concentration: 0.2 μM, 1 μM; 30 nM, 100 nM, 300 nM
Incubation Time: 3 h
Result: Degraded the level of total STAT3 protein in acute leukemia Molm-16 cells.
In Vivo

SD-91 (Compound 92) (i.v.; 50 mg/kg; 6 h, 24 h, 48 h) decreased the level of total STAT3 protein and phosphorylated STAT3 (Y705) protein in acute leukemia Molm-16 tumors and SU-DHL-1 tumors in mice[1].
SD-91 (i.v.; 25, 50 mg/kg; qw) shows antitumor activity against Molm-16 xenograft tumors in mice[1].

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

Animal Model: Mice[1]
Dosage: 25, 50 mg/kg
Administration: i.v.; qw
Result: Showed antitumor activity in Molm-16 and SU-DHL-1 xenograft mice.
Peso molecular

1136.15

Fòrmula

C59H62N9O13P
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C[C@@H](C(N2[C@@](CC[C@H]2C(N[C@@H](CCC(N)=O)C(NC(C3=CC=CC=C3)C4=CC=CC=C4)=O)=O)([H])CC1)=O)NC(C5=CC6=CC(C(P(O)(O)=O)=O)=CC=C6N5)=O)CCCCCC#CC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8)=O)=CC=C7
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (88.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8802 mL 4.4008 mL 8.8017 mL
5 mM 0.1760 mL 0.8802 mL 1.7603 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8802 mL 4.4008 mL 8.8017 mL 22.0041 mL
5 mM 0.1760 mL 0.8802 mL 1.7603 mL 4.4008 mL
10 mM 0.0880 mL 0.4401 mL 0.8802 mL 2.2004 mL
15 mM 0.0587 mL 0.2934 mL 0.5868 mL 1.4669 mL
20 mM 0.0440 mL 0.2200 mL 0.4401 mL 1.1002 mL
25 mM 0.0352 mL 0.1760 mL 0.3521 mL 0.8802 mL
30 mM 0.0293 mL 0.1467 mL 0.2934 mL 0.7335 mL
40 mM 0.0220 mL 0.1100 mL 0.2200 mL 0.5501 mL
50 mM 0.0176 mL 0.0880 mL 0.1760 mL 0.4401 mL
60 mM 0.0147 mL 0.0733 mL 0.1467 mL 0.3667 mL
80 mM 0.0110 mL 0.0550 mL 0.1100 mL 0.2751 mL
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SD-91 Related Classifications

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-912497583-03-4STAT3 degrader-2SD91SD 91PROTACsSTATPROTACSTAT3cancerInhibitorinhibitorinhibit

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Nombre del producto:
SD-91
Cat. No.:
HY-150251
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