2. JAK/STAT Signaling Apoptosis
  3. Pim c-Myc Apoptosis
  4. SGI-1776-VHL-02

SGI-1776-VHL-02 is a stereoselective PIM PROTAC degrader. SGI-1776-VHL-02 promotes the ubiquitination and degradation of PIM1, PIM2 and PIM3. SGI-1776-VHL-02 downregulates c-myc protein levels, induces Apoptosis. SGI-1776-VHL-02 has anti-cancer activity against prostate cancer. SGI-1776-VHL-02 can be used in studies related to prostate cancer.
(Pink: Pim ligand (HY-13287); Blue: VHL ligand (HY-112078); Black: linker (HY-W015300)).

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SGI-1776-VHL-02

SGI-1776-VHL-02 Estructura química

No. CAS : 3013618-84-0

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
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SGI-1776-VHL-02 Related Antibodies

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Descripciòn

SGI-1776-VHL-02 is a stereoselective PIM PROTAC degrader. SGI-1776-VHL-02 promotes the ubiquitination and degradation of PIM1, PIM2 and PIM3. SGI-1776-VHL-02 downregulates c-myc protein levels, induces Apoptosis. SGI-1776-VHL-02 has anti-cancer activity against prostate cancer. SGI-1776-VHL-02 can be used in studies related to prostate cancer[1]. (Pink: Pim ligand (HY-13287); Blue: VHL ligand (HY-112078); Black: linker (HY-W015300)).

IC50 & Target[1]

PIM1

 

PIM2

 

PIM3

 

In Vitro

SGI-1776-VHL-02 (0.75-10 μM; 24 h) dose-dependently degrades doxycycline-induced PIM1 in PC3-dox-PIM1 cells, with the effective degradation starting at a concentration of 0.75 μM[1].
SGI-1776-VHL-02 (0.75-10 μM; 24 h) stereoselectively degrades doxycycline-induced PIM1 in PC3-dox-PIM1 cells, whereas its inactive epimer control fails to induce such degradation[1].
SGI-1776-VHL-02 (1.5 μM; 24 h) does not alter the level of PIM1 mRNA in PC3 cells, confirming that its effect on PIM1 is post-transcriptional[1].
SGI-1776-VHL-02 (1.5-3.75 μM; 24 h) degrades all three PIM kinase isoforms in PC3 cells, with PIM3 degraded at 1.5 μM and PIM2 degraded at 3.75 μM[1].
SGI-1776-VHL-02 (0.75-6.25 μM; 10 days) inhibits colony formation of prostate cancer cell lines PC3, LNCaP and C4-2[1].
SGI-1776-VHL-02 (3.75 μM; 24 h) downregulates c-myc protein levels in PC3 and LNCaP prostate cancer cells[1].
SGI-1776-VHL-02 (3.75 μM; 4 h) induces apoptosis in PC3 cells[1].

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

SGI-1776-VHL-02 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: PC3, LNCaP, and C4-2 prostate cancer cells
Concentration: 0.75-6.25 μM
Incubation Time: 10 days, with media replacement every 96 h
Result: Showed a more potent inhibitory effect on colony formation in PC3, LNCaP, and C4-2 cells compared to its parent inhibitor SGI-1776.
Efficiently reduced colony formation at tested concentrations.

Western Blot Analysis[1]

Cell Line: PC3 and LNCaP prostate cancer cells
Concentration: 3.75 μM
Incubation Time: 24 h
Result: Downmodulated c-myc after treatment in both PC3 and LNCaP cells.
Showed no c-myc downmodulation effect with the parent inhibitor SGI-1776 or PIM447-VHL-01.

Apoptosis Analysis[1]

Cell Line: PC3 cells
Concentration: 3.75 μM (SGI-1776-VHL-02); 2 nM (docetaxel)
Incubation Time: 4 h (SGI-1776-VHL-02 pre-treatment); 48 h (docetaxel incubation)
Result: Increased apoptosis significantly to 24% of cells as a single agent.
Increased the percentage of apoptotic cells significantly to 40% when co-treated with docetaxel, which was greater than the combination of docetaxel and SGI-1776.
Peso molecular

974.14

Fòrmula

C50H62F3N9O6S
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@@H](C[C@H](C1)O)C(N[C@H](C2=CC=C(C3=C(N=CS3)C)C=C2)C)=O)[C@H](C(C)(C)C)NC(CCCCCCC(N(CC4)CCC4CNC5=NN6C(C7=CC(OC(F)(F)F)=CC=C7)=CN=C6C=C5)=O)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (102.65 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 1.0265 mL 5.1327 mL 10.2655 mL
5 mM 0.2053 mL 1.0265 mL 2.0531 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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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 (sealed storage, away from moisture). 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 1.0265 mL 5.1327 mL 10.2655 mL 25.6637 mL
5 mM 0.2053 mL 1.0265 mL 2.0531 mL 5.1327 mL
10 mM 0.1027 mL 0.5133 mL 1.0265 mL 2.5664 mL
15 mM 0.0684 mL 0.3422 mL 0.6844 mL 1.7109 mL
20 mM 0.0513 mL 0.2566 mL 0.5133 mL 1.2832 mL
25 mM 0.0411 mL 0.2053 mL 0.4106 mL 1.0265 mL
30 mM 0.0342 mL 0.1711 mL 0.3422 mL 0.8555 mL
40 mM 0.0257 mL 0.1283 mL 0.2566 mL 0.6416 mL
50 mM 0.0205 mL 0.1027 mL 0.2053 mL 0.5133 mL
60 mM 0.0171 mL 0.0855 mL 0.1711 mL 0.4277 mL
80 mM 0.0128 mL 0.0642 mL 0.1283 mL 0.3208 mL
100 mM 0.0103 mL 0.0513 mL 0.1027 mL 0.2566 mL
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SGI-1776-VHL-02 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:

SGI-1776-VHL-023013618-84-0Pimc-MycApoptosisPim kinasesMycprostate cancer cellsLNCaP cellsPIM1PC3-dox-PIM1 cellsVHL E3 ubiquitin ligasePIM2PIM3C4-2 cellsPC3 cellsubiquitin-proteasome pathwayInhibitorinhibitorinhibit

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Nombre del producto:
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Cat. No.:
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