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Art. -Nr.: HY-158048

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UNC9036

UNC9036 is a STING PROTAC degrader with a DC₅₀ value of 227 nM. UNC9036 binds to and activates STING, recruits the VHL E3 ligase to target phosphorylated STING for ubiquitination and proteasomal degradation. UNC9036 inhibits downstream innate immune signaling events triggered by cytoplasmic DNA sensing, including IRF3 phosphorylation. UNC9036 reduces the antiviral response of cells infected with HSV-1. UNC9036 can be used in the research of renal cell carcinoma.
(Pink: STING ligand (HY-184545); Blue: VHL ligand (HY-138678B); Black: linker (HY-W105727)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3094059-54-5
Formel: C₇₃H₉₅N₁₇O₁₁S
Molecular Weight:1418.71

Speicherung:

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

Data Sheet (275 KB)

UNC9036 Chemical Structure

CAS. Nr.: 3094059-54-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

UNC9036 is a STING PROTAC degrader with a DC₅₀ value of 227 nM. UNC9036 binds to and activates STING, recruits the VHL E3 ligase to target phosphorylated STING for ubiquitination and proteasomal degradation. UNC9036 inhibits downstream innate immune signaling events triggered by cytoplasmic DNA sensing, including IRF3 phosphorylation. UNC9036 reduces the antiviral response of cells infected with HSV-1. UNC9036 can be used in the research of renal cell carcinoma^[1]. (Pink: STING ligand (HY-184545); Blue: VHL ligand (HY-138678B); Black: linker (HY-W105727)).

IC₅₀ & Target^[1]

VHL

HSV-1

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle HSV Isoform-spezifische Produkte anzeigen :

In Vitro

UNC9036 (0-31.6 μM; 0-24 h) potently degrades STING in Caki-1 renal cell carcinoma cells with a DC₅₀ of 227 nM and achieves 91.68% maximal degradation after 24 h, with significant degradation detectable within 8 h^[1].
UNC9036 (5 μM; 24 h) degrades wild-type, cGAMP binding-deficient (R238A), and TBK1 phosphorylation-deficient (S366A) STING, but does not degrade trafficking-deficient (EDAA) or palmitoylation/activation-deficient (CACA) STING in Caki-1 renal cell carcinoma cells^[1].
UNC9036 (0.316 μM; 6 h) dampens STING-mediated DNA sensing signaling in Caki-1 renal cell carcinoma cells by reducing STING protein levels and suppressing ISD90-induced and 2'3'-cGAMP-induced IRF3 phosphorylation, while having minimal effect on poly(I:C)-induced IRF3 phosphorylation^[1].
UNC9036 (3 μM; 16 h) treatment significantly reduces the anti-viral response in Caki-1 renal cell carcinoma cells infected with HSV-1, as evidenced by increased viral titers compared to DMSO control^[1].

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

Western Blot Analysis^[1]

Cell Line:

Caki-1 renal cell carcinoma cells
Concentration:

0-31.6 μM (dose-response); 1 μM (time-course)
Incubation Time:

24 h (dose-response); 0-24 h (time-course)
Result:

Triggered dose-dependent and time-dependent degradation of STING protein.
Achieved a DC₅₀ of 227 nM and a Dmax of 91.68% after 24 h treatment.
Induced significant STING degradation within 8 h of treatment with 1 μM.

Western Blot Analysis^[1]

Cell Line:

Caki-1 renal cell carcinoma cells (transfected with Flag-tagged wild-type or mutant STING)
Concentration:

5 μM
Incubation Time:

24 h
Result:

Degraded wild-type STING, R238A (2'3'-cGAMP binding-deficient) mutant, and S366A (TBK1 phosphorylation-deficient) mutant.
Failed to degrade EDAA (trafficking-deficient) mutant and CACA (palmitoylation/activation-deficient) mutant.

Western Blot Analysis^[1]

Cell Line:

Caki-1 renal cell carcinoma cells
Concentration:

0.316 μM UNC9036; 5 μg/mL ISD90, 5 μg/mL 2'3'-cGAMP, 5 μg/mL poly(I:C)
Incubation Time:

6 h pre-incubation; 0-6 h stimulation
Result:

Reduced STING protein abundance.
Suppressed ISD90-induced and 2'3'-cGAMP-induced phosphorylated IRF3 signals.
Minimally affected poly(I:C)-induced phosphorylated IRF3 signals.

Chemical Information

CAS. Nr. 3094059-54-5
Molecular Weight 1418.71
Formel C₇₃H₉₅N₁₇O₁₁S
SMILES

O=C(NCCCCCCCCC(N[C@@H](C(N1[C@H](C(NCC2=CC=C(C=C2)C3=C(C)N=CS3)=O)C[C@H](C1)O)=O)C(C)(C)C)=O)C4=CC5=C(C(OC)=C4)N(C/C=C/CN6C(NC(C7=CC(C)=NN7CC)=O)=NC8=C6C(OCCCN9CCOCC9)=CC(C(N)=O)=C8)C(NC(C%10=CC(C)=NN%10CC)=O)=N5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhu Z, et al. Development of VHL-recruiting STING PROTACs that suppress innate immunity. Cellular and molecular life sciences : CMLS. 2023 May 14;80(6):149. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
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UNC9036

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle HSV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

UNC9036 Related Classifications

HY-158048 Related Classifications