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Cat. No.: HY-157577

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PROTAC(H-PGDS)-8

PROTAC (H-PGDS)-8 is an H-PGDS PROTAC inhibitor with a IC₅₀ of 0.14 μM. PROTAC (H-PGDS)-8 binds to H-PGDS and inhibits its enzymatic activity. PROTAC (H-PGDS)-8 inhibits the production of PGD₂ in cancer cells. PROTAC (H-PGDS)-8 can be used for the research of Duchenne muscular dystrophy.
(Pink: Target protein ligand; Blue: Cereblon ligand (HY-W460193); Black: linker).

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

CAS No.: 2761281-51-8
Formula: C₄₁H₄₀N₈O₇
Molecular Weight:756.81

Storage:

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

Data Sheet (274 KB)

PROTAC(H-PGDS)-8 Chemical Structure

CAS No.: 2761281-51-8

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC (H-PGDS)-8 is an H-PGDS PROTAC inhibitor with a IC₅₀ of 0.14 μM. PROTAC (H-PGDS)-8 binds to H-PGDS and inhibits its enzymatic activity. PROTAC (H-PGDS)-8 inhibits the production of PGD₂ in cancer cells. PROTAC (H-PGDS)-8 can be used for the research of Duchenne muscular dystrophy^[1]. (Pink: Target protein ligand; Blue: Cereblon ligand (HY-W460193); Black: linker).

IC₅₀ & Target^[1]

H-PGDS

0.14 μM (IC₅₀)

All PROTACs Isoforms :

All Prostaglandin Receptor Isoforms :

In Vitro

PROTAC(H-PGDS)-8 (0-10000 pM; 6 h) does not induce degradation of H-PGDS protein in KU812 cells at concentrations up to 10000 pM over 6 h^[1].
PROTAC(H-PGDS)-8 (2.44 nM-2.50 μM; 1 h) binds to recombinant human H-PGDS protein with an IC₅₀ of 0.14 μM^[1].
PROTAC(H-PGDS)-8 (100-3000 pM; 6 h) suppresses PGD₂ production in KU812 cells at concentrations ≥1000 pM after 6 h incubation, with less potent activity than PROTAC(H-PGDS)-7 (compound 6)^[1].

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

Western Blot Analysis^[1]

Cell Line:

KU812 cells
Concentration:

0, 10, 100, 1000, 10000 pM
Incubation Time:

6 h
Result:

Showed no reduction of H-PGDS protein levels across all tested concentrations and incubation time, with H-PGDS expression remaining at ~90-100% of the DMSO-treated control.

Chemical Information

CAS No. 2761281-51-8
Molecular Weight 756.81
Formula C₄₁H₄₀N₈O₇
SMILES

O=C(C1CCN(CC1)C2=CC=C(C=C2)NC(C3=CN=C(N=C3)OC4=CC=CC=C4)=O)N5CCN(CC5)C6=C(C7=CC=C6)C(N(C7=O)C8CCC(N(C8=O)C)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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)

References

[1]. Yokoo H, et al. Discovery of a Highly Potent and Selective Degrader Targeting Hematopoietic Prostaglandin D Synthase via In Silico Design. Journal of medicinal chemistry. 2021 Nov 11;64(21):15868-15882. [Content Brief]

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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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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PROTAC(H-PGDS)-8

All PROTACs Isoforms

All Prostaglandin Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC(H-PGDS)-8 Related Classifications

HY-157577 Related Classifications