Cat. No.: HY-139972

PROTAC(H-PGDS)-7

Name: PROTAC(H-PGDS)-7
Brand: MedChemExpress
SKU: HY-139972
Price: 160.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

PROTAC (H-PGDS)-7 is a selective, linker-free H-PGDS PROTAC degrader with a DC₅₀ of 17.3 pM. PROTAC (H-PGDS)-7 binds to CRBN and forms a ternary complex with H-PGDS, inducing the degradation of H-PGDS via the ubiquitin-proteasome system through polyubiquitination and proteasomal degradation processes. PROTAC (H-PGDS)-7 inhibits the upregulated expression of TNFα, IL-1β, TGFβ1 and CD11b in mice with cardiac hypertrophy models. PROTAC (H-PGDS)-7 can be used in studies related to Duchenne muscular dystrophy and allergic diseases.
(Pink: ligand (HY-110167); Blue: Cereblon ligand (HY-41547); Black: linker).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.42%
CAS No.: 2761281-50-7
화학식: C₄₀H₃₈N₈O₇
분자량:742.78

보관:

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

PROTAC(H-PGDS)-7 Chemical Structure

CAS No.: 2761281-50-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

PROTAC (H-PGDS)-7 is a selective, linker-free H-PGDS PROTAC degrader with a DC₅₀ of 17.3 pM. PROTAC (H-PGDS)-7 binds to CRBN and forms a ternary complex with H-PGDS, inducing the degradation of H-PGDS via the ubiquitin-proteasome system through polyubiquitination and proteasomal degradation processes. PROTAC (H-PGDS)-7 inhibits the upregulated expression of TNFα, IL-1β, TGFβ1 and CD11b in mice with cardiac hypertrophy models. PROTAC (H-PGDS)-7 can be used in studies related to Duchenne muscular dystrophy and allergic diseases^[1]^[2]^[3]. (Pink: ligand (HY-110167); Blue: Cereblon ligand (HY-41547); Black: linker).

IC₅₀ & Target

^[1]

Cereblon

IL-1β

All PROTACs Isoforms :

All TNF Receptor Isoforms :

All TGF-β Receptor Isoforms :

All Interleukin Related Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
KU812 cell line	DC₅₀	26.3 pM	Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells after 6 h incubation, measured via Western blot relative to β-actin. Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells after 6 h incubation, measured via Western blot relative to β-actin.	34652145
KU812 cell line	DC₅₀	17.3 pM	Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells after 24 h incubation, measured via Western blot relative to β-actin. Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells after 24 h incubation, measured via Western blot relative to β-actin.	34652145
KU812 cell line	DC₅₀	0.094 nM	Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells assessed via western blot after 24 h incubation. Half-maximal degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells assessed via western blot after 24 h incubation.	40937104
KU812 cell line	DC₅₀	18.7 pM	Degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells assessed via western blotting after 24 h incubation. Degradation of H-PGDS protein in human chronic myelogenous leukemia KU812 cells assessed via western blotting after 24 h incubation.	36561070

In Vitro

PROTAC(H-PGDS)-7 (0-10000 pM; 6-24 h) potently and selectively degrades H-PGDS protein in KU812 cells via the ubiquitin-proteasome system, with a DC₅₀ of 17.3 pM after 24 h incubation^[1].
PROTAC(H-PGDS)-7 (30-3000 pM; 6 h) potently suppresses PGD₂ production in KU812 cells, with greater efficacy than non-degrading H-PGDS inhibitors^[1].
PROTAC(H-PGDS)-7 (24 h) induces concentration-dependent degradation of H-PGDS in KU812 cells with a DC₅₀ of 0.094 nM after 24 h incubation^[2].
PROTAC(H-PGDS)-7 (5-200 pM; 24 h) potently degrades H-PGDS in KU812 cells with a DC₅₀ of 18.7 pM^[3].

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

Western Blot Analysis^[1]

Cell Line:

human chronic myelogenous leukemia KU812 cells
Concentration:

0-10000 pM (24 h incubation: 0,10,30,100 pM; 6 h incubation: 0,10,100,1000,10000 pM)
Incubation Time:

6 h, 24 h
Result:

Showed potent dose-dependent reduction of H-PGDS protein levels in KU812 cells.
Achieved a half-maximal degradation concentration (DC₅₀) of 26.3 pM after 6 h of incubation and 17.3 pM after 24 h of incubation.
Reduced H-PGDS protein levels to ~30.8% of vehicle control levels at 100 pM with 6 h treatment.
Reduced H-PGDS protein levels to ~12.9% of vehicle control levels at 10 nM with 6 h treatment.

In Vivo

Cytokines & Chemokines

PROTAC(H-PGDS)-7 (45 mg/kg; s.c.; daily; 14 days) shows greater activity than a conventional H-PGDS inhibitor at suppressing T3-induced upregulation of inflammatory and fibrosis-related cardiac gene expression in mdx mice with cardiac hypertrophy^[1].

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

Animal Model:

mdx mice (male, 9-12 weeks old, dystrophin-deficient, cardiac hypertrophy induced by subcutaneous injection of 2 mg/kg/day T3 for 14 days)^[1]
Dosage:

45 mg/kg
Administration:

s.c.; daily; 14 days
Result:

Suppressed the T3-induced upregulation of cardiac mRNA levels of TNFα, IL-1β, TGFβ1, and CD11b.

Related Protocols :

Chemical Information

CAS No. 2761281-50-7
Appearance Solid
분자량 742.78
화학식 C₄₀H₃₈N₈O₇
Color Light yellow to yellow
SMILES

O=C(C1CCN(C2=CC=C(NC(C3=CN=C(OC4=CC=CC=C4)N=C3)=O)C=C2)CC1)N5CCN(C6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)CC5
선적

Room temperature in continental US; may vary elsewhere.
보관

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

용액&용해도

In Vitro:

DMSO : 100 mg/mL (134.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.3463 mL

6.7315 mL

13.4629 mL

5 mM

0.2693 mL

1.3463 mL

2.6926 mL

10 mM

0.1346 mL

0.6731 mL

1.3463 mL

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]

[2]. Osawa H, et al. Optimizing linker rigidity to improve intracellular behavior of PROTACs targeting hematopoietic prostaglandin D synthase. RSC medicinal chemistry. 2025 Sep 02;16(10):4721-30.

[3]. Murakami Y, et al. Structure-activity relationship study of PROTACs against hematopoietic prostaglandin D synthase. RSC medicinal chemistry. 2022 Dec 14;13(12):1495-1503.

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.3463 mL	6.7315 mL	13.4629 mL	33.6573 mL
	5 mM	0.2693 mL	1.3463 mL	2.6926 mL	6.7315 mL
	10 mM	0.1346 mL	0.6731 mL	1.3463 mL	3.3657 mL
	15 mM	0.0898 mL	0.4488 mL	0.8975 mL	2.2438 mL
	20 mM	0.0673 mL	0.3366 mL	0.6731 mL	1.6829 mL
	25 mM	0.0539 mL	0.2693 mL	0.5385 mL	1.3463 mL
	30 mM	0.0449 mL	0.2244 mL	0.4488 mL	1.1219 mL
	40 mM	0.0337 mL	0.1683 mL	0.3366 mL	0.8414 mL
	50 mM	0.0269 mL	0.1346 mL	0.2693 mL	0.6731 mL
	60 mM	0.0224 mL	0.1122 mL	0.2244 mL	0.5610 mL
	80 mM	0.0168 mL	0.0841 mL	0.1683 mL	0.4207 mL
	100 mM	0.0135 mL	0.0673 mL	0.1346 mL	0.3366 mL

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PROTAC(H-PGDS)-7

All PROTACs Isoforms

All TNF Receptor Isoforms

All TGF-β Receptor Isoforms

All Interleukin Related Isoforms