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Cat. No.: HY-183995

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SH-26

SH-26 is a PHD1 PROTAC degrader with DC₅₀s of 1.06 μM, 4.16 μM and 4.91 μM in MDA-MB-231, HepG2 and HEK-293T cells, respectively. SH-26 recruits CRBN to induce PHD1 degradation via the ubiquitin-proteasome system. SH-26 attenuates APAP (HY-66005)-triggered ROS accumulation, mitochondrial dysfunction, and NLRP3 inflammasome activation. SH-26 can be used for the research of acute liver injury.
(Pink: HIF/HIF Prolyl-Hydroxylase ligand (HY-183996); Blue: Cereblon ligand (HY-10984); Black: linker).

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Formule: C₃₈H₄₁N₉O₈
Masse moléculaire:751.79

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

SH-26 Chemical Structure

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
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Description

SH-26 is a PHD1 PROTAC degrader with DC₅₀s of 1.06 μM, 4.16 μM and 4.91 μM in MDA-MB-231, HepG2 and HEK-293T cells, respectively. SH-26 recruits CRBN to induce PHD1 degradation via the ubiquitin-proteasome system. SH-26 attenuates APAP (HY-66005)-triggered ROS accumulation, mitochondrial dysfunction, and NLRP3 inflammasome activation. SH-26 can be used for the research of acute liver injury^[1]. (Pink: HIF/HIF Prolyl-Hydroxylase ligand (HY-183996); Blue: Cereblon ligand (HY-10984); Black: linker).

IC₅₀ & Target^[1]

NLRP3 inflammasome

PHD1

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In Vitro

SH-26 (Compound 26) (0.25-10 μM; 2-72 h) induces concentration- and time-dependent PHD1 degradation in MDA-MB-231 cells, with a DC₅₀ of 1.06 μM and a D_max of 77.5% in 48 h^[1].
SH-26 (0.25-50 μM; 48 h) induces concentration-dependent PHD1 degradation in HepG2 cells with a DC₅₀ of 4.16 μM^[1].
SH-26 (0-50 μM; 48 h) induces concentration-dependent PHD1 degradation in HEK-293T cells with a DC₅₀ of 4.91 μM^[1].
SH-26 (2-25 μM; 48 h) mediates PHD1 degradation in MDA-MB-231, HepG2, and HEK-293T cells in a ubiquitin-proteasome system-dependent manner that requires both PHD1 target engagement and CRBN recruitment^[1].
SH-26 (1-25 μM; 4 h pretreatment) degrades PHD1 and PHD2 (but not PHD3) and stabilizes HIF-1α in APAP-challenged AML12 hepatocytes under normoxic conditions^[1].
SH-26 (1-25 μM; 4 h pretreatment) exhibits enhanced concentration-dependent PHD1 degradation (DC₅₀ = 0.13 μM) and stabilizes HIF-1α in APAP-challenged AML12 hepatocytes under hypoxic conditions^[1].
SH-26 (1-50 μM; 4 h pretreatment) protects AML12 hepatocytes from APAP-induced injury in a concentration-dependent manner without inherent cytotoxicity^[1].
SH-26 (1-25 μM; 4 h pretreatment) restores expression of HIF-1α target genes BNIP3 and SLC2A1, does not affect PHD1 mRNA levels, and suppresses IL-1β mRNA levels in APAP-challenged AML12 hepatocytes^[1].
SH-26 (1-50 μM; 4 h pretreatment) dose-dependently degrades PHD1 and suppresses IL-1β protein levels in APAP-challenged AML12 hepatocytes^[1].
SH-26 (1 μM; 24 h) degrades PHD1 and downregulates pro-inflammatory mediators IL-1β, IL-6, and TNF-α in LPS (HY-D1056)+IFN-γ-stimulated THP-1-derived M1 macrophages^[1].
SH-26 (1-25 μM; 4 h pretreatment) dose-dependently reduces mitochondrial reactive oxygen species accumulation in APAP-challenged AML12 hepatocytes^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 breast cancer cells
Concentration:

0.25μM; 0.5 μM; 1 μM; 2 μM; 2.5 μM; 5 μM; 10 μM
Incubation Time:

2 h; 4 h; 8 h; 12 h; 24 h; 48 h; 72 h
Result:

Induced 67% PHD1 degradation at 24 h, 70% at 48 h, and 80% at 72 h at 2 μM.
Induced concentration-dependent PHD1 degradation with a DC₅₀ of 1.06 μM and a maximum degradation (D_max) of 77.5%.
Caused significant degradation within 4 h, with maximal depletion achieved by 72 h.
Showed no hook effect at concentrations up to 10 μM.

Western Blot Analysis^[1]

Cell Line:

HepG2 hepatoma cells
Concentration:

0.25μM; 0.5 μM; 1 μM; 2.5 μM; 5 μM; 10 μM
Incubation Time:

48 h
Result:

Induced concentration-dependent PHD1 degradation with a DC₅₀ of 4.16 μM.

Western Blot Analysis^[1]

Cell Line:

HEK-293T embryonic kidney cells
Concentration:

0.25μM; 0.5 μM; 1 μM; 2.5 μM; 5 μM; 10 μM
Incubation Time:

48 h
Result:

Induced concentration-dependent PHD1 degradation with a DC₅₀ of 4.91 μM.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231, HepG2, and HEK-293T cells
Concentration:

2 μM; 25 μM
Incubation Time:

48 h
Result:

Had its PHD1-degrading activity blocked in all three cell lines when cotreated with MG132, MLN4924, Takeda-54, or SH-28.

Western Blot Analysis^[1]

Cell Line:

AML12 hepatocytes
Concentration:

1 μM; 2.5 μM; 5 μM; 10 μM; 25 μM
Incubation Time:

4 h pretreatment
Result:

Degraded PHD1 in a concentration-dependent manner.
Degraded PHD2 with a DC₅₀ of 1.83 μM and a D_max of 71.8%.
Did not degrade PHD3.
Stabilized HIF-1α in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:

AML12 hepatocytes
Concentration:

1 μM; 2.5 μM; 5 μM; 10 μM; 25 μM
Incubation Time:

4 h pretreatment
Result:

Exhibited enhanced PHD1 degradation under hypoxia with a DC₅₀ of 0.13 μM.
Stabilized HIF-1α in a concentration-dependent manner.

Cell Viability Assay^[1]

Cell Line:

AML12 hepatocytes (APAP-induced injury)
Concentration:

1 μM; 2.5 μM; 5 μM; 10 μM; 25 μM; 50 μM
Incubation Time:

4 h pretreatment
Result:

Attenuated APAP-induced hepatotoxicity in a concentration-dependent manner.
Exhibited no inherent cytotoxicity at tested concentrations.

Real Time qPCR^[1]

Cell Line:

AML12 hepatocytes (APAP-induced injury)
Concentration:

1 μM; 5 μM; 25 μM
Incubation Time:

4 h pretreatment
Result:

Restored BNIP3 mRNA to baseline levels and significantly upregulated SLC2A1 mRNA at 10 μM.
Did not alter PHD1 mRNA levels.
Dose-dependently suppressed IL-1β mRNA levels.

Western Blot Analysis^[1]

Cell Line:

AML12 hepatocytes (APAP-induced injury)
Concentration:

1 μM; 2.5 μM; 5 μM; 10 μM; 25 μM; 50 μM
Incubation Time:

4 h pretreatment
Result:

Dose-dependently degraded PHD1.
Dose-dependently suppressed IL-1β protein levels.

Parmacokinetics

Species	Dose	Route	C_max	T_max	Plasma Concentration
Mice^[1]	30 mg/kg	i.p.	7 μM	0.5 h	~10 nM

In Vivo

SH-26 (Compound 26) (10-30 mg/kg; i.p.; single dose) confers robust hepatoprotective effects in APAP-induced acute liver injury^[1].

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

Animal Model:

C57BL/6 (male, 8 weeks old, APAP-induced acute liver injury)^[1]
Dosage:

10 mg/kg; 30 mg/kg
Administration:

i.p.; single dose
Result:

Significantly reduced serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), creatinine (CRE), and blood urea nitrogen (BUN) at 30 mg/kg.
Markedly attenuated APAP-induced hepatic damage, confirmed by histopathological analysis and necrotic area quantification at 10 mg/kg and 30 mg/kg.
Effectively reversed APAP-induced upregulation of PHD1 protein expression and induced robust PHD1 degradation in liver tissue at 10 mg/kg and 30 mg/kg.
Significantly reduced the upregulation of inflammasome components (NLRP3, GSDMD, cleaved caspase 1, cleaved IL-1β) at 10 mg/kg and 30 mg/kg.
Attenuated pro-apoptotic signals (increased BAX/BCL2 ratio, elevated cleaved caspase 3 levels) at 10 mg/kg and 30 mg/kg.
Significantly reduced liver tissue expression of immune cell markers LY6G, F4/80, CD31, and CD3 at 10 mg/kg and 30 mg/kg.

Chemical Information

Masse moléculaire 751.79
Formule C₃₈H₄₁N₉O₈
SMILES

O=C1N(C(C2=CC=CC(NCCOCCOCCOCCNC(CCNC3=CC4=NC=NN4C(C5=C(C=C(C=C5)C#N)C)=C3)=O)=C21)=O)C6CCC(NC6=O)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Su H, et al. Targeted Degradation of Prolyl Hydroxylase Domain Enzyme 1 (PHD1) as a Novel Therapeutic Strategy for Acetaminophen-Induced Acute Liver Injury. J Med Chem. 2026;69(10):12122-12143. [Content Brief]

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SH-26

Voir tous les produits spécifiques à Isoform PROTACs

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase

Voir tous les produits spécifiques à Isoform NOD-like Receptor (NLR)

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SH-26 Related Classifications

Cat. No.: HY-183995