2. PROTAC Metabolic Enzyme/Protease
  3. PROTACs Indoleamine 2,3-Dioxygenase (IDO)
  4. NU227326

NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer.
(Pink: IDO1 ligand (HY-173067); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-173068)).

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

NU227326

NU227326 Chemical Structure

CAS No. : 3048196-52-4

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Customer Review

Based on 1 publication(s) in Google Scholar

NU227326 Related Antibodies

Top Publications Citing Use of Products

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IDO1 IDO2 IDO

  • Biological Activity

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Description

NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer[1]. (Pink: IDO1 ligand (HY-173067); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-173068)).

IC50 & Target[1]

IDO1

4.5 nM (DC50)

Cereblon

 

In Vitro

NU227326 (4.5 nM; 24 h) potently degrades IDO1 in U87-HiBit-IDO1 human glioblastoma (GBM) cells, with a DC50 of 4.5 nM and a maximum degradation efficiency of 63%[1].
NU227326 (0.001-10 μM; 24 h) induces dose-dependent degradation of IDO1 in IFNγ-stimulated human U87 glioblastoma (GBM) cells, with a degradation rate of 88% at 100 nM after 24 h, and a hook effect is observed at higher concentrations[1].
NU227326 (0.001-10 μM; 24 h) reduces kynurenine production in IFNγ-stimulated human U87 glioblastoma (GBM) cells in a dose-dependent manner, and its inhibitory effect persists despite a hook effect on IDO1 protein levels[1].
NU227326 (100 nM; 0-24 h) initiates IDO1 degradation between 8 and 16 hours and sustains continuous degradation within 24 hours in IFNγ-stimulated human U87 glioblastoma (GBM) cells[1].
NU227326 (50-100 nM; 24-72 h) induces persistent degradation of IDO1 in IFNγ-stimulated human U87 glioblastoma (GBM) cells; the effect lasts up to 72 hours with continuous treatment, and persists for 48 hours when cells are subjected to 24-hour pulse treatment followed by 0-48 hours of washout[1].
NU227326 (100 nM; 24 h) mediates IDO1 degradation in IFNγ-stimulated human U87 glioblastoma (GBM) cells, a process that requires binding to the active site of IDO1, recruitment of the CRL4CRBN E3 ubiquitin ligase complex, and functional proteasomal activity[1].
NU227326 (50-100 nM; 24 h) potently and dose-dependently degrades IDO1 in multiple human cancer cell lines stimulated with IFNγ, including glioblastoma multiforme (GBM) models, prostate cancer cells, breast cancer cells, pancreatic cancer cells, and ovarian cancer cells, and this effect occurs after treatment at 50 or 100 nM for 24 h[1].
NU227326 binds directly to CRBN (Kd = 380 nM) and IDO1 (Kd = 140 nM), and forms a stable ternary complex with IDO1 and CRBN[1].
NU227326 (1 μM; 24 h) exhibits high selectivity for IDO1 degradation, with only a small number of off-target proteins (ADO, EPHX2, CDK8, SALL4, ITCH) being significantly degraded in Kelly human neuroblastoma cells after treatment with 1 μM for 24 h[1].

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

NU227326 Related Antibodies

Western Blot Analysis[1]

Cell Line: U87 human GBM cells
Concentration: 0.001, 0.01, 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Induced dose-dependent IDO1 degradation, with maximum degradation (88% reduction) observed at 100 nM.
Increased IDO1 levels at concentrations above 100 nM due to the hook effect.

Western Blot Analysis[1]

Cell Line: U87 human GBM cells
Concentration: 100 nM
Incubation Time: 0, 1, 2, 4, 8, 16, 24 h
Result: Initiated IDO1 degradation between 8 and 16 hours.
Reduced IDO1 levels to 34% of baseline at 16 hours and 26% at 24 hours.

Western Blot Analysis[1]

Cell Line: U87 human GBM cells
Concentration: 50, 100 nM (continuous treatment); 50, 100 nM (pulse treatment)
Incubation Time: 24-72 h (continuous treatment); 24 h pulse, followed by 0-48 h washout
Result: Maintained reduced IDO1 levels for up to 72 hours with continuous treatment with 50 or 100 nM.
Sustained degradation effect significantly for at least 48 hours post-washout after a 24-hour pulse treatment with 50 or 100 nM.

Western Blot Analysis[1]

Cell Line: U87 human GBM cells
Concentration: 100 nM (in combination with pathway inhibitors: NU223618 250 nM, BGB-7204 1 μM, pomalidomide 1 μM, MLN4924 1 μM, MG132 1 μM)
Incubation Time: 24 h
Result: Was blocked by cotreatment with NU223618, pomalidomide, MLN4924, or MG132.
Was not affected by cotreatment with BGB-7204.

Western Blot Analysis[1]

Cell Line: GBM43 human GBM cells, PDX-6 and PDX-38 human adult GBM patient-derived xenograft lines, U87-GFP-IDO1 human GBM cells, PC-3 human prostate cancer cells, KNS-42 human pediatric GBM cells, MDA-MB-231 human triple-negative breast cancer cells, SW-1990 human pancreatic cancer cells, SKOV-3 human ovarian cancer cells
Concentration: 50, 100 nM
Incubation Time: 24 h
Result: Consistently induced potent, dose-dependent degradation of IDO1 in all tested cell lines.
Molecular Weight

941.10

Formula

C53H61FN8O7
CAS No.
SMILES

O=C(NC1=CC=CC(OC2CCN(C(CN3CCC(N4CCN(C5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5)CC4)CC3)=O)CC2)=C1)[C@H](C)[C@@]8([H])CC[C@](C9=C%10C(C=CC(F)=C%10)=NC=C9)([H])CC8
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
References
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NU227326 Related Classifications

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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:

NU2273263048196-52-4NU 227326NU-227326PROTACsIndoleamine 2,3-Dioxygenase (IDO)CRBNubiquitin-proteasome systemkynureninecereblonglioblastomaprostate cancertriple negative breast cancerIDO1Indoleamine 23-dioxygenase 1U87-HiBit-IDO1 human GBM cellsInhibitorinhibitorinhibit

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