Cat. No.: HY-174371

INNO-220

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INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.

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Pureté: 98.60%
CAS No.: 3032576-92-1
Formule: C₂₃H₂₀N₄O₃
Masse moléculaire:400.43

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

INNO-220 Chemical Structure

CAS No.: 3032576-92-1

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Fluorescent Dye

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

Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Casein Kinase :

In Vitro

INNO-220 (Compound INNO-220) (0.0001-10 μM, 24-72 h) demonstrates broad-spectrum antiproliferative effects against wild-type p53-expressing lymphoma cell lines^[1].

INNO-220 (0.0001-10 μM, 24-72 h) inhibits IL-2 in a CRBN-dependent manner^[1].

INNO-220 (2-1250 nM, 24 h) inhibits the growth of lymphoma cells by activating the apoptotic pathway and inducing cell cycle arrest at the G0/G1 phase^[1].

INNO-220 (50 nM, 8 h) modulates the p53/NF-κB signaling pathway in OCI-Ly3 and Z-138 cells^[1].

INNO-220 (2-1250 nM, 6-24 h) activates p53 via CK1α degradation in OCI-Ly3, Z-138, and OCI-Ly19 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

18 B-cell lymphoma cell lines, multiple wild-type p53 cell lines, DLBCL and MCL patients' cells
Concentration:

0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time:

24 h, 72 h
Result:

Significantly inhibited the viability of wild-type p53 lymphoma cell lines (OCI-Ly3 cells, OCI-Ly10 cells, TMD8 cells, OCI-Ly19 cells, Will-2 cells, Z-138 cells).
Significantly reduced the viability of primary patient cells.
Significantly inhibited IL-2 secretion, while having minimal effect on cell viability of PBMC and THLE-2 cells.
Had no inhibitory effect on IL-2 in CRBN knockout Jurkat cells.

Apoptosis Analysis^[1]

Cell Line:

OCI-Ly3 cells
Concentration:

2 nM, 10 nM, 50 nM, 250 nM, 1250 nM
Incubation Time:

24 h
Result:

Induced apoptosis in a dose-dependent manner.
Cleaved PARP and Caspase 3/8/9 expression increased.

Cell Cycle Analysis^[1]

Cell Line:

OCI-Ly3 cells
Concentration:

2 nM, 10 nM, 50 nM, 250 nM, 1250 nM
Incubation Time:

24 h
Result:

Significantly increased the proportion of cells in the G0/G1 phase and decreased the proportion in the S/G2/M phase.

Real Time qPCR^[1]

Cell Line:

OCI-Ly3 cells, Z-138 cells
Concentration:

50 nM
Incubation Time:

8 h
Result:

Up-regulated the expression of p53 target genes (CDKN1A, BAX, MDM2) and down-regulated NF-κB target genes.

Western Blot Analysis^[1]

Cell Line:

OCI-Ly3 cells, Z-138 cells, MOLT-4 cells, OCI-Ly19 cells
Concentration:

2 nM, 10 nM, 50 nM, 250 nM, 1250 nM
Incubation Time:

6 h, 8 h, 24 h
Result:

Dose-dependently degraded CK1α (DC50 = 3.8 nM in OCI-Ly3 cells, DC50 = 23.4 nM in Z-138 cells).
Activated the p53 pathway (upregulation of p53, p21, and MDM2), inhibited CBM complex assembly, and suppressed NF-κB signaling.

In Vivo

INNO-220 (Compound INNO-220) (3-20 mg/kg, i.g, daily for 43 days) induces tumor regression in DLBCL and MCL xenograft models and inhibits NF-κB activity without significant changes in mouse body weight, providing a new direction for lymphoma-related research^[1].

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

Animal Model:

DLBCL xenograft model established in nude male mice (4 weeks)^[1]
Dosage:

3 mg/kg, 10 mg/kg, 20 mg/kg
Administration:

Daily Oral gavage (i.g.), at the corresponding doses for 43 days.
Result:

Significantly inhibited tumor growth at 20 mg/kg.
Degraded CK1α, upregulated p53 expression, and reduced Ki67 levels in tumor tissues.

Chemical Information

CAS No. 3032576-92-1
Appearance Solid
Masse moléculaire 400.43
Formule C₂₃H₂₀N₄O₃
Color White to off-white
SMILES

CN1N=CC(C2=CC3=C(C(N(C3)C4CCC(NC4=O)=O)=O)C=C2)=C1C5=CC=CC=C5
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 2.5 mg/mL (6.24 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

2.4973 mL

12.4866 mL

24.9732 mL

5 mM

0.4995 mL

2.4973 mL

4.9946 mL

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Shi Feng, et al. A highly selective and orally bioavailable casein kinase 1 alpha degrader through p53 signaling pathway targets B-cell lymphoma cells. Leukemia. 2025 May 27. [Content Brief]

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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4973 mL	12.4866 mL	24.9732 mL	62.4329 mL
DMSO	5 mM	0.4995 mL	2.4973 mL	4.9946 mL	12.4866 mL

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INNO-220

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Ferroptosis Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Cancer Stem Cells Compound Library

Molecular Glue Compound Library

Protease Inhibitor Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform Casein Kinase