2. PROTAC Stem Cell/Wnt Cell Cycle/DNA Damage Apoptosis NF-κB Metabolic Enzyme/Protease
  3. Molecular Glues Casein Kinase MDM-2/p53 MALT1
  4. INNO-220

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.

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

INNO-220

INNO-220 Chemical Structure

CAS No. : 3032576-92-1

Size Price Stock Quantity
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

INNO-220 Related Antibodies

Top Publications Citing Use of Products

View All Casein Kinase Isoform Specific Products:

View All Isoforms
CK1 CK2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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.

INNO-220 Related Antibodies

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.
Molecular Weight

400.43

Formula

C23H20N4O3
CAS No.
Appearance

Solid

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7 mg/mL (17.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4973 mL 12.4866 mL 24.9732 mL
5 mM 0.4995 mL 2.4973 mL 4.9946 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
5 mM 0.4995 mL 2.4973 mL 4.9946 mL 12.4866 mL
10 mM 0.2497 mL 1.2487 mL 2.4973 mL 6.2433 mL
15 mM 0.1665 mL 0.8324 mL 1.6649 mL 4.1622 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

INNO-220 Related Classifications

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:

INNO-2203032576-92-1INNO220INNO 220Molecular GluesCasein KinaseMDM-2/p53MALT1mucosa associated lymphoid tissue lymphoma translocation gene 1DLBCL/MCL cellsCK1αlymphomaCRBNDLBCL/MCL xenograft modelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
INNO-220
Cat. No.:
HY-174371
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.