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[1].

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INNO-220 Chemical Structure

INNO-220 Chemical Structure

CAS No. : 3032576-92-1

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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.
SMILES

CN1N=CC(C2=CC3=C(C(N(C3)C4CCC(NC4=O)=O)=O)C=C2)=C1C5=CC=CC=C5
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INNO-220 Related Classifications

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    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

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