INNO-220
Based on 1 Customer Validation
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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- 純度: 98.60%
- CAS 番号: 3032576-92-1
- 分子式: C23H20N4O3
- 分子量:400.43
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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.
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Cell Line:18 B-cell lymphoma cell lines, multiple wild-type p53 cell lines, DLBCL and MCL patients' cells
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Concentration:0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM
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Incubation Time:24 h, 72 h
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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.
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Cell Line:OCI-Ly3 cells
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Concentration:2 nM, 10 nM, 50 nM, 250 nM, 1250 nM
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner.
Cleaved PARP and Caspase 3/8/9 expression increased.
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Cell Line:OCI-Ly3 cells
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Concentration:2 nM, 10 nM, 50 nM, 250 nM, 1250 nM
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Incubation Time:24 h
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Result:Significantly increased the proportion of cells in the G0/G1 phase and decreased the proportion in the S/G2/M phase.
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Cell Line:OCI-Ly3 cells, Z-138 cells
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Concentration:50 nM
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Incubation Time:8 h
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Result:Up-regulated the expression of p53 target genes (CDKN1A, BAX, MDM2) and down-regulated NF-κB target genes.
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Cell Line:OCI-Ly3 cells, Z-138 cells, MOLT-4 cells, OCI-Ly19 cells
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Concentration:2 nM, 10 nM, 50 nM, 250 nM, 1250 nM
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Incubation Time:6 h, 8 h, 24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DLBCL xenograft model established in nude male mice (4 weeks)[1]
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Dosage:3 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:Daily Oral gavage (i.g.), at the corresponding doses for 43 days.
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Result:Significantly inhibited tumor growth at 20 mg/kg.
Degraded CK1α, upregulated p53 expression, and reduced Ki67 levels in tumor tissues.
化学情報
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CAS 番号 3032576-92-1
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性状 Solid
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分子量 400.43
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分子式 C23H20N4O3
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Color White to off-white
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SMILES
CN1N=CC(C2=CC3=C(C(N(C3)C4CCC(NC4=O)=O)=O)C=C2)=C1C5=CC=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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取扱説明書 (2659 KB)
参考文献
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 |