IBT21
IBT21 is an endoplasmic reticulum stress inhibitor that binds to unfolded or misfolded proteins and prevents their aggregation. IBT21 inhibits UPR activation of the ATF6, IRE1 and PERK branches under ER stress, with IC50 values of 0.24 μM, 0.33 μM, and 0.46 μM, respectively. IBT21 protects cells from ER stress-induced death and mutant prion protein (protein toxin)-induced growth inhibition. IBT21 exhibits chemical chaperone activity distinct from UPR modulators, does not affect protein translation, moderately reduces DTT (HY-15917)-induced ER stress, and fails to inhibit the heat shock response. IBT21 is useful for research related to prion diseases.
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- CAS 番号: 692744-81-3
- 分子式: C16H12N2O2S2
- 分子量:328.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
IBT21 (0.5-5 μM; overnight) inhibits UPR activation in HEK293A cells with an IC50 of 0.61 μM[1].
IBT21 is a more potent inhibitor of Tm-induced UPR activation in HEK293A and Hap1 cells, with an IC50 of 0.95 μM[1].
IBT21 inhibits the three branches of the UPR in HEK293A cells in a dose-dependent manner, with IC50 values of 0.24 μM for ATF6, 0.33 μM for IRE1, and 0.46 μM for PERK[1].
IBT21 (10 μM; overnight) inhibits the induction of downstream target genes of all three branches of the UPR in HEK293A cells, supporting its role as a chemical chaperone[1].
IBT21 (10 μM; overnight) reduces the levels of Tm-induced SDS-resistant HMW BiP-containing complexes in HEK293A cells and prevents the aggregation of 125 proteins induced by Tm, including ER client proteins and protein homeostasis-related proteins[1].
IBT21 (10 μM; overnight) directly inhibits intracellular protein aggregation and acts as a chemical chaperone in in vitro assays using human insulin at a concentration 100-fold lower than that of 4PBA[1].
IBT21 (1-10 μM; 3 h) directly binds a large number of unfolded or misfolded proteins in HEK293A cells under ER stress, and significantly overlaps with the proteins whose aggregation it prevents, supporting its direct chemical chaperone mechanism[1].
IBT21 (1-10 μM; 48 h) protects HEK293A cells against ER stress-induced cell death by restoring cell proliferation and viability in a dose-dependent manner[1].
IBT21 (5 μM; 0-72 h) protects HEK293T cells against cytotoxicity induced by mutant prion protein overexpression and restores cell growth and viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293A
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Concentration:10 μM
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Incubation Time:overnight
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Result:Abolished the Tm-induced increases in the levels of ATF4, GADD34, and CHOP in a dose-dependent manner.
Decreased the levels of DNAJB9, SEL1L and HERPUD1 induced by Tm.\nSuppressed the Tm-induced increase of BiP in the AGGREGATED fraction from 3.1-fold to 1.7-fold of untreated.
Prevented the Tm-induced aggregation of 125 proteins, including ANXA1, TAGLN2, HSPA5, and PDIA4.
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Cell Line:HEK293A
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Concentration:1, 5, 10 μM
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Incubation Time:48 h
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Result:Restored cell growth inhibited by Tm to 69.8% of untreated at 1 μM.
Stimulated cell growth to 112.7% and 115.8% of untreated cells at 5 μM and 10 μM, respectively.
Attenuated viability loss and cell death in a dose-dependent manner.
化学情報
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CAS 番号 692744-81-3
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分子量 328.41
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分子式 C16H12N2O2S2
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SMILES
O=S(C1=CC=C2C(SC3=NC(C4=CC=CC=C4)=CN32)=C1)(C)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)