DIQ01 | KHSRP inhibitor | Probechem Biochemicals

Chemical Structure : DIQ01

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DIQ01 (DIQ-01)

货号: PC-27659Not For Human Use, Lab Use Only.

DIQ01 is a specific small-molecule inhibitor of KH-type splicing regulatory protein (KHSRP), targets KH3 domain of KHSRP (MST Kd=387.4 nM) and disrupts RNA binding, exhibits potent antitumor efficacy.

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生物&药学活性

DIQ01 is a specific small-molecule inhibitor of KH-type splicing regulatory protein (KHSRP), targets KH3 domain of KHSRP (MST Kd=387.4 nM) and disrupts RNA binding, exhibits potent antitumor efficacy.
DIQ01 exhibits superior activity against three distinct cancer cell lines, with IC50 of 64.7 nM for HCT116 colorectal cancer model.
DIQ01 functionally inactivates KHSRP, triggering destabilization and downregulation of its target PLK1 mRNA.
DIQ01 induces irreparable DNA damage in cancer cells, induces S-phase arrest in HCT116 colorectal cancer cells, significantly decreases the expression levels of key cell cycle and proliferation-regulatory proteins, such as CDK2, CDK4, and c-Myc, while upregulating p53 in a dose-dependent manner.
DIQ01 targets the KH3 domain of KHSRP and disrupts RNA binding, disrupts KHSRP-RNA binding in a concentration-dependent manner with IC50 values of 2.82 uM for full-length KHSRP.
DIQ01 inhibits PRMT5-mediated methylation of KHSRP.
DIQ01 (3-6 mg/kg, i.v.) suppresses KHSRP-dependent colorectal cancer growth in vivo, exhibits robust antiproliferative activity with IC50 of 0.85 uM for patient-derived colorectal cancer organoid models.
KHSRP is a multifunctional RNA-binding protein that promotes the decay of AU-rich element (ARE)-containing mRNAs and regulates microRNA biogenesis.

物理化学性质&存储条件

分子量	392.43
分子式	C22H16N8
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(3-amino-2H-indazol-2-yl)-N-(1H-indazol-3-yl)quinazolin-4-amine

参考文献

1. Chen S, et al. Acta Pharm Sin B. 2026 Aug;16(8):5237-5258.

DIQ01 (DIQ-01)

生物&药学活性

物理化学性质&存储条件

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DIQ01 (DIQ-01)

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物理化学性质&存储条件

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