Checkpoint Kinase (Chk) Activator

Benfluron hydrochloride is an Apoptosis inducer and inhibitor of the HIV-1 Rev-RRE complex, with an IC₅₀ of 5.0 μM against the HIV-1 Rev-RRE complex. Benfluron hydrochloride induces p53 activation, and triggers phosphorylation of Chk1 at serine 345, Chk2 at threonine 68, as well as ERK1/2 at threonine 202 and tyrosine 204. Benfluron hydrochloride activates Caspase 8, Caspase 9 and Caspase 3/7, inhibits HIV-1 viral transcription, and acts as a substrate for 11β-HSD 1 and cytosolic carbonyl reductase. Benfluron hydrochloride can be used in research related to leukemia and HIV-1 infection.

Tubulozole hydrochloride (R 46846 hydrochloride) is an orally active inhibitor of tubulin polymerization with an ID₅₀ of 0.34 μM. Tubulozole hydrochloride induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole hydrochloride arrests Mitosis at the metaphase stage. Tubulozole hydrochloride causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole hydrochloride exerts anticancer activity against colon cancer. Tubulozole hydrochloride produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole hydrochloride is used in studies related to colon cancer, fascioliasis, MO4 fibrosarcoma, and Lewis lung carcinoma.

CX-5461 (Standard) is the analytical standard of CX-5461 (HY-13323). This product is intended for research and analytical applications. CX-5461 is a selective, orally active RNA polymerase I inhibitor. CX-5461 disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors.