MDM-2/p53 Activator

YO-2 is a plasmin inhibitor and TP53 upregulator with anti-tumor and apoptosis-inducing activities. YO-2 upregulates the expression of TP53 and the tumor-suppressive miR-103/107, downregulates LRP1, and induces cellular DNA fragmentation and caspase cascade activation. YO-2 effectively blocks the growth of melanoma. YO-2 has been widely used in studies related to melanoma and colon cancer.

IG-105 is an orally active and potent tubulin inhibitor that competitively inhibits [³H] colchicine binding to tubulin with an IC₅₀ of 0.6 μM and inhibits tubulin polymerization with an IC₅₀ of 3 μM. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces G2-M phase arrest, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation, inducing apoptosis. IG-105 effectively overcomes multidrug resistance as a non-Pgp substrate. IG-105 can be used for research on leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer, and colon cancer.

HX531 (Standard) is the analytical standard of HX531 (HY-108521). This product is intended for research and analytical applications. HX531 is an orally active RXR antagonist with an IC₅₀ of 18 nM. HX531 upregulates the p53-p21Cip1 pathway. HX531 abrogates the anti-apoptotic effect of t-RA. HX531 exerts anti-obesity, anti-diabetic and anti-melanoma activities.

N-Desmethyl clomipramine-d₆ (Desmethylclomipramine-d₆; Norclomipramine-d₆) is the deuterated-labeled N-Desmethyl clomipramine (HY-12388). N-Desmethyl clomipramine (Desmethylclomipramine; Norclomipramine) is the orally active major active metabolite of the tricyclic antidepressant Clomipramine (HY-B0457A), possessing multiple activities including anti-inflammatory, antioxidant, antibacterial, and antiparasitic effects. N-Desmethyl clomipramine blocks autophagosome-lysosome fusion, leading to the accumulation of LC3-II, p62, ATG7, WIPI2, and ATG5-12, reactivates the p53/p21 pathway, induces apoptosis through C-PARP and C-CAS3, and inhibits the proliferation, migration, and invasion of renal cancer cells. N-Desmethyl clomipramine inhibits LdTOPIA, inducing R-loop accumulation in the nucleus of Leishmania, ultimately causing parasite death. N-Desmethyl clomipramine can be used for research on depression, metastatic renal cell carcinoma, and leishmaniasis.

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.

TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC₅₀ of 5.90 μM) and the cell viability of p53 expressing A549R (IC₅₀ of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models.