ccrcc

Crenigacestat (LY3039478) is an orally bioavailable Notch inhibitor with an IC50 of ~1 nM in most tumor cell lines tested. It effectively inhibits mutant Notch receptor activity and, in a xenograft tumor model, inhibits the expression of Notch-regulated genes and N1ICD cleavage in the tumor microenvironment.

CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.

Belzutifan (MK-6482) is a potential treatment for clear cell renal cell carcinoma (ccRCC). Belzutifan is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). Belzutifan , as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile.

Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.

SPOP-IN-2 (Compound E1) is a potent inhibitor of speckle-type POZ protein (SPOP), with an IC50 of 0.58 μM. It disrupts the interaction between SPOP and substrates and selectively inhibits the proliferation of clear cell renal cell carcinoma (ccRCC).

Antitumor agent-180 (Compound 13a) is an inhibitor of BUB1 mitotic checkpoint serine/threonine kinase B (BUB1B). It suppresses the proliferation of ccRCC cells Caki-1 with an IC50 of 2.047 µM and induces necrosis and apoptosis in Caki-1 cells.

DDO-4033 is an SPOP inhibitor with an IC50 of 16.9 μM and a Kd of 15.1 μM. It hinders the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts the recruitment of the substrate LATS1 by SPOP, inhibiting its polyubiquitination and subsequent degradation, which leads to the upregulation of LATS1 expression. This compound demonstrates significant antitumor activity and can be utilized in renal cell carcinoma research.

HIF-1/2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α. Its inhibitory effect on HIF-2α activity is significant, with an IC 50 value of 0.92 μM. Furthermore, HIF-1/2α-IN-1 has the ability to decrease HIF-1α levels. This compound is particularly valuable for research on clear cell renal cell carcinoma (ccRCC) [1].

XPW1 is a new potent and selective CDK9 inhibitor with antitumour activity that transcriptionally inhibits the DNA repair process in ccRCC cells.XPW1 can be used to study clear cell renal cell carcinoma.

Casdaitifan (AB521) is an orally active hypoxia inducible factor 2 alpha (HIF-2 alpha) inhibitor. Casdaitifan exhibits significant anti-tumor effects in the clear cell renal cell carcinoma (ccRCC) model.

NVP-DFF332 is a HIF-2 inhibitor that can be used in ccRCC related research