spop

SPOP-IN-6b is an effective inhibitor of speckle-type POZ protein (SPOP) with an IC50 of 3.58 μM and can be used in stuides about the treatment of renal cancer.

SPOP-IN-6lc is a potent SPOP inhibitor with multiple roles in cancer, oncostatic in a variety of tumors, but functions as an oncogene in renal cancer.SPOP-IN-6lc can be used to study cell signaling and apoptosis.

NEO2734 (EP31670) is an orally active, selective inhibitor of p300/CBP and BET bromodomains, with an IC50 of less than 30 nM for both targets.

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).

SPOP-IN-6b hydrochloride is a highly effective inhibitor of speckle-type POZ protein (SPOP), with an IC50 value of 3.58 μM.

SPOP-IN-6b dihydrochloride, with an IC50 of 3.58 μM, is a potent inhibitor of spotted POZ protein (SPOP).

MS1262-C3-amide-C10-amine is an E3 Ligase Ligand-Linker conjugate. It includes a GLP ligand targeting the E3 ligase SPOP and a PROTAC linker. This compound can be utilized in designing PROTACs such as example [MS479].

MS479 is a BRD4 PROTAC degrader that binds with high affinity to BRD4-BD2 and GLP (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). It effectively reduces the protein levels of BRD4 short isoforms. By directly binding to its substrate GLP, MS479 recruits the E3 ligase SPOP as a bridging protein. Additionally, MS479 can be utilized to inhibit the proliferation of colorectal cancer 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.