WH244 is a second-generation PROTAC that selectively degrades the anti-apoptotic proteins BCL-xL and BCL-2 with a DC50 of 0.6 nM for BCL-xL and 7.4 nM for BCL-2.

SPA-10091-HCl is a degrader of DOT1L that selectively degrades DOT1L protein through the nuclear ubiquitin-proteasome pathway, thereby suppressing H3K79 methylation in CRPC cells. It also inhibits DOT1L enzymatic activity with an IC50 of 0.87 μM, induces apoptosis, and significantly reduces tumor growth in vivo.

GDC-2992 (RO7656594, Compound 28A) is an orally active degrader of androgen receptor (AR) with a DC50 of 2.7 nM. It binds to AR and cereblon (CRBN), inducing AR ubiquitination and degradation. GDC-2992 also inhibits cell proliferation in VCaP cells and exhibits potential to reduce treatment resistance and disease relapse in prostate cancer.

Golidocitinib 1-hydroxy-2-naphthoate is a derivative of Golidocitinib, an oral, potent, selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 70 nM. It exhibits enhnaced antitumor activity and can be used for the treatment of cancer, including peripheral T cell lymphoma (PTCL).

Golidocitinib 1-hydroxy-2-naphthoate is a derivative of Golidocitinib, an oral, potent, selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 70 nM. It exhibits enhnaced antitumor activity and can be used for the treatment of cancer, including peripheral T cell lymphoma (PTCL).

Golidocitinib 1-hydroxy-2-naphthoate is a derivative of Golidocitinib, an oral, potent, selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 70 nM. It exhibits enhnaced antitumor activity and can be used for the treatment of cancer, including peripheral T cell lymphoma (PTCL).

Z57346765 hydrochloride is an inhibitor of phosphoglycerate kinase 1 (PGK1) that binds to the ADP-binding pocket with a KD value of 2.09 × 10⁻⁵ M, reducing PGK1 metabolic enzyme activity, glucose consumption, and lactate production. It also inhibits DNA replication, impairs DNA damage repair, and induces cell cycle arrest in kidney renal clear cell carcinoma (KIRC) […]

Z57346765 hydrochloride is an inhibitor of phosphoglycerate kinase 1 (PGK1) that binds to the ADP-binding pocket with a KD value of 2.09 × 10⁻⁵ M, reducing PGK1 metabolic enzyme activity, glucose consumption, and lactate production. It also inhibits DNA replication, impairs DNA damage repair, and induces cell cycle arrest in kidney renal clear cell carcinoma (KIRC) […]

Golidocitinib 1-hydroxy-2-naphthoate is a derivative of Golidocitinib, an oral, potent, selective inhibitor of Janus kinase 1 (JAK1) with an IC50 of 70 nM. It exhibits enhnaced antitumor activity and can be used for the treatment of cancer, including peripheral T cell lymphoma (PTCL).

Z57346765 hydrochloride is an inhibitor of phosphoglycerate kinase 1 (PGK1) that binds to the ADP-binding pocket with a KD value of 2.09 × 10⁻⁵ M, reducing PGK1 metabolic enzyme activity, glucose consumption, and lactate production. It also inhibits DNA replication, impairs DNA damage repair, and induces cell cycle arrest in kidney renal clear cell carcinoma (KIRC) […]