BI8626 is a novel, potent and specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM. Deregulated expression of MYC is a driver of colorectal carcinogenesis, necessitating novel strategies to inhibit MYC function. The ubiquitin ligase HUWE1 (HECTH9, ARF-BP1, MULE) associates with both MYC and the MYC-associated protein MIZ1.

Pomiferin (formerly known as NSC 5113) is a naturally occuring flavonoid isolated from the fruits of Maclura pomifera, which acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).

PROTAC ABL binding moiety 2 is the GNF5 (an ABL inhibitor) moiety that binds to IAP (inhibitor of apoptosis protein) ligand via a linker to form SNIPER. Chromosomal translocation occurs in some cancer cells, which results in the expression of aberrant oncogenic fusion proteins that include BCR-ABL in chronic myelogenous leukemia (CML). Inhibitors of ABL […]

KRas G12C inhibitor 4 is a novel and potent inhibitor of KRAS. The compound inhibits KRAS G12C which is a well-validated driver mutation present in approximately 14% of NSCLC adenocarcinoma patients and 5% of CRC patients. Patients with KRAS mutation-positives cancers generally have a poor prognosis and resistant to standard therapies.

K-Ras G12C-IN-3 is a novel, potent and irreversible/covalent inhibitor of K-Ras protein with G12C mutation. The compound inhibits KRAS G12C which is a well-validated driver mutation present in approximately 14% of NSCLC adenocarcinoma patients and 5% of CRC patients. Patients with KRAS mutation-positives cancers generally have a poor prognosis and resistant to standard therapies.

K-Ras G12C-IN-2 is a novel, potent and irreversible/covalent inhibitor of K-Ras protein with G12C mutation. The compound inhibits KRAS G12C which is a well-validated driver mutation present in approximately 14% of NSCLC adenocarcinoma patients and 5% of CRC patients. Patients with KRAS mutation-positives cancers generally have a poor prognosis and resistant to standard therapies.

NED3238 is a novel, highly potent and selective inhibitor of human arginase I and II with IC50 values of 1.3 and 8.1 nM, respectively.

TAK-778, a derivative of ipriflavone, has been shown to induce bone growth both in vitro and in vivo. Recently, it has been shown that TAK-778 can enhance osteoblast differentiation of human bone marrow cells via an estrogen receptor (ER)-dependent pathway. TAK-778 enhanced bone formation in OVX rats and that this effect was dependent on an […]

LY 254155 is a potent antifolate compound which inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.

CHMFL-BTK-01 (compound 9) is a novel, potent, highly selective and irreversible/covalent BTK (Bruton’s tyrosine kinase) inhibitor with an IC50 of 7 nM. It potently inhibited the auto-phosphorylation of BTK Y223 auto-phosphorylation.