dBRD9 is a PROTAC and can Selective Degrades BRD9
BRD9 is a subunit of the human BAF (SWI/SNF) nucleosome remodeling complex. Besides, BRD9 contains a bromodomain and is closely related to BRD7. Importantly, The BRD9 gene is frequently present in variable copy numbers in lung cancer and has emerged as an attractive therapeutic target in cancer. Moreover, the...
YX-2-107, a PROTAC, is a Selective CDK6 Degrader
Ph+ALL (Philadelphia chromosome-positive acute lymphoblastic leukemia) is a rare subtype of leukemia characterized by the abnormal formation of the Philadelphia chromosome, which occurs when pieces of chromosomes 9 and 22 switch with each other. The incidence of Ph+ ALL increases with age, and occurs in up to 50 %...
SIAIS100 is a Potent BCR-ABL PROTAC Degrader
Chronic myeloid leukemia (CML) is a kind of myeloproliferative neoplasms (MPN). It is characterized by the proliferation of a pluripotential stem cell that can differentiate along the granulocytic lineage. In terms of mechanism, it is consistently related to the BCR-ABL1 fusion gene. CML is typically relevant to a balanced...
SJ988497, a PROTAC JAK2 Degrader, used for Acute Lymphoblastic Leukemia Research
CRLF2-rearranged (CRLF2r) acute lymphoblastic leukemia (ALL) is relevant with a poor outcome in children and adults. CRLF2r-ALL accounts for more than half of Philadelphia chromosome-like (Ph-like) ALL. Noticeably, the overexpression of CRLF2 activates JAK-STAT and parallel signaling pathways. However, small molecules inhibiting JAKs are variable and limited. Importantly, Using...
U7D-1 is a Selective USP7 PROTAC Degrader For Leukemia Research
Ubiquitin-specific proteinase 7 (USP7) is a kind of de ubiquitination enzyme (DUB), which can remove ubiquitin and protect substrate protein from degradation. Besides, the full activity of USP7 requires the C-terminal Ub-like domain to fold back to the catalytic domain. Moreover, this allows the active site to be remodeled...
ARV-471 is an Estrogen Receptor PROTAC Degrader for Breast Cancer
PROTAC is a heterobifunctional molecule containing two small molecule binding moieties. Specifically, PROTACs in cells seek and selectively bind to target proteins. PROTAC then recruits specific E3 ligases to the target protein. Besides, it forms a ternary complex in close proximity to the target protein and E3 ligase. In...
MS159 is a First-In-class NSD2 PROTAC degrader for Multiple Myeloma Research
Proteolytic targeting chimera (PROTAC) is a heterobifunctional small molecule, including two active domains, and a linker. Importantly, it can remove specific unwanted proteins. PROTAC is a technology based on the ligand binding of TAP and then the degradation of TAP. PROTAC provides an alternative approach to those so-called non-druggable...