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 %...
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...
Mitonafide is a Cytostatic Agent, Inhibiting DNA and RNA Synthesis
Cytostatic agents are cell components or drugs that inhibit cell division. Specifically, cell growth arrest is an important prerequisite for structured multicellular organisms. Cell inhibitors achieve these growth-inhibitory effects through specific mechanisms of action. Some cell inhibitors are not only used in cancer treatment, but also for other diseases...
Mogamulizumab is a Defucosylated Anti-CCR4 Monoclonal Antibody
C-C Motif Chemokine Receptor 4 (CCR4) is a G-coupled-protein receptor for C-C chemokines. It’s on surface of tumor cells in leukemia and lymphoma patients. For example, adult T-cell leukemia-lymphoma (ATLL), peripheral T-cell lymphoma (PTCL) and cutaneous T-cell lymphoma (CTCL) all expresses CCR-4. Furthermore, leukemia and lymphoma are clinically and...
Spiruchostatin A is a Potent HDAC Inhibitor with anticancer activity
Histone deacetylase (HDAC) is an enzyme that catalyzes the removal of acetyl functional groups from the lysine residues of histones and non-histones. Among other things, histone lysine acetylation is highly reversible. HDAC-catalyzed epigenetic modification of histone acetylation regulates chromatin structure and transcription, while non-histone deacetylation controls a variety of...
Purinostat mesylate is a Selective HDAC Inhibitor With anti-Leukemia Effects
Purinostat mesylate is a selective inhibitor of HDAC. This compound inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate (1-10 μM) inhibits HDAC1, 2, 3, and 8. And the IC50s are 0.81, 1.4, 1.7, and 3.8 nM, respectively. It also inhibits HDAC6 and 10,...
Rebeccamycin, an Antitumor Antibiotic, Inhibits DNA Topoisomerase I
Rebeccamycin, a yellow crystalline product, is isolated from the mycelium. It has activity against P388 leukemia, L1210 leukemia, and B16 melanoma implanted in mice. Rebeccamycin is also an antitumor antibiotic produced by the actinomycete Saccharotrix aerocolonigenes with activity against several human tumor cell lines, including A549 (lung adenocarcinoma), HCT-116...