lymphocytic

Cladribine (2CdA), an adenosine deaminase inhibitor, is utilized in the treatment of lymphoproliferative diseases.

Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

MP07-66 is a novel FTY720-analog devoid of immunosuppressive effects leads to the reactivation of PP2A, which in turn triggers apoptosis of CLL cells.

Orelabrutinib (ICP-022) is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).

Umbralisib (TGR 1202) is a PI3Kδ inhibitor.

Ofatumumab is a humanized monoclonal antibody targeting CD20. Ofatumumab acts on CD20-expressing B lymphocytes, inducing antibody-dependent cell-mediated cytotoxicity and complement-dependent cytotoxicity.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

GS-9901 is a selective, orally active and potent PI3Kδ inhibitor (IC50: 1 nM) for the study of non-Hodgkin's lymphoma and chronic lymphocytic leukemia.

Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM. Bcl-xL antagonist 2 induces apoptosis in cancer cells and can be used in studies about chronic lymphocytic leukemia and non-Hodgkin's lymphoma.

Ethacrynic acid (Edecrin) is a nonsulfonamide loop diuretic that inhibits the activity of the Na+/K+/2Cl- cotransporter NKCC2 in the thick ascending limb of the loop of Henle. It also inhibits glutathione S-transferase and Wnt signalling, producing cytotoxicity in chronic lymphocytic leukaemia cells and other tumour cells.

Lisaftoclax (Bcl-2/Bcl-xl inhibitor 1) is an oral dual inhibitor of Bcl-2 and Bcl-xl, with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively. Lisaftoclax is used to treat chronic lymphocytic leukemia (CLL) by inhibiting the action of the BCL-2 protein, which promotes the death of leukemia cells.

MT-802 is an effective BTK degrader based on PROTAC technology (DC50: 1 nM). MT-802 has the potential to treat C481S mutant chronic lymphocytic leukemia (CLL).

8-Chloroadenosine (NSC-354258) is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine (NSC-354258) is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2/M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine (NSC-354258) has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

PROTAC BTK Degrader-10 (Example 1P) is a PROTAC compound that targets BTK for degradation. It is applicable in the research of chronic lymphocytic leukemia (CLL). [Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon].

Lonitoclax is an inhibitor of B-cell lymphoma 2 (Bcl-2). It demonstrates antitumor activity in B-cell and myeloid malignancy models comparable to Venetoclax. Lonitoclax holds potential for research in relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas.

TLT8 is a ByeTAC protein degrader that targets BTK. It induces BTK degradation by non-covalently binding to Rpn-13 and BTK. TLT8 is applicable in research on chronic lymphocytic leukemia.

VV261 is an orally active inhibitor of the Influenza Virus. It exhibits activity against the Severe Fever with Thrombocytopenia Syndrome Virus (SFTSV) and the Lymphocytic Choriomeningitis Virus (LCMV), with EC50 values of 0.89 and 0.15, respectively.

DDD2 is a selective and efficient VHL-mediated PROTAC degrader specifically targeting NUDT5. It effectively induces substantial degradation of NUDT5. DDD2 consists of the warhead TH10184 and the VHL-recruiting ligand VH032, connected via a saturated aliphatic eight-carbon linker. DDD2 is applicable in cancer research, including studies on lymphocytic leukemia and osteosarcoma.

CFON-026 is a selective, orally active, non-covalent BTK inhibitor with an IC50 of 0.27 nM. It demonstrates significant antitumor activity against wild-type BTK (TMD8 and REC-1) as well as all clinically relevant BTK resistance mutations (BTKC481S, T474I, L528W, and V416L). CFON-026 induces complete tumor regression in the TMD8 xenograft mouse model. This compound is applicable for research into hematologic cancers, such as chronic lymphocytic leukemia and Waldenström's macroglobulinemia.

JP-163-16 is a RelA/p65 PROTAC degrader. It selectively reduces the expression of RelA/p65 in cells via a proteasome-dependent mechanism. JP-163-16 induces apoptosis by inhibiting the NF-κB signaling pathway. This compound is applicable for research on RelA/p65-dependent tumors, such as chronic lymphocytic leukemia (CLL).

FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor, exhibiting an IC50 of 4.5 nM for the Bcl-2/BAK interaction. It effectively suppresses tumor growth in mouse models of follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenografts without causing significant weight loss. FCN-338 demonstrates broad-spectrum anticancer activity, making it suitable for treating FL, chronic lymphocytic leukemia (CLL)/small lymphocytic leukemia (SLL), AML, and ALL.

FGFR-IN-22 (Compound 23) is an FGFR inhibitor with IC50 values of 0.631 nM for FGFR1, 1.26 nM for FGFR2, 0.851 nM for FGFR3, and 1 nM for FGFR4. It effectively inhibits cell proliferation dependent on FGFR1 and FGFR3 signaling pathways. FGFR-IN-22 is applicable in research related to cancers such as chronic lymphocytic leukemia (CLL).

TAN 420E is a bacterial metabolite originally isolated from Streptomyces. It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 1.3 μM) and reduces thiobarbituric acid reactive substances (TBARS) in rat liver microsomes by 72% when used at a concentration of 100 μg/ml. TAN 420E is active against B. brevis, B. cereus, M. flavus, and S. aureus (MICs = 50-100 μg/ml). It is cytotoxic to P388 and KB lymphocytic leukemia cells (EC50s = 0.022 and 0.3 μg/ml, respectively).

A410099.1 is a BIRC (baculoviral IAP repeat-containing protein) inhibitor with EC50 values of 4.6, 9.2, 15.6, 19.9, and 93.9 nM for BIRC2/3/4/7/8 respectively, suitable for studying E3 ligases and PROTAC synthesis.