lymphoid

Phytohemagglutinin (PHA-M) is a lectin, isolated from the red kidney bean , induces apoptosis via increasing proapoptotic protein Bax and activating caspases-3. Anti-tumor activity

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

Mepazine (Pecazine) is a potent and selective inhibitor of MALT1, inhibiting GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 μM and 0.42 μM, respectively. Mepazine enhances apoptosis and impacts cell viability.

BLK degrader 1 is a selective B lymphoid tyrosine kinase (BLK) degrader with anticancer activity and can be used for cancer research.

Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.

2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor that covalently blocks the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)) with a Ki value of 43 μM and PTP1B with a Ki value of 42 μM [1]. SHP-1 and PTP1B both have known roles in regulating insulin signaling as well as myeloid and lymphoid cell differentiation, making inhibitors of these phosphatases of interest in diabetes, cancer, allergy, and inflammation research [2].

RO7567132 (FAP-LTBR) is a novel bispecific antibody that binds and agonizes LTBR bivalently while binds and antagonizes FAP monovalently, thereby limiting the activation of LTBR to the tumor microenvironment, inducing the formation of local tertiary lymphoid structures (TLS), and reducing systemic toxicity. Its mouse alternative can inhibit breast cancer growth, and the effect is better when combined with atezolizumab. In the mouse colorectal cancer model, it can also enhance immune cell infiltration and TLS-like structure formation.

1-beta-D-Arabinofuranosylthymine (Thymine 1-β-D-arabinofuranoside) is a purine nucleoside analog. Purine nucleoside analogs have a broad spectrum of antitumor activity, targeting inert lymphoid malignancies and inducing apoptosis.1-beta-D-Arabinofuranosylthymine's anticancer mechanism is dependent on the inhibition of DNA synthesis.1-beta-D-Arabinofuranosylthymine is a purine nucleoside analog.

LTV-1 has the potential for autoimmunity treatment. LTV-1 is a potent lymphoid tyrosine phosphatase (LYP) inhibitor in T cells with an IC50 of 508 nM.

FTY720 (S)-Phosphate is the active stereoisomeric phosphate derivative of FTY720 that acts as a potent modulator of sphingosine-1-phosphate (S1P) receptors. FTY720 (S)-Phosphate binds to S1P receptor subtypes S1P1, S1P3, S1P4, and S1P5 with Ki values of 2.1, 5.9, 23, and 2.2 nM respectively, causing receptor internalization on lymphocytes， preventing S1P-mediated lymphocyte egress from lymphoid tissues. FTY720 (S)-Phosphate also enhances endothelial barrier integrity, stimulates transporters such as Abcb1 and Abcc1, and inhibits cytosolic phospholipase A2 activity, highlighting its multifunctional pharmacological properties, making it an compound of interest in the research of diseases including multiple sclerosis, autoimmune diseases and cancer.

Pladienolide B is a potent spliceosome inhibitor, a macrolide isolated from Streptomyces obtusususus Mer-12, which targets the SF3B1 subunit of the spliceosome.Pladienolide B exerts its antitumor effects by inhibiting pre-mRNA splicing and inducing necrosis.Pladienolide B possesses antitumor activity and can be used to study leukemia and lymphoid tumors. Pladienolide B has antitumor activity and can be used to study leukemia and lymphoid tumors.

Safimaltib is an inhibitor of mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) and exhibits antitumor activity.

ASTX295 is a selective mouse double minute 2 (MDM2) antagonist with an IC50 value of less than 1 nM. It specifically inhibits the interaction between MDM2 and p53, reactivating wild-type (WT) TP53, which subsequently induces the expression of related transcriptional targets, leading to cell death and cell cycle arrest. ASTX295 holds potential for research in lymphoid malignancies such as diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), and T-cell lymphoma.

MALT1-IN-13 (compound 10m) is an inhibitor of the mucosa-associated lymphoid tissue lymphoma translocation protein (MALT1), forming a covalent and irreversible bond with the MALT1 protease, thereby inhibiting its activity with an IC50 of 1.7 μM. It suppresses the proliferation of ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1 cells. Additionally, MALT1-IN-13 regulates the mTOR and PI3K-Akt pathways.

Lenalidomide hydrochloride (CC-5013 hydrochloride), a Thalidomide derivative, functions as molecular glue and serves as an orally active immunomodulator. As a ligand for the ubiquitin E3 ligase cereblon (CRBN), it facilitates the selective ubiquitination and degradation of the lymphoid transcription factors IKZF1 and IKZF3 through the CRBN-CRL4 ubiquitin ligase. Specifically, Lenalidomide hydrochloride inhibits the growth of mature B-cell lymphomas, including multiple myeloma, and promotes IL-2 release from T cells [1] [2].

Lenalidomide hemihydrate is a derivative of Thalidomide, an orally active immunomodulator that acts as a molecular gel. It is a ligand for the ubiquitin E3 ligase cereblon, which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase.

MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor.

8-Deazafolic acid is a potent folate-dependent bacteria inhibitor, Streptococcus faecium (ATCC 8043) and Lactobacillus casei (ATCC 7469), and to have activity against lymphoid leukemia L1210 in mice.

CCT036477 is a selective inhibitor of wingless-type MMTV integration site family dependent transcription. CCT036477reduces the transcriptional activity of the T-cell factor and lymphoid enhancer factor transcription factor family at the ß-catenin level.

ND-2110, a selective interleukin-1 receptor-associated kinase 4 inhibitors, is used for the treatment of autoimmune disorders and lymphoid malignancy.

Yadanzioside E is a natural product that inhibits HIV viral replication in the H9 T lymphoid cell line, and is widely used in biochemical experiments and drug synthesis research.

JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric inhibitor of MALT1 protease . JNJ-67856633 lead to tumor stasis in some cases.

Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).

Azido-FTY720 (azido-Fingolimod) is an analogue of FTY720 featuring an azido group suitable for click chemistry reactions. FTY720 is an orally available S1P analogue and S1P1R modulator capable of crossing the blood-brain barrier (BBB), reducing neuroinflammation, and is indicated for multiple sclerosis (MS).