Diffuse Large B-cell Lymphoma

Auristatin S is a potent Auristatin payload. Auristatin S binds to the vinca-binding site on tubulin, thereby inhibiting microtubule assembly and inducing cell cycle arrest and apoptosis. Auristatin S acts as a cytotoxic component of antibody-drug conjugates (ADCs) and exerts target-specific cytotoxicity against cancer cells. Auristatin S can be used in the research of lymphoma, anaplastic large cell lymphoma and Hodgkin lymphoma.

FDU73 is a potent and selective BTK PROTAC degrader with a DC₅₀ value of 2.9 nM (JeKo-1). FDU73 degrades BTK via the ubiquitin-proteasome system. FDU73 exerts antiproliferative effects on cancer cells. FDU73 can be used for the research of B-cell malignancies.

PROTAC TBL1X degrader-1 is a TBL1X PROTAC degrader. PROTAC TBL1X degrader-1 induces TBL1X degradation via the Cereblon-mediated proteasomal pathway. PROTAC TBL1X degrader-1 exerts cytotoxic effects on cancer cells. PROTAC TBL1X degrader-1 can be used in studies related to diffuse large B-cell lymphoma.

PROTAC IRAK4 degrader-12 is an orally active IRAK4 PROTAC degrader with a DC₅₀ of 4.87 nM in K562 IRAK4-HiBiT cells. PROTAC IRAK4 degrader-12 induces protein degradation of IRAK4, IKZF1 and IKZF3. It inhibits the proliferation of diffuse large B-cell lymphoma cells. It suppresses tumor growth in mouse xenograft models of lymphoma cells. PROTAC IRAK4 degrader-12 can be used for the research of B-cell lymphoma and diffuse large B-cell lymphoma.

PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC₅₀ of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma.

PROTAC BRD4 Degrader-23 is a visible light-regulated BRD4 PROTAC degrader, with DC₅₀ values of 6871 nM and < 30 nM in the dark and under light exposure, respectively; its IC₅₀ values are 1172 nM and 140 nM under the corresponding conditions. PROTAC BRD4 Degrader-23 shows inhibited activity in dark environments, and recovers BRD4 degradation ability upon irradiation with 405 nm visible light. PROTAC BRD4 Degrader-23 inhibits tumor cell proliferation in a visible light-dependent manner. PROTAC BRD4 Degrader-23 can be used in studies of BRD4-dependent B-cell lymphoma.

PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC₅₀ value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC₅₀ of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma.

PROTAC BRD4 Degrader-20 (Compound 195) is a PROTAC degrader that targets BRD4 for degradation by recruiting VHL. PROTAC BRD4 Degrader-20 is applicable to the research of diffuse large B-cell lymphoma.

S-Geranylgeranyl-L-glutathione is a P2RY8 inhibitor and intercellular signaling molecule that exists endogenously in human bone marrow interstitial fluid. S-Geranylgeranyl-L-glutathione promotes the internalization of P2RY8 and antagonizes chemokine-induced activation of pAkt. S-Geranylgeranyl-L-glutathione negatively regulates the migration of B cells and T cells to the bone marrow, inhibits chemokine-mediated migration of germinal center B cells and follicular helper T cells, participates in lymphocyte guidance regulation, and modulates the germinal center response process. S-Geranylgeranyl-L-glutathione can be used in research related to diffuse large B-cell lymphoma and Burkitt lymphoma.

HH2853 is an orally active EZH1/EZH2 inhibitor, with an IC₅₀ of 9.26 nM for EZH1 and IC₅₀ values ranging from 2.21 to 3.75 nM for both wild-type and mutant EZH2. HH2853 simultaneously inhibits the methyltransferase activities of EZH1 and EZH2, blocks the compensatory pathway that arises following EZH2 inhibition, and reduces H3K27me3 levels. HH2853 upregulates the expression of c-Myc and TfR-1 to induce intracellular iron accumulation, and stabilizes GPX4 via HSPA5 to suppress ferroptosis. HH2853 combined with Erastin (HY-15763) synergistically inhibits EZH2 wild-type DLBCL cell proliferation. HH2853 alone shows weak activity against EZH2 wild-type DLBCL and is well tolerated. HH2853 is applicable for research related to diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, epithelioid sarcoma, and follicular lymphoma.

JH-I-25 is an orally active IRAK1 and IRAK4 inhibitor. JH-I-25 inhibits LPS-induced IRAK4 phosphorylation, IRAK1 degradation, MAPK activation, and the expression of proinflammatory cytokines TNF-α and IL-6 in lung tissues. JH-I-25 improves the survival rate of LPS-induced septic mice and serves as an IRAK4 recruiter in the design of proteolysis-targeting chimeric molecules. JH-I-25 can be used in research related to diffuse large B-cell lymphoma, Waldenström's macroglobulinemia, septic shock, rheumatoid arthritis, atherosclerosis, Alzheimer's disease, acute lung injury, sepsis, and psoriasis.

Lenalidomide-d₄ (CC-5013-d₄) is the d₄-labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8⁺ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.

Cobomarsen scrambled control is the negative control form of Cobomarsen (HY-132601), with the sequence: ACAUCAUAGUGACU. The modification method is the same as that of Cobomarsen. Cobomarsen sodium is an oligonucleotide inhibitor of miR-155 and can be used in the research of B-cell lymphoma.

(R,R)-Birelentinib ((R,R)-DZD8586) (Compound 14) is a potent BTK inhibitor with IC₅₀ values for BTK WT and BTK C481S of 0.7 and 0.86 nM, respectively. (R,R)-Birelentinib inhibits the self-phosphorylation of BTK and its IC₅₀ is 24.3 nM. (R,R)-Birelentinib exhibits significant anti-proliferative activity against wild-type and C481S mutant HEK293 cells. (R,R)-Birelentinib can be used for the study of drug-resistant B-cell malignancies.

Anti-CD19 Antibody (FMC63) is an antibody that binds to CD19, with a human K_d value ranging from 0.42 nM to 149 nM. Anti-CD19 Antibody (FMC63) mediates tumor cell killing, cytokine secretion, stable CAR expression, T cell activation and memory differentiation. Anti-CD19 Antibody (FMC63) fails to eliminate lymphoma cells carrying CD19 point mutations or co-expressing FMC63-CAR19, induces higher levels of activation-induced cell death, and reduces cell persistence. Anti-CD19 Antibody (FMC63) can be used in research related to B-cell non-Hodgkin's lymphoma, B-cell acute lymphoblastic leukemia, relapsed or refractory diffuse large B-cell lymphoma, etc.