Multiple Myeloma

Tocilizumab (Anti-Human IL6R, Humanized Antibody) is an anti-human interleukin-6 receptor (IL-6R) neutralizing antibody, prevents binding of IL-6 to the IL-6R, thereby inhibiting both classic and trans-signaling. Tocilizumab (Anti-Human IL6R, Humanized Antibody) can be used for the treatment of rheumatoid arthritis. Tocilizumab is remarkablely effective for the study of severe COVID-19 (coronavirus disease).

Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine inhibits the membrane aggregation of NINJ1 and prevents plasma membrane rupture during cell death. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis.

Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC₅₀ of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.

Rituximab (anti-CD20) is an anti-CD20 chimeric monoclonal antibody used to treat certain autoimmune diseases and types of cancer.

Belantamab (GSK2857916) is a humanized IgG1 anti-BCMA/TNFRSF17 monoclonal antibody. Belantamab is linked to MMAF (HY-15579) through a non-cleavable ADC linker to synthesize the antibody-active molecule conjugate (ADC) Belantamab mafodotin (HY-P3239). After binding to BCMA on the surface of tumor cells, Belantamab mafodotin enters the cell through receptor-mediated endocytosis. After entering the cell, Belantamab mafodotin releases MMAF, blocks cell division by inhibiting tubulin polymerization, arrests the cell cycle and induces cell apoptosis. Belantamab can be used for the study of multiple myeloma, especially relapsed/refractory multiple myeloma.

SB-405483 is a CRBN orthosteric ligand bindign enhancer. SB-405483 potentiates degradation of CRBN substrates including CK1α, Wee1, IKZF1/3. SB-405483 stabilizes CRBN and reduces CRBN autoubiquitination. SB-405483 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia.

ZNL-02-096 is a selective Wee1 PROTAC degrader. ZNL-02-096 binds to CRBN and Wee1 to form a ternary complex, inducing CRBN- and proteasome-dependent ubiquitination and proteasomal degradation of Wee1. ZNL-02-096 inhibits recombinant PLK1 with an IC₅₀ of 102 nM, but does not induce its degradation in cells. ZNL-02-096 induces G₂/M phase arrest, Apoptosis, transient integrated stress response, upregulation of ATF4, and phosphorylation of GCN2. ZNL-02-096 reduces Tyr15 phosphorylation of CDK1. ZNL-02-096 can be used in research related to ovarian cancer, acute lymphoblastic leukemia, triple-negative breast cancer, multiple myeloma, and pancreatic ductal adenocarcinoma.

dCBP-30 is an orally active, selective and dual-acting CBP/p300 PROTAC degrader with DC₅₀ values of 0.05 nM (CBP) and 0.04 nM (p300), respectively. dCBP-30 reduces the acetylation levels of histone substrates H3K27, H3K18, H2BK5 and H2BK20, downregulates multiple myeloma-specific dependency programs, and induces multiple myeloma cell apoptosis. dCBP-30 triggers tumor regression and prolongs survival in multiple myeloma xenograft mouse models, and exhibits synergistic antiproliferative activity with dexamethasone. dCBP-30 can be used for the research of multiple myeloma.

AU-24118 is an orally active PROTAC degrader that recruits cereblon to target the degradation of SMARCA2, SMARCA4 and PBRM1. AU-24118 impairs the chromatin accessibility of oncogenic transcription factors, inhibits colony formation, dislodges chromatin-bound transcription factors, attenuates downstream signal transduction, induces apoptosis, and exerts antiproliferative and cytotoxic effects. AU-24118 can be used in research related to castration-resistant prostate cancer, colorectal cancer, small cell lung cancer and multiple myeloma (including the t (4;14) subtype).

Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC₅₀ values ranging 0.460-2.17 nM and NSD2 SET domain IC₅₀ of 2.32 nM and K_d values ranging 6.3-70.4 nM.Gintemetostat reduces H₃K₃₆me₂ levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents.Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma.

Anti-Mouse IFN gamma Antibody (XMG1.2) is a kind of rat-derived IgG1 antibody inhibitor, targeting to IFN-γ. Anti-Mouse IFN gamma Antibody (XMG1.2) can neutralize IFN-γ. Anti-Mouse IFN gamma Antibody (XMG1.2) can be used for the researches of cancer, inflammation and immunology, such as multiple myeloma and chronic inflammation.

NP-OVAL (Ovalbumin) is a complex formed by 4-Hydroxy-3-nitrophenylacetyl (NP, a hapten) with Ovalbumin (OVAL, a carrier protein). NP-OVAL (Ovalbumin) can induce specific immune responses and NP-specific antibodies production. NP-OVAL (Ovalbumin) can accelerate the construction of multiple myeloma models.

Lisaftoclax is an orally active, selective BCL-2 inhibitor with a K_i of < 0.1 nM against human BCL-2. Lisaftoclax selectively binds to BCL-2, disrupts the BCL-2:BIM complex, and antagonizes the antiapoptotic function of BCL-2. Lisaftoclax induces BAX/BAK-dependent, caspase-mediated apoptosis, upregulates the pro-death proteins BIM and Noxa, and downregulates mitochondrial respiratory function and ATP production. Lisaftoclax can be used in the research of hematological malignancies including chronic lymphocytic leukemia, multiple myeloma, and diffuse large B-cell lymphoma.

Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition.

Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models.

Durvalumab (anti-PD-L1)(MEDI 4736) is a human anti-PD-L1 protein monoclonal antibody. Durvalumab (anti-PD-L1) completely blocks PD-L1 binding to PD-1 and CD80, IC ₅₀ are 0.1 and 0.04 nM respectively, has anti-tumor activity.

Clodronic acid (Clodronate) disodium salt is an orally active bisphosphonate. Clodronic acid disodium salt inhibits osteoclast-mediated bone resorption. Clodronic acid disodium salt reduces skeletal event risk in malignant bone disease, impairs malignant osteolysis, blocks bone matrix growth-factor release, induces apoptosis in osteoclasts and macrophages. Clodronic acid disodium salt is effective in the maintenance or improvement of bone mineral density. Clodronic acid disodium salt can be used for the research of multiple myeloma and postmenopausal osteoporosis.

Zigakibart (BION-1301) is an IgG4-kappa, humanized monoclonal antibody against TNFSF13 (tumor necrosis factor (TNF) superfamily member 13, APRIL, CD256). Zigakibart exhibits anti-inflammatory activity.

CRBN-6-5-5-VHL is a potent and selective VHL E3 ligand-based Cereblon (CRBN) PROTAC degrader with a DC₅₀ value of 1.5 nM. CRBN-6-5-5-VHL forms a heterotrimeric complex with CRBN and VHL E3 ligase, thereby promoting CRBN ubiquitination and proteasomal degradation without inducing VHL degradation. CRBN-6-5-5-VHL protects myeloma from the toxic effects of IMiDs. CRBN-6-5-5-VHL can be used in the research of multiple myeloma.

Glutarimide is a CRBN binder. Glutarimide exerts its function by binding to the thalidomide-binding domain of the CRBN protein. Glutarimide serves as an important structural component of many biologically active compounds. Glutarimide can be used in studies related to anemia, multiple myeloma and cycloheximide.