CD38 Inhibitor

Kuromanin chloride (Chrysontemin) is derived from mulberry leaves and has the effect of increasing blood sugar concentration and maintaining lipid metabolism balance to reduce obesity. Kuromanin chloride can inhibit CD38 enzymatic activities.

Isatuximab is a monoclonal antibody targeting the transmembrane receptor and ectoenzyme CD38, a protein highly expressed on hematological malignant cells, including those in multiple myeloma (MM). Isatuximab has antitumor activity via multiple biological mechanisms, including antibody-dependent cellular-mediated cytotoxicity, complement-dependent cytotoxicity, antibody-dependent cellular phagocytosis, and direct induction of apoptosis without crosslinking. Isatuximab also directly inhibits CD38 ectoenzyme activity, which is implicated in many cellular functions.

CD38-IN-6 is an orally active CD38 inhibitor. CD38-IN-6 regulates NAD⁺ metabolite levels in the liver of aged obese mice by increasing NAD⁺ and NMN levels, and decreasing NAM and ADPR levels. CD38-IN-6 alleviates inflammatory responses in mice. CD38-IN-6 can be used for research related to obesity and inflammation.

A-8531 is an orally active CD38 inhibitor with IC₅₀ values of 1.10 nM against human CD38, IC₅₀ values of 2.93 nM against mouse CD38, and a human K_a of 0.32 nM. A-8531 exerts its inhibitory activity via its 4-pyridine reactive warhead interacting with the CD38 substrate NAD⁺, and binds stably to CD38 only in the presence of NAD⁺, with a binding K_D of 0.32 nM as detected by SPR. A-8531 dose-dependently increases NAD⁺ levels in mouse skin, lung and liver tissues, while simultaneously reducing the contents of NAM and ADPR in these tissues. A-8531 derivative A-3190 (HY-184206) has blood-brain barrier penetration. A-8531 can be used in studies related to neurodegenerative diseases.

FTL004 is an anti-CD38 monoclonal antibody. FTL004 exhibits enhanced Proapoptotic activity and displays stronger ADCC against CD38⁺ malignant cells. FTL004 can be used for the research of multiple myeloma and non-Hodgkin lymphoma[1].

MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC₅₀ values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD⁺ (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart.

Felzartamab (MOR-202) is a human monoclonal antibody that targets CD38 and can be used in multiple myeloma research.

Anti-Mouse CD38 Antibody (NIMR5) is an anti-mouse CD38 IgG2a monoclonal antibody. Anti-Mouse CD38 Antibody (NIMR5) can activate the ERK signaling pathway and promote cell apoptosis. Anti-Mouse CD38 Antibody (NIMR5) can restore T cell function. Anti-Mouse CD38 Antibody (NIMR5) upregulates the expression of CD1d protein and enhances spleen cell proliferation, dendritic cell (DC) and natural killer T cell (NKT) expansion. Anti-Mouse CD38 Antibody (NIMR5) can be used for researches on cancer and immunology such as melanoma and colon cancer.

Mezagitamab (TAK-079) is a IgG1λ anti-CD38 monoclonal antibody. Mezagitamab depletes tumor cells expressing CD38 through antibody and complement dependent cytotoxicity. Mezagitamab has potential application in relapsed/refractory multiple myeloma (RRMM) and idiopathic thrombocytopenic purpura (ITP).

Luteolinidin chloride is a deoxyanthocyanidin isolated from the plant Sorghum bicolor with antioxidant activity. Luteolinidin chloride is a potent CD38 inhibitor (K_i=11.4 μM) and protects the heart from ischemia/reperfusion injury by preserving endothelial nitric oxide synthase (eNOS) function and preventing endothelial dysfunction. Luteolinidin chloride is also a competitive inhibitor of tyrosinase (IC₅₀=3.7 μM) and blocks the production of melanin.

Ara-F-NAD+ sodium is an arabino analogue of NAD⁺. Ara-F-NAD+ sodium is a potent, reversible and slow-binding CD38 NADase inhibitor.

ISB2001 is a trispecific antibody targeting CD38, CD3 and BCMA. ISB2001 effectively counteracts tumor immune escape mechanisms caused by antigen downregulation, antigen loss, soluble factor competition and other factors. ISB2001 is applicable to relevant research on multiple myeloma and relapsed/refractory multiple myeloma.

Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice.

Erzotabart is an IgG1-kappa, anti-CD38 (ADP-ribosyl cyclase 1, cyclic ADP-ribose hydrolase 1, cADPr hydrolase 1, cADPR1) Homo sapiens monoclonal antibody. Erzotabart shows antineoplastic activity.

AMG-424 (XmAb968) is a human bispecific antibody (bsAb) targeting CD38 & CD3E. AMG-424 kills CD38-expressing cancer cells, triggers T-cell proliferation and attenuates cytokine release. AMG 424 has antitumor activity in a bone marrow-invasive mouse cancer model and induces peripheral B-cell depletion in cynomolgus monkeys. AMG-424 can be used in multiple myeloma research. Recommended isotype control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3.

Lumrotatug is an anti-CD38 human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

Sanritatug (SG-301) is an anti-CD38 IgG1κ antibody with potential antineoplastic activity. The corresponding isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).

Ara-F-NAD+ is an arabino analogue of NAD⁺. Ara-F-NAD+ is a potent, reversible and slow-binding CD38 NADase inhibitor.

NOTA-MK0159 is a NOTA (HY-134418) and MK0159 (HY-150508) conjugate. NOTA-MK0159 inhibits human and mouse CD38 with IC₅₀ values of 72.58 and 7.55 nM. NOTA-MK0159 coupled with radioactive elements acts as a imaging agent with specific uptake in CD38-positive multiple myeloma cells, enabling noninvasive whole-body assessment of CD38 expression in multiple myeloma xenografts. NOTA-MK0159 can be used for the research of multiple myeloma.

CVN14 is a potent, selective and brain-penetrant CD38 inhibitor with human IC₅₀ 19 nM, mouse IC₅₀ 2.4 nM. CVN14 binds uncompetitively to form a complex with CD38 and ADPR, and inhibits CD38 enzymatic activity. CVN14 can be used for the research of neurodegenerative diseases.