Cancer Immunotherapy

PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC₅₀=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability.

PD-1/PD-L1-IN-22 (Example 2) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-22 blocks PD-1/PD-L1 with the IC₅₀ of 0.732 μM. PD-1/PD-L1-IN-22 can be used for the research of cancers, infectious diseases and autoimmune diseases.

P53 Activator 16 (Compound JC16) is a p53 activator. P53 Activator 16 exhibits selective cytotoxicity and pro-apoptotic (apoptosis) activity towards p53-Y220C mutant cancer cells, while having little effect on wild-type or P53-deficient cells. P53 Activator 16 induces the conformational transition of cell p53-Y220C from the mutant form to the wild-type form, accompanied by the transcriptional activation of p53 target genes, without increasing the overall level of p53 protein. P53 Activator 16 can be used for the study of p53 mutant cancers.

SR8185 is a potent and selective TBK1/IKKi dual inhibitor with IC₅₀s of 3 nM and < 10 nM against IKKi and TBK1, respectively. SR8185 exhibits potent and broad spectrum antiproliferative effects on human cancer cells. SR8185 can be used for cancer research.

Sintilimab (Anti-PD-1) (IBI308 (Anti-PD-1)) is a safe and effectivel humanized IgG4 monoclonal antibody that binds to PD-1 with a K_D value of 74 pM. Sintilimab (Anti-PD-1) blocks the interaction of PD-1 with its ligands (PD-L1 and PL-L2), consequently helping to restore the endogenous antitumour T-cell response. Sintilimab (Anti-PD-1) combined with prebiotics inhibits tumor volume and regulates immune cell subpopulation balance in lung adenocarcinoma mice. Sintilimab (Anti-PD-1) can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer.

S095024 is a humanized IgG1 monoclonal antibody inhibitor targeting CD73. S095024 can be used to study acute respiratory distress syndrome (ARDS), non-small cell lung cancer (NSCLC) and advanced solid tumor malignancies.

NH4-6 is a SIRT2 inhibitor with an IC₅₀ of 0.032 μM against SIRT2 and an IC₅₀ of 3 μM against SIRT1. NH4-6 inhibits the deacetylase activity of SIRT1. As a cytotoxic agent, NH4-6 reduces cancer cell viability, suppresses anchorage-independent growth of cancer cells, induces acetylation of α-tubulin, and promotes acetylation of p53. NH4-6 can be used in the research of breast cancer.

Saikosaponin D (Standard) is the analytical standard of Saikosaponin D. This product is intended for research and analytical applications. Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.

PD-L1/HDAC6-IN-1 is an orally active dual inhibitor of PD-L1 and HDAC6, with IC₅₀ values of 26.8 nM and 78 nM, respectively. PD-L1/HDAC6-IN-1 binds to human and murine PD-L1 proteins with high affinity, while it reduces STAT3 phosphorylation and downregulates PD-L1 expression by inhibiting HDAC6, thus blocking the PD-1/PD-L1 interaction. PD-L1/HDAC6-IN-1 exhibits potent anti-tumor activity in a mouse melanoma model. PD-L1/HDAC6-IN-1 is suitable for research on tumor immune regulation related to melanoma.

SBT-100 (His Tag) is a human monoclonal antibody (mAb) targeting STAT3. SBT-100 (His Tag) inhibits IL-6-mediated P-STAT3 nuclear translocation in HEp-2 and PANC-1 cells. SBT-100 (His Tag) has tumor growth inhibitory effects on MDA-MB-231.

HBM1007 is a fully human monoclonal antibody targeting CD73. HBM1007 is an extracellular enzyme expressed on the surface of stromal cells and tumor cells, capable of converting extracellular adenosine monophosphate (AMP) into adenosine, and recognizing CD73 via a unique antigenic epitope. HBM1007 inhibits both CD73-dependent and CD73-independent enzyme activities.

PROTAC Cbl-b-IN-1 (compound 64) is a potent Cbl-b PROTAC degrader with a DC₅₀ of less than 30 nM. PROTAC Cbl-b-IN-1 can be used for cancer research.

Duocarmycin A is an antitumor antibiotic and DNA alkylating agent with broad-spectrum antibacterial activity, which can serve as a payload for synthesizing antibody-drug conjugates (ADCs). Duocarmycin A selectively binds to the AT-rich minor groove of DNA, forms covalent adducts by alkylating the adenine N3 residue, thereby disrupting DNA structure and inhibiting its replication and transcription. Duocarmycin A induces apoptosis, sub-G1 phase accumulation and chromatin condensation, reduces the levels of pro-caspase-3/9, and induces p53-independent p21 expression. Duocarmycin A is widely used in the research of various malignancies, including leukemia, sarcoma, glioblastoma, as well as multiple solid tumor models such as lung cancer, breast cancer, and colorectal cancer.

Methyl aminolevulinate is a sensitizer used in photodynamic therapy (PDT). Methyl aminolevulinate penetrates the skin and induces the production of photoactive porphyrins including protoporphyrin IX in cells; upon exposure to appropriate light, it generates ROS, which triggers cellular oxidation and cell death. Methyl aminolevulinate acts as a photo-damage reversing agent through epidermal reconstruction, cytokine-mediated activation of dermal fibroblasts, elastin breakdown, new collagen formation, and compression of dilated capillaries. Methyl aminolevulinate reduces the expression of the proliferation marker K_i-67 and the early skin carcinogenesis marker TP53. Methyl aminolevulinate delays the onset of ultraviolet-induced skin tumors and reduces tumor burden in hairless mice. Methyl aminolevulinate is applicable to research related to actinic keratosis and basal cell carcinoma.

Plaunotol is an orally active acyclic diterpene alcohol. Plaunotol has antibacterial activity against Helicobacter pylori which causes peptic ulcer . Plaunotol inhibits tumor angiogenesis and cell proliferation. Plaunotol induces apoptosis by activation of caspase 8 and caspase 9 pathways. Plaunotol is a potential anticancer agent against colon cancer .

Antitumor agent-49 (Compound 10) is a Harmine derivative-furoxan hybrids containing NO donor, with antitumor activities. Antitumor agent-49 shows cytotoxic activity against HepG2 cells with an IC₅₀ of 1.79 µM. Antitumor agent-49 produces high levels of NO in vitro.

Imaprelimab (powder) is a humanized IgG1κ anti-CD146 antibody. Imaprelimab (powder) exerts anti-angiogenic effects on brain metastasis of lung cancer in animal models. Imaprelimab (powder) can be used in studies related to brain metastasis of non-small cell lung cancer.

BSO-07 is a ROS/JNK activator with significant anticancer effects, having an IC₅₀ value of 24.81 μM against human breast cancer (BC) cells. BSO-07 induces apoptosis (Apoptosis) and paraptosis by activating JNK and increasing ROS levels, including enhancing the expression of apoptosis-associated proteins such as PARP, Bax, phosphorylated p53, ATF4, and CHOP, while decreasing the levels of anti-apoptotic proteins like Bcl-2, Bcl-xL, and Survivin. BSO-07 holds promise for research in the field of breast cancer.

LUF8100 is a dual-target antagonist of CCR2/CCR5 with pK_i values for CCR2 and CCR5 of 5.23 and 4.97 respectively. LUF8100 can be used for research on immune homeostasis and cancer.

Trastuzumab-DM12 (T-DM21) is an antibody-drug conjugate (ADC). Trastuzumab-DM12 binds to HER2, inhibits HER2 shedding, and mediates antibody-dependent cellular cytotoxicity. Trastuzumab-DM12 is formed by conjugating the antibody Trastuzumab (HY-P9907) with DM-21 (HY-139441). Trastuzumab-DM12 can be used for cancer research.