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Epigenetic Repression Enhances T Cell Function

Cancer Immunotherapy DNA Metabolism And Repair Cellular Stress Proteostasis

Epigenetic repression can enhance T-cell function when it selectively silences programs that enforce exhaustion or terminal differentiation. This qualification is essential: epigenetic repression is not inherently beneficial, because the same mechanisms can suppress cytokines, memory formation, or cytotoxic genes. Chronic antigen exposure creates an exhaustion-associated chromatin landscape that differs from ordinary activation and persists even when inhibitory signaling is removed. Foundational studies showed that exhausted T cells retain a distinct accessibility program, explaining why checkpoint blockade often reinvigorates function only partially. Current work uses chromatin profiling and CRISPR perturbation to identify regulators whose modification preserves persistence without eliminating the controls required for safe, antigen-dependent immunity The therapeutic idea is therefore to repress the repressors of useful immunity while leaving activation thresholds and lineage flexibility intact[1][2][3].

Repeated stimulation activates transcription factors and chromatin modifiers that stabilize inhibitory receptors, altered metabolism, reduced effector output, and limited self-renewal. DNA methylation and histone modifications can lock these states, while factors such as TOX and NR4A coordinate broad exhaustion programs. Genome-wide CRISPR screens extend this model by identifying chromatin-remodeling genes that limit persistence under sustained stimulation. Removing or attenuating a restrictive regulator can maintain accessibility at memory and effector loci, but the effect depends on timing and cellular state. An intervention applied during priming may change lineage commitment, whereas the same intervention in a terminally exhausted cell may not rebuild the lost regulatory architecture Progenitor exhausted cells remain more responsive to checkpoint therapy than terminal populations, linking chromatin state to clinical reversibility[1][2][3].

Therapeutic applications include ex vivo exposure to epigenetic drugs during cell manufacturing, targeted gene disruption, locus-specific epigenome editing, and combinations with PD-1 blockade. CAR-T and T-cell receptor therapies are particularly suitable because cells can be modified and tested before infusion. In cancer, DNA methyltransferase, histone deacetylase, or methyltransferase inhibitors may also alter tumor antigen presentation and the microenvironment, producing effects beyond the T cell. Broad systemic inhibitors can suppress hematopoiesis or activate unwanted genes, so improved cellular function cannot be assumed from a favorable change in one marker. Product testing must measure proliferation, repeated killing, cytokines, differentiation, genomic stability, and tumor control together Locus-specific approaches could avoid the broad transcriptional effects that make systemic epigenetic drugs difficult to interpret in immune therapy[1][3].

The research priority is precision rather than maximal chromatin disruption. Single-cell multi-omics can connect regulatory elements with functional states and distinguish reversible progenitor exhaustion from terminal dysfunction. Screens should be repeated across donors, antigens, costimulatory domains, and metabolic conditions before a target is treated as universal. Transient editing or programmable repressors may offer a safer alternative to permanent gene loss, and inducible circuits could restrict the intervention to manufacturing or tumor exposure. Long-term studies must assess clonal dominance, autoimmunity, and loss of activation control. Selective epigenetic repression can create more durable therapeutic T cells, but success requires preserving the flexible chromatin needed for memory while preventing the fixed program that follows chronic stimulation A functional endpoint should require serial antigen challenges, because a single short killing assay cannot establish resistance to exhaustion[1][2][3].

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Cat. No. Product Name Information Application Publication
HY-13030 (+)-JQ-1
(+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
Epigenetic Reader Domain   Autophagy   Ligands for Target Protein for PROTAC   SWI/SNF Complex  
Neurological, Eye or Ear Disease   Leukemia/Lymphoma/Myeloma  
306
HY-A0004 Decitabine
Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell Apoptosis. Decitabine has potent anticancer activity.
DNA Methyltransferase   Apoptosis   Nucleoside Antimetabolite/Analog  
Pancreatic Cancer   Viral Infection   Digestive System Inflammation   Urogenital Cancer   Non-Small Cell Lung Cancer   Acute Myeloid Leukemia   SARS-CoV-2 Infection   Rheumatoid Arthritis  
177
HY-10586 5-Azacytidine
5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
Organoid   Nucleoside Antimetabolite/Analog   DNA Methyltransferase   Bacterial   Autophagy   Antibiotic  
Lung Cancer   Prostate Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Bacterial Infection   SARS-CoV-2 Infection   Rheumatoid Arthritis  
139
HY-L251 Ionizable Lipid Compound Library
Ionizable lipids are a class of specialized, functional lipid molecules with pH-sensitive charge characteristics. They are primarily divided into two major categories: ionizable cationic lipids and ionizable anionic lipids, though the term typically specifies ionizable cationic lipids within the biomedical field. Structurally, these lipids consist of an ionizable hydrophilic headgroup, a biodegradable linker, and hydrophobic tails. Their primary application is serving as the key delivery vehicle in lipid nanoparticles (LNPs) to encapsulate negatively charged nucleic acid macromolecules, such as mRNA vaccines, siRNA therapeutics, and CRISPR gene-editing components. In a physiological, neutral environment, they remain electrically neutral to minimize systemic toxicity and prolong circulation time. Upon entering the acidic microenvironment of cellular endosomes, however, they undergo protonation to become positively charged, thereby inducing membrane fusion and enabling the highly efficient intracellular release of the nucleic acid cargo. Consequently, they serve as the technological cornerstone for bringing nucleic acid therapies into clinical application. To accelerate the translational process of cutting-edge nucleic acid drugs, MCE has meticulously constructed an ionizable lipid compound library containing 95 high-performance molecules, aiming to provide researchers and pharmaceutical professionals with a high-throughput, multi-dimensional lipid screening platform.

Structure Classified Libraries

83
HY-16141 Cilengitide
Cilengitide (EMD 121974) is a BBB-permeable integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.
Integrin   Autophagy   Apoptosis   STAT   PD-1/PD-L1  
Neurological, Eye or Ear Disease   Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Digestive System Inflammation   SARS-CoV-2 Infection   Obesity  
74
HY-13067 Celastrol
Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.
Proteasome   Autophagy   Mitophagy   Apoptosis   Endogenous Metabolite   Antibiotic   Bacterial   Nuclear Hormone Receptor 4A/NR4A  
Cancer   Infection   Inflammation or Immune System Disease  
66
HY-W250163 NAD+ lithium
NAD+ lithium (β-DPN lithium) is a lithium salt of nicotinamide adenine dinucleotide. NAD+ is a coenzyme in the REDOX reaction. NAD+ can directly or indirectly affect several key cellular functions, including metabolic pathways, DNA repair, chromatin remodeling, cell aging, and immune cell function.
Biochemical Assay Reagents  
Metabolic or Endocrine Disease  
50
HY-119374 BRM/BRG1 ATP Inhibitor-1
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.
SWI/SNF Complex  
Cancer  
40
HY-P9904 Atezolizumab
Atezolizumab (MPDL3280A) is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.

Species: Human

PD-1/PD-L1   Apoptosis   Autophagy  
Colorectal Cancer   Liver Cancer   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
40
HY-112288 C188-9
C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia.
STAT   Apoptosis   DNA Methyltransferase  
Lung Cancer   Breast Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Digestive System Inflammation   Obesity  
36
HY-P9902 Pembrolizumab
Pembrolizumab (MK-3475) is a humanized IgG4 antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.

Species: Human

PD-1/PD-L1  
Non-Small Cell Lung Cancer   Lung Adenocarcinoma   HER-2 Positive Breast Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
35
HY-19991 BMS-1
BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction (IC50 between 6 and 100 nM).
PD-1/PD-L1   Apoptosis  
Lung Cancer   Breast Cancer   Colorectal Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Ovarian Cancer   Digestive System Inflammation  
32
HY-P99144 Anti-Mouse PD-1 Antibody (RMP1-14)
Anti-Mouse PD-1 Antibody (RMP1-14) is an anti-mouse PD-1 IgG2a antibody. Anti-Mouse PD-1 Antibody (RMP1-14) can be used for the study of colon carcinoma.

Species: Mouse

PD-1/PD-L1  
Cancer   Inflammation or Immune System Disease  
27
HY-19745 BMS-202
BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC50 of 18 nM and a KD of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity.
PD-1/PD-L1   Apoptosis  
Neurological, Eye or Ear Disease   Lung Cancer   Breast Cancer   Colorectal Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Ovarian Cancer   Digestive System Inflammation  
26
HY-111558 Bobcat339
Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
DNA Methyltransferase   TET Protein  
Leukemia/Lymphoma/Myeloma   Rheumatoid Arthritis  
26
HY-135146 GSK-3484862
GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.
DNA Methyltransferase   Apoptosis  
Lung Cancer   Breast Cancer   Leukemia/Lymphoma/Myeloma  
26
HY-P9903 Nivolumab
Nivolumab is a programmed death receptor-1 (PD-1) blocking human IgG4 antibody to treat advanced (metastatic) non-small cell lung cancer.

Species: Human

PD-1/PD-L1  
Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Triple-Negative Breast Cancer   Metastatic Breast Cancer   SARS-CoV-2 Infection  
23
HY-13962 SGI-1027
SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
DNA Methyltransferase   Apoptosis  
Digestive System Disease   Leukemia/Lymphoma/Myeloma   Digestive System Inflammation   Rheumatoid Arthritis  
19
HY-P99145 Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2)
Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2) is an anti-mouse PD-L1/B7-H1 IgG2b antibody inhibitor derived from host rat. Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2) blocks PD-1 signaling. Anti-Mouse PD-L1/B7-H1 Antibody (10F.9G2) can be used for the research of cancer, such as colon cancer.

Species: Mouse

PD-1/PD-L1  
Colorectal Cancer  
19
HY-N2148 Cytosporone B
Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.

Source: fungus?Eupenicillium?sp. HJ002

Nuclear Hormone Receptor 4A/NR4A  
Neurological, Eye or Ear Disease   Lung Cancer   Glucose Metabolism  
18
HY-145388 AU-15330
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.
PROTACs   SWI/SNF Complex  
15
HY-139664 GSK-3685032
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.
DNA Methyltransferase  
Leukemia/Lymphoma/Myeloma   Rheumatoid Arthritis  
15
HY-13642 RG108
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
DNA Methyltransferase  
Leukemia/Lymphoma/Myeloma   Rheumatoid Arthritis  
14
HY-13765 6-Thioguanine
6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
SARS-CoV   Deubiquitinase   DNA Methyltransferase   Autophagy   Apoptosis   Endogenous Metabolite  
Digestive System Disease   Leukemia/Lymphoma/Myeloma   Viral Infection   Digestive System Inflammation   SARS-CoV-2 Infection   Rheumatoid Arthritis  
13
HY-B1322B Amodiaquine dihydrochloride
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
Nuclear Hormone Receptor 4A/NR4A   Parasite   Histone Methyltransferase  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Leukemia/Lymphoma/Myeloma   Viral Infection   Parasitic Infection  
12
HY-B1322 Amodiaquine dihydrochloride dihydrate
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
Nuclear Hormone Receptor 4A/NR4A   Parasite   Histone Methyltransferase  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Leukemia/Lymphoma/Myeloma   Viral Infection   Parasitic Infection   SARS-CoV-2 Infection  
12
HY-B1322A Amodiaquine
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
Nuclear Hormone Receptor 4A/NR4A   Parasite   Histone Methyltransferase  
Infection   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
12
HY-128359 ACBI1
ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis.
PROTACs   SWI/SNF Complex   Apoptosis  
Non-Small Cell Lung Cancer  
11
HY-112055 DIM-C-pPhOH
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
Nuclear Hormone Receptor 4A/NR4A   Apoptosis  
Cancer   Digestive System Disease   Digestive System Inflammation  
9
HY-P9919 Durvalumab
Durvalumab (MEDI 4736) is an human anti-PD-L1 monoclonal antibody. Durvalumab (MEDI4736) completely blocks the binding of PD-L1 to both PD-1 and CD80, with IC50s of 0.1 and 0.04 nM, respectively.

Species: Human

PD-1/PD-L1  
Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Triple-Negative Breast Cancer   Metastatic Breast Cancer  
6
HY-12409 PFI-3
PFI-3, a chemical probe, is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.
SWI/SNF Complex  
Cancer  
5
HY-18555 TMPA
TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation.
Nuclear Hormone Receptor 4A/NR4A   AMPK  
Pancreatic Cancer   Pain   Digestive System Inflammation   Glucose Metabolism   Obesity  
3
HY-144835 Camibirstat
FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia.
Oxidative Phosphorylation   SWI/SNF Complex  
Acute Myeloid Leukemia  
3
HY-19808 C-DIM12
C-DIM12 is a potent, orally active Nurr1 modulator. C-DIM12 inhibits the tumor growth and autophagy, and induces the cell apoptosis. C-DIM12 has anti-inflammatory and neuroprotective effects, and can be used for cancer and neurological disease study.
Nuclear Hormone Receptor 4A/NR4A  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
2
HY-144896 FHT-1015
FHT-1015 is a selective SMARCA4 (IC50 = 4 nM) and SMARCA2 (IC50 = 5 nM) (also known as BRG1 and BRM) inhibitor. FH-1015 is an allosteric inhibitor that causes conformation change in the BRG1/BRM protein upon interaction with an allosteric site, inhibiting ATPase activity. FH-1015 interferes with tumor cell growth and migration. FH-1015 can be studied in research for uveal melanoma and hematologic cancer.
SWI/SNF Complex  
Leukemia/Lymphoma/Myeloma  
2
HY-P1624 Teduglutide
Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.
Nuclear Hormone Receptor 4A/NR4A   FXR  
Inflammation or Immune System Disease  
2
HY-163410 AU-24118
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).
PROTACs   SWI/SNF Complex   Apoptosis  
Colorectal Cancer   Prostate Cancer   Small Cell Lung Cancer   Multiple Myeloma  
2
HY-155659 4A7C-301
4A7C-301 is a blood-brain barrier-permeable Nurr1 agonist, with IC50 values of 48.22 nM and 107.71 nM for binding to Nurr1-LBD in the [3H]-CQ competition assay and TR-FRET assay, respectively. The EC50 of 4A7C-301 for activating Nurr1 transcriptional activity is 6.53 μM, and its EC50 in N27-A dopaminergic cells is approximately 0.2 μM. 4A7C-301 binds directly to Nurr1-LBD, enhances the transcriptional function of Nurr1, and restores the reduction of Nurr1 protein induced by MPP+ or αSyn. 4A7C-301 alleviates oxidative stress and mitochondrial dysfunction, protects midbrain dopaminergic neurons, inhibits microglial activation, and restores impaired autophagic flux. 4A7C-301 can be used in studies related to neuroprotection and Parkinson's disease.
Nuclear Hormone Receptor 4A/NR4A  
Parkinson's Disease  
1
HY-145446 SGC-SMARCA-BRDVIII
SGC-SMARCA-BRDVIII, a chemical probe, is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII also inhibits PB1(2) and PB1(3), with Kds of 3.7 and 2.0 μM, respectively. SGC-SMARCA-BRDVIII can block adipogenesis of 3T3-L1 murine fibroblasts.
SWI/SNF Complex  
Obesity  
1
HY-P99117 Cadonilimab
Cadonilimab (AK104) is a humanized tetravalent IgG1 bispecific antibody targeting PD1/CTLA4. Cadonilimab blocks both PD-1 and CTLA-4 pathways, thereby relieving their corresponding immunosuppressive effects and reversing tumor specific T cell exhaustion. Cadonilimab significantly downregulates Fc-mediated effector functions, including antibody-dependent cell-mediated cytotoxicity (ADCC), antibody-dependent cellular phagocytosis (ADCP), complement dependent cytotoxicity (CDC). Cadonilimab can be used for research of metastatic cervical cancer, as well as other malignancies such as gastric cancer, GEJ adenocarcinoma and non-small cell lung cancer (NSCLC).

Species: Human

PD-1/PD-L1   CTLA-4  
Inflammation or Immune System Disease   Gastric Cancer   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer  
1
HY-151623 ACBI2
ACBI2 is a highly potent and orally active VHL PROTAC SMARCA2 degrader (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer.
PROTACs   SWI/SNF Complex  
Lung Cancer  
1
HY-158301 MY-1B
MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes.
DNA Methyltransferase   Ligands for E3 Ligase   RNA MTase  
Prostate Cancer  
1
HY-P99675 Ivonescimab
Ivonescimab (AK112) is a PD-1/VEGF bispecific antibody. Ivonescimab competitively inhibiting PD-1/PD-L1 interaction, reversing the immunosuppression mediated by it, and blocks the binding of VEGF-A to VEGFR2, inhibiting tumour angiogenesis in the tumour microenvironment. Ivonescimab also has significantly anticancer activity against EGFR-mutated locally advanced or metastatic non-squamous non-small cell lung cancer (NSCL).

Species: Human

PD-1/PD-L1   VEGFR  
Respiratory Disease   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer  
1
HY-P11903 dTBP-3
dTBP-3 is a fully D-configured polypeptide competitive inhibitor that targets TIGIT. dTBP-3 can competitively occupy the binding interface between TIGIT and its ligand PVR, block TIGIT-mediated immunosuppressive signals, and reverse the immune exhaustion of NK cells and CD8+ T cells. dTBP-3 possesses anti-proteolytic activity and tumor tissue penetration ability, and can also enhance the tumor penetration capacity and cellular internalization efficiency of nanocarriers. dTBP-3 can be used in studies related to liver cancer, triple-negative breast cancer and non-small cell lung cancer.
Transmembrane Glycoprotein   Drug Intermediate  
Liver Cancer   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer  
/
HY-141432G NX-1607 (GMP)
NX-1607 (Cbl-b-IN-3) (GMP) is a GMP-grade NX-1607 (HY-141432). GMP-grade small molecules can be used as adjuvant agents in cell therapy. NX-1607 (GMP) enhances antigen recall, reduces T cell exhaustion and increases cytokine production. NX-1607 is an inhibitor of Cbl-b (an E3 enzyme).
E1/E2/E3 Enzyme  
Cancer   Inflammation or Immune System Disease  
/
HY-P99027 Ieramilimab
Ieramilimab (LAG525; IMP701) is a humanized IgG4 monoclonal antibody that binds to LAG-3, resulting in inhibition of LAG-3 interaction with MHC-II molecules. Ieramilimab restores T-cell and NK-cell-mediated antileukemic immunity by reducing exhaustion and augmenting cytokine output and cytotoxicity. Ieramilimab increases the infiltration of cytotoxic T lymphocytes and reduces baseline densities of regulatory T cells (Tregs) and ADAM10-expressing tumor cells. Ieramilimab can be used for the study of various malignancies including melanoma, RCC, and advanced solid tumors.

Species: Human

LAG-3  
Triple-Negative Breast Cancer  
/
HY-P990120 Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5)
Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5) is an anti-rat Kappa Immunoglobulin Light Chain IgG2a monoclonal antibody. Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5) can enhance B cell depletion. Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5) can enhance T cell exhaustion after the injection of CD4 mAb (HY-P990792) and CD8 mAb (HY-P99129). Anti-Rat Kappa Immunoglobulin Light Chain Antibody (MAR 18.5) can be used for research on immunology.

Species: Rat

Others  
Inflammation or Immune System Disease  
/
HY-N0600 Ginsenoside F3
Ginsenoside F3 is a saponin extracted from the leaves of Panax ginseng with immunoenhancing and antitumor immunostimulatory activities. Ginsenoside F3 upregulates RIPOR2 with a Kd value of 3.77 μM. Ginsenoside F3 enhances NF‑κB activation, upregulates T‑bet and downregulates GATA‑3, increases the production of IL‑2 and IFN‑γ, decreases the production of IL‑4 and IL‑10, reverses CD8⁺ T‑cell exhaustion, restores cytokine secretion, and enhances antitumor immunity in a mouse non‑small cell lung cancer model. Ginsenoside F3 can be used for the research of non-small cell lung cancer.
Interleukin Related   IFNAR   NF-κB  
Digestive System Disease   Cancer Immunology   Digestive System Inflammation  
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HY-P991449 LY3415244
LY3415244 is a bispecific antibody that targets and inhibits TIM-3 and PD-L1. LY3415244 blocks the interaction between TIM-3 on immune cells and PD-L1 on the surface of tumor cells, establishes intercellular connections between TIM-3-positive immune cells and PD-L1-positive tumor cells, and blocks dual immunosuppressive signals. LY3415244 alleviates T cell exhaustion and restores T cell proliferation. LY3415244 induces broad-spectrum anti-drug antibodies, which impairs the binding capacity to soluble TIM-3 targets. LY3415244 can be used in research related to various advanced solid tumors.

Species: Human

PD-1/PD-L1   Tim3  
Cancer  
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HY-N6588 3,4,5-Tricaffeoylquinic acid
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases.
Akt   NF-κB  
Inflammation or Immune System Disease  
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HY-P99139 Anti-Mouse IL-1b Antibody (B122)
Anti-Mouse IL-1b Antibody (B122) is an anti-mouse IL-1b IgG monoclonal antibody. Anti-Mouse IL-1b Antibody (B122) enhances ferroptosis and increases levels of reactive oxygen species (ROS) combined with Sulfasalazine (SAS) (HY-14655). Anti-Mouse IL-1b Antibody (B122) can reduce monocyte infiltration and alleviate T cell exhaustion by blocking IL-1β signaling. Anti-Mouse IL-1b Antibody (B122) can be used for researches on cancer and cardiovascular conditions such as oral squamous cell carcinoma (OSCC), glioblastoma (GBM) and heart failure.

Species: Mouse

Interleukin Related   Reactive Oxygen Species (ROS)   Ferroptosis  
Blood or Cardio-cerebrovascular Disease   Glioma  
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HY-P74601 RBBP4 Protein, Human (sf9, His)
The RBBP4 protein regulates chromatin assembly by binding to core histones and interacting with chromatin assembly factors, remodelers, and histone deacetylases. Its activity is determined by its interaction with nucleosomal DNA. RBBP4 Protein, Human (sf9, His) is the recombinant human-derived RBBP4 protein, expressed by Sf9 insect cells , with N-His labeled tag.

Species: Human; Source: Sf9 insect cells

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HY-P74600 RBBP4 Protein, Mouse (sf9, His)
The RBBP4 protein is a core histone-binding subunit that directs chromatin regulators and histone deacetylases to their substrates and participates in chromatin metabolism.RBBP4 Protein, Mouse (sf9, His) is the recombinant mouse-derived RBBP4 protein, expressed by Sf9 insect cells , with N-His labeled tag.

Species: Mouse; Source: Sf9 insect cells

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HY-P703421 SPT16 Protein, Arabidopsis thaliana
SPT16 Protein, Arabidopsis thaliana is the recombinant SPT16, expressed by E. coli , with tag Free labeled tag. ,

Species: Others; Source: E. coli

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HY-P701613 CECR2 Protein, Human (His)
The CECR2 protein is a regulatory subunit in the CERF-1 and CERF-5 ISWI chromatin remodeling complexes that assembles ordered nucleosome arrays to help DNA enter replication, transcription, and repair. Despite lacking mononucleosome sliding ability, these complexes make crucial contributions to various developmental processes. CECR2 Protein, Human (His) is the recombinant human-derived CECR2 protein, expressed by E. coli , with N-6*His labeled tag.

Species: Human; Source: E. coli

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HY-P85564 SMARCC1 Antibody (YA5256)
SMARCC1 Antibody (YA5256) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to SMARCC1.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Primary Antibodies

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HY-P86786 BAF170 Antibody (YA6479)
BAF170 Antibody (YA6479) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to BAF170.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

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Keywords

T-cell epigenetics | T-cell exhaustion | chromatin remodeling | CRISPR screening | epigenetic repression | adoptive cell therapy