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BI-

" in MedChemExpress (MCE) Product Catalog:

275

Inhibitors & Agonists

4

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11

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4

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5

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23

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3

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6

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16

Isotope-Labeled Compounds

8

Antibodies

2

Click Chemistry

2

Oligonucleotides

1

GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50698
    BI 2536
    55+ Cited Publications

    		 Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis Cancer
    BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription .
    BI 2536
  • HY-153724
    BI-2865
    10+ Cited Publications

    		 Ras Cancer
    BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM) .
    BI-2865
  • HY-125817
    BI-3406
    10+ Cited Publications

    		 SOS1 Ras p38 MAPK Cancer
    BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity .
    BI-3406
  • HY-153723
    BI-2493
    4 Publications Verification

    		 Ras Cancer
    BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. BI-2493 can attenuate tumor growth. BI-2493 can be used for cancer iseases research .
    BI-2493
  • HY-100351
    BI-7273
    1 Publications Verification

    		 Epigenetic Reader Domain Cancer
    BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.
    BI-7273
  • HY-108705
    BI-3802
    3 Publications Verification

    		 Molecular Glues Bcl-2 Family Cancer
    BI-3802, a chemical probe, is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity .
    BI-3802
  • HY-126247
    BI-2852

    		Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
    BI-2852
  • HY-111925
    BI-749327
    15+ Cited Publications

    		 TRP Channel Cardiovascular Disease
    BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .
    BI-749327
  • HY-19730
    Olmutinib
    10+ Cited Publications

    HM61713; BI 1482694

    		 EGFR Cancer
    Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC .
    Olmutinib
  • HY-120350
    BI-1347
    5+ Cited Publications

    		 CDK Cancer
    BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity .
    BI-1347
  • HY-108469
    BI-6015
    5 Publications Verification

    		 Orphan Nuclear Receptor Metabolic Disease Cancer
    BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes .
    BI-6015
  • HY-P991488
    BI-765423

    		Interleukin Related Inflammation/Immunology
    BI-765423 is a selective monoclonal antibody inhibitor targeting IL-11. BI-765423 blocks IL-11-mediated signaling, inhibits fibroblast activation, and can extend the healthy lifespan of mammals, counteract cellular senescence in human cells, and alleviate inflammatory aging-related pathological processes. BI-765423 is primarily used in research on fibrotic diseases such as idiopathic pulmonary fibrosis (IPF) .
    BI-765423
  • HY-129550
    BI-4020

    		EGFR Cancer
    BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .
    BI-4020
  • HY-121251
    BI-167107
    2 Publications Verification

    		 Adrenergic Receptor Neurological Disease Endocrinology Cancer
    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM .
    BI-167107
  • HY-23999
    BI-0115
    2 Publications Verification

    		 LOX-1 Cardiovascular Disease
    BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 μM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain .
    BI-0115
  • HY-116835
    BI-6901
    1 Publications Verification

    		 CCR Inflammation/Immunology
    BI 6901 is a potent, selective CCR10 antagonist (pIC50=9.0). BI 6901 shows high selectivity over other GPCRs, including a number of other chemokine receptors. BI 6901 is efficacious in the murine DNFB model of contact hypersensitivity and can be used for inflammation research .
    BI-6901
  • HY-120929
    BI8622
    4 Publications Verification

    		 E1/E2/E3 Enzyme c-Myc Inflammation/Immunology Cancer
    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. BI8622 can decrease the protein expression levels of c-myc and glycolytic markers as well as immune modulatory markers after HUWE1 inhibition in triple-negative breast cancer (TNBC) cell lines. BI8622 significantly protects against cisplatin (HY-17394)-induced acute kidney injury (AKI). BI8622 significantly reduces the growth of multiple myeloma (MM) cell lines and induces cell cycle arrest. BI8622 can prevent HUWE1-dependent TTBK2 ubiquitination. BI8622 can be studied in research for various diseases including medulloblastoma, acute kidney injury, breast cancer and MM .
    BI8622
  • HY-124625
    BI-4464

    		FAK Target Protein Ligand-Linker Conjugates Infection Cancer
    BI-4464 is a highly selective, ATP competitive PTK2/FAK protein kinase inhibitor with an IC50 value of 17 nM. BI-4464 is a FAK (HY-43760) ligand and linker conjugate. BI-4464 can be used to construct proteolysis targeting chimeras (PROTACs), such as PROTAC FAK degrader 4 (HY-178467). PROTAC FAK degrader 4 is a highly potent and selective FAK PROTAC degrader .
    BI-4464
  • HY-126254
    BI-4924
    1 Publications Verification

    		 Phosphoglycerate Dehydrogenase (PHGDH) Cancer
    BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h .
    BI-4924
  • HY-18955
    BI-847325
    2 Publications Verification

    		 MEK Aurora Kinase Apoptosis Cancer
    BI-847325 is an ATP competitive dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively. BI-847325 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    BI-847325
  • HY-126253
    BI-4916
    5+ Cited Publications

    		 Phosphoglycerate Dehydrogenase (PHGDH) Infection Inflammation/Immunology Cancer
    BI-4916 is a proagent of BI-4924. BI-4924 is a NADH/NAD +-competitive PHGDH inhibitor. BI-4916 inhibits cancer cell migration. BI-4916 can be used for cancer, inflammation and infection study .
    BI-4916
  • HY-111546
    BI-3663
    1 Publications Verification

    		 PROTACs FAK Cancer
    BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker . Anti-cancer activity .
    BI-3663
  • HY-107779
    BI-882370

    		Raf Cancer
    BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .
    BI-882370
  • HY-16100
    BI 99179
    3 Publications Verification

    		 Fatty Acid Synthase (FASN) Metabolic Disease Cancer
    BI 99179, a chemical probe, is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats .
    BI 99179
  • HY-100352
    BI-9564
    2 Publications Verification

    		 Epigenetic Reader Domain Cancer
    BI-9564, a chemical probe, is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family .
    BI-9564
  • HY-150024
    BI-4142

    		EGFR Cancer
    BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM .
    BI-4142
  • HY-111381
    BI-3812
    3 Publications Verification

    		 BCL6 Cancer
    BI-3812, a chemical probe, is a highly efficient BCL6 inhibitor that is capable of suppressing the BTB domain of BCL6, with an IC50 value of ≤ 3 nM, exhibiting antitumor activity .
    BI-3812
  • HY-124063
    BI-1935
    1 Publications Verification

    		 Epoxide Hydrolase Cardiovascular Disease
    BI-1935, a chemical probe, is a potent soluble epoxide hydrolase (sEH) inhibitor. BI-1935 can be used for the research of cardiovascular disease .
    BI-1935
  • HY-18071
    BI-9627
    3 Publications Verification

    		 Na+/H+ Exchanger (NHE) Autophagy Cardiovascular Disease
    BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
    BI-9627
  • HY-168906
    BI-113823

    		Bradykinin Receptor PI3K Akt TNF Receptor ERK Neurological Disease Inflammation/Immunology
    BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .
    BI-113823
  • HY-124772
    BI-2545
    1 Publications Verification

    		 Phosphodiesterase (PDE) Inflammation/Immunology
    BI-2545, a chemical probe, is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC50s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively .
    BI-2545
  • HY-161275
    BI-4732

    		EGFR Akt ERK Ribosomal S6 Kinase (RSK) Cancer
    BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
    BI-4732
  • HY-114208A
    BI-9321 trihydrochloride

    		Histone Methyltransferase Cancer
    BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells .
    BI-9321 trihydrochloride
  • HY-18071A
    BI-9627 hydrochloride
    3 Publications Verification

    		 Na+/H+ Exchanger (NHE) Autophagy Cardiovascular Disease
    BI-9627 hydrochloride is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride decreases autophagy in HTR-8/SVneo cells. BI-9627 hydrochloride can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 hydrochloride prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
    BI-9627 hydrochloride
  • HY-161993
    BI-9787

    		Ketohexokinase Metabolic Disease
    BI-9787 is a zwitterionic inhibitior for ketohexokinase, with an IC50 of 12 and 12.8 nM for hKHK-A and hKHK-C. BI-9787 exhibits good metabolic stability in rat hepatocyte and good pharmacokinetic characteristics in rats .
    BI-9787
  • HY-148278
    BI-0474

    		SOS1 Ras Cancer
    BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
    BI-0474
  • HY-P991517
    BI-836858

    		Transmembrane Glycoprotein Reactive Oxygen Species (ROS) Cardiovascular Disease Cancer
    BI-836858 is a fully human anti-CD33 monoclonal antibody. BI-836858 reduces CD33+ cells via antibody-dependent cellular cytotoxicity (ADCC), blocks downstream signaling of S100A9/CD33, decreases the secretion of immunosuppressive cytokines and reactive oxygen species-induced genomic instability, and restores bone marrow hematopoietic function. BI-836858 is applicable to the research of myelodysplastic syndrome (MDS) and AML .
    BI-836858
  • HY-P991513
    BI-655064

    		TNF Receptor Inflammation/Immunology
    BI-655064, a humanised anti-CD40 antibody with has fragment crystallisable (Fc) regions with two mutations that prevent Fc-mediated antibody-dependent or complement-mediated cellular cytotoxicity and platelet activation. BI-655064 can be used for the study of autoimmune disease, such as lupus nephritis and rheumatoid arthritis (RA) .
    BI-655064
  • HY-114141
    BI-671800

    		Prostaglandin Receptor Inflammation/Immunology Endocrinology
    BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively . BI-671800 has potential for the treatment of poorly controlled asthma .
    BI-671800
  • HY-P990555
    BI-765063

    OSE-172

    		 CD47 Inflammation/Immunology
    BI-765063 (OSE-172) is a humanized antibody expressed in CHO that targets SIRPa/CD172a. BI-765063 contains an IgG4-type heavy chain and a huκ-type light chain, with a predicted molecular weight (MW) of 146.3 kDa. The isotype control for BI-765063 can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
    BI-765063
  • HY-124040
    BI-1950

    		Integrin Inflammation/Immunology
    BI-1950 is a lymphocyte function-associated antigen 1 (LFA-1) inhibitor. BI-1950 regulates immune system function through interaction with LFA-1. BI-1950 can be used in the research of inflammatory diseases .
    BI-1950
  • HY-P991225
    BI-1206

    		Fc Receptor (FcR) CD20 Inflammation/Immunology Cancer
    BI-1206 is a recombinant and antagonistic human monoclonal antibody targeting FcγRIIB (CD32B). BI-1206 can block CD20 internalization induced by Rituximab (HY-P9913) itself or combined with others including Ibrutinib (HY-10997), Venetoclax (HY-15531), and CHOP. BI-1206 can enhance or recover the activity of Rituximab or other anti-CD20 monoclonal antibodies. BI-1206 has cytolytic activity against malignant B cells. BI-1206 can be studied for cancer research such as mantle cell lymphoma (MCL) .
    BI-1206
  • HY-P991402
    BI-1910

    		TNF Receptor Cancer
    BI-1910 is a human monoclonal antibody (mAb) targeting TNFRSF1B. BI-1910 enhances T cell activation and induces CD8 T cell-dependent anti-tumor effects. BI-1910 can be used in solid tumors research. Recommended isotype control: Human IgG2 lambda, Isotype Control (HY-P991206) .
    BI-1910
  • HY-150023
    BI-1622

    		EGFR Itk PI4K Btk CDK Raf JAK Cancer
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
    BI-1622
  • HY-171878
    BI-4659

    		TGF-β Receptor PDGFR TGF-beta/Smad Inflammation/Immunology Cancer
    BI-4659 is a TGFβRI and PDGFRα inhibitor with IC50 values of 19 nM and 99 nM, respectively. BI-4659 inhibits the kinase activities of TGFβRI and PDGFRα, blocks the downstream TGFβRI signaling pathway, and reduces the phosphorylation level of Smad2/3 without altering the expression of TGF-β1. BI-4659 is applicable to research related to pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury .
    BI-4659
  • HY-114208
    BI-9321

    		Histone Methyltransferase Cancer
    BI-9321, a chemical probe, is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells .
    BI-9321
  • HY-100765
    BI-0252

    		MDM-2/p53 E1/E2/E3 Enzyme Cancer
    BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis .
    BI-0252
  • HY-12946
    BI 653048

    		Glucocorticoid Receptor Cytochrome P450 HCV Protease Infection Inflammation/Immunology
    BI 653048, a chemical probe, is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
    BI 653048
  • HY-50698G
    BI 2536

    		Polo-like Kinase (PLK) Apoptosis Epigenetic Reader Domain Cancer
    BI 2536 (GMP) is BI 2536 (HY-50698) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription .
    BI 2536
  • HY-171883
    BI-5756

    		Cannabinoid Receptor CETP MHC Metabolic Disease Inflammation/Immunology Cancer
    BI-5756 is a CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. BI-5756 can significantly increase HDL-C levels and reduce LDL-C levels. BI-5756 can also enhance the function of regulatory T cells while maintaining T cell-mediated anti-tumor activity. BI-5756 can directly inhibit the growth of tumor cells and upregulate the expression of MHC I, MHC II, and CD80 on tumor cells. BI-5756 has a protective effect in graft-versus-host disease models. BI-5756 can be used in research on tumors, graft-versus-host disease, and metabolic diseases .
    BI-5756

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