Search Result
Results for "
Jurkat
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-153161
-
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Caspase
Apoptosis
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Cancer
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CASP8-IN-1 (Compound 63-R) is a selective inhibitor for caspase 8 (CASP8), with an IC50 of 0.7 μM. CASP8-IN-1 inhibits FasL-induced apoptosis in cell Jurkat .
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- HY-163786
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PROTACs
CDK
Apoptosis
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Cancer
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PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))
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- HY-137704
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TRP Channel
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Others
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2′-Deoxy-ADPR is an agonist for transient receptor potential melastatin 2 channel (TRPM2 channel). 2′-Deoxy-ADPR may acts as the signaling molecule in Jurkat T-lymphocytes .
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- HY-173009
-
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PROTACs
Cyclophilin
HCV
HIV
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Infection
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PROTAC CG167 is a selective and potent CypA PROTAC degrader. PROTAC CG167 degrades CypA in a dose-dependent manner (Jurkat: DC50: 123 nM). PROTAC CG167 can inhibit HIV-1 and HCV and exhibits antiviral activity . (Pink: CypA Ligand (HY-170997); Black: Linker (HY-W123015); Blue: E3 Ligase Ligand (HY-112078))
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- HY-155396
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PROTACs
HDAC
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Cancer
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PRO-HD1 is a PROTAC HDAC6 degrader. PRO-HD1 degrades HDAC6 in A549 cells, and inhibits proliferation of Jurkat cells (IC50: 5.8 μM) .
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-
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- HY-149206
-
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MAP4K
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Cancer
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HPK1-IN-33 (compound 21) is a potent Hematopoietic Progenitor Kinase 1 (HPK1) inhibitor with a Ki value of 1.7 nM. HPK1-IN-33 inhibits the produce of IL-2 with EC50s of 286, >10000 nM in Jurkat WT and Jurkat HPK1 KO cells, respectively .
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- HY-172110
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EGFR
Akt
p38 MAPK
ERK
Apoptosis
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Cancer
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Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis .
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- HY-163787
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CDK
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Cancer
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YY173 is a dual inhibitor for CDK4 and CDK6 with IC50 of 7.7 and 88 nM. YY173 inhibits the proliferation of cell Jurkat with an IC50 of 1.46 μM. YY173 can be used for synthesis of PROTAC CDK4/6 degrader 1 (HY-163786) .
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- HY-112335
-
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Src
Interleukin Related
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Cancer
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Lck Inhibitor III (compound 12h) is a potent Lck inhibitor, with an IC50 of 867 nM. Lck Inhibitor III inhibits IL-2 synthesis in Jurkat cells, with an IC50 of 1.270 μM .
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- HY-P5870
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Potassium Channel
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Inflammation/Immunology
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KTX-Sp2 is a potassium channel toxin. KTX-Sp2 effectively blocks three types of exogenous voltage-gated potassium channels: Kv1.1, Kv1.2 and Kv1.3. Ktx-Sp2 inhibits endogenous Kv1.3 and suppresses Ca 2+ signaling in Jurkat T cells. Ktx-Sp2 inhibits IL-2 secretion from activated Jurkat T cells .
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- HY-153702
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JAK
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Cancer
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JAK-IN-27 (compound 1) is an orally active and potent JAKS family kinase inhibitor with IC50s of 3.0 nM (TYK2), 7.7 nM (JAK1), 629.6 nM (JAK3), respectively. JAK-IN-27 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=23.7 nM) .
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- HY-158371
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HDAC
Casein Kinase
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Cancer
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HDAC/CK2-IN-1 (compound 38) is a HDAC1 (IC50 = 1.46 μM), HDAC6 (IC50 = 0.66 μM), and CK2 (IC50 = 3.67 μM) inhibitor. HDAC/CK2-IN-1 exhibits promising antproliferative activity against Jurkat, MCF-7, HCT-116, and HL-60 cell lines .
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- HY-157838
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MAP4K
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Cancer
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HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC50 = 1.39 nM) that potentiates anti-PD-L1 efficacy. HMC-B17 potently enhances the IL-2 secretion in Jurkat cells (EC50 = 11.56 nM). HMC-B17 can be used for the research of cancer .
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- HY-P3083
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PKC
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Inflammation/Immunology
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N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor with an IC50 value of 75 μM. N-Myristoyl-Lys-Arg-Thr-Leu-Arg inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat .
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- HY-153701
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JAK
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Cancer
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JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=17.2 nM) .
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- HY-151066
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PD-1/PD-L1
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Cancer
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BMS-1233 is an orally active inhibitor for programmed cell death-ligand 1 (PD-L1), with IC50 of 14.5 nM. BMS-1233 promotes cell death of HepG2 in a Jurkat T cell and HepG2 cell co-culture model, exhibits antitumor activity against melanoma in mouse model .
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- HY-145322
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Casein Kinase
Molecular Glues
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Cancer
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TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma .
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- HY-110177
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NF-κB
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Inflammation/Immunology
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SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA) .
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- HY-142648A
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MALT1
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Cancer
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(R)-MLT-985 (compound 11) is a potent MALT1 protease inhibitor with an IC50 of 3 nM. (R)-MLT-985 has an IC50 of 20 nM for MALT1-dependent IL-2 production in Jurkat cells. (R)-MLT-985 suppresses growth and aberrant CARD11/BCL10/MALT1 complex signaling in ABC-DLBCL cells .
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- HY-19344
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SAR 1118; SHP-606
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Integrin
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Inflammation/Immunology
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Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
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- HY-19344A
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SAR 1118 sodium; SHP-606 sodium
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Integrin
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Inflammation/Immunology
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Lifitegrast (SAR 1118) sodium is a potent integrin antagonist. Lifitegrast sodium blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast sodium inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast sodium can be used for researching dry eye disease .
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- HY-162643
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PD-1/PD-L1
PARP
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Cancer
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Antitumor agent-169 (Compound B3) is a dual inhibitor PD-1/PD-L1 interaction and PARP7, with IC50s of 0.426 μM and 2.50 nM. Antitumor agent-169 exhibits an affinity to human PD-L1, with Ki of 20.2 nM. Antitumor agent-169 restores the T cell function, increases IFN-γ secretion. Antitumor agent-169 inhibits cell viability of MDA-MB-231 and Jurkat T, exhibits antitumor efficacy against melanoma in mouse model and good pharmacokinetic characteristics .
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- HY-19344R
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Integrin
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Inflammation/Immunology
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Lifitegrast (Standard) is the analytical standard of Lifitegrast. This product is intended for research and analytical applications. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
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- HY-145321
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Phosphodiesterase (PDE)
Molecular Glues
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Cancer
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TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC50 values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma .
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- HY-B1046
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- HY-P10838
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PD-1/PD-L1
Apoptosis
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Inflammation/Immunology
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PL120131 is a PD-1/PD-L1 inhibitory peptide that can interfere with the interaction of PD-1/PD-L1 by binding to PD-1. PL120131 is capable of inhibiting the PD-1-mediated apoptotic signaling pathway, protecting Jurkat cells and primary lymphocytes from apoptosis. PL120131 aids in the antitumor activity of cytotoxic T lymphocytes (CTLs) .
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- HY-115756
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Others
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Others
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4-Maleimidosalicylic acid is a polar maleimide, and does not suppress IL-2 production in JURKAT T cells .
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- HY-172200
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PD-1/PD-L1
HDAC
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Cancer
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PD-L1/HDAC6-IN-1 (Compound HP29) is the inhibitor for PD-L1 and HDAC6 that inhibits the PD-L1/PD-1 interaction and HDAC6 with an IC50 of 26.8 nM and 69 nM. PD-L1/HDAC6-IN-1 enhances the killing ability of Jurkat T cells against HepG2 cells with an IC50 of 3.4 μM. PD-L1/HDAC6-IN-1 exhibits good pharmacokinetics characteristics in rats with a drug exposure of 871.62 ng·h/mL, and exhibits antitumor activity in mouse B16-F10 xenograft models .
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- HY-B1046R
-
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Bacterial
Antibiotic
DNA/RNA Synthesis
Interleukin Related
Apoptosis
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Infection
Inflammation/Immunology
Cancer
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Clofazimine (Standard) is the analytical standard of Clofazimine. This product is intended for research and analytical applications. Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research .
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- HY-N1726
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Others
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Inflammation/Immunology
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cis-Burchellin is a bioactive neolignan with anti-allergic activity. cis-Burchellin inhibits IL-2 production in Jurkat T-cells .
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- HY-109151
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E6007
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Others
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Inflammation/Immunology
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Milategrast is useful as cell adhesion inhibitor or cell infiltration inhibitor. Milategrast in vitro inhibites the adhesion of Jurkat cells to human fibronectin with an IC50 of ＜5 μM .
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- HY-156085
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PD-1/PD-L1
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Cancer
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LP23 is a non-arylmethylamine PD-1/PD-L1 inhibitor (IC50: 16.7 nM) with anti-tumor activity. LP23 restores immune cell function in HepG2/Jurkat T cells and promotes HepG2 cell death. LP23 is active in vivo in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg) .
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- HY-14622
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RIP kinase
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Cancer
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Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. Necrostatin 2 is also a RIPK1 inhibitor.
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- HY-N6681
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Caspase
Bacterial
Apoptosis
Antibiotic
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Infection
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15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3 .
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- HY-158052
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1 antagonist 1 (Compound A5) is an antagonist for programmed cell death-1 (PD-1) and programmed cell death ligand-1 (PD-L1) interaction, with an IC50 of 23.78 nM .
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- HY-168963
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PROTACs
Btk
Itk
p38 MAPK
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Inflammation/Immunology
Cancer
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PROTAC BTK Degrader-13 (Compound 25) is the PROTAC degrader for BTK with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 inhibits the activity of BTK with an IC50 of 0.44 μM, inhibits IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. PROTAC BTK Degrader-13 inhibits p38 MAPK signaling pathway, block the activation of the BCR (B cell receptor) signaling pathway . (Pink: ligand for target protein BTK ligand 15 (HY-168965); Black: linker (HY-Y0524); Blue: ligand for E3 ligase cereblon (HY-103596))
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- HY-15760
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- HY-163902
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CRM1
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Cancer
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SP100030 analogue 1 (compound 11), a SP100030 (HY-110177) analogue, is a selective inhibitor of transcriptional activation (SITA) with an EC50 of 137 nM for suppressing the XPO1-dependent upregulation of IL2 by Jurkat-based IL2-Luc reporter assay .
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- HY-W033813
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Caspase
Apoptosis
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Cancer
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Caspase-3/7 inhibitor I is a potent and reversible inhibitor of caspase-3 and caspase-7, with Kis of 60 and 170 nM, respectively. Caspase-3/7 inhibitor I can inhibit apoptosis in Camptothecin (HY-16560)-treated Jurkat cells and in chondrocytes .
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- HY-170814
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G-quadruplex
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Cancer
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G-quadruplex ligand 3 (Compound 16) is a G-quadruplex ligand with anticancer effects that chelate iron. G-quadruplex ligand 3 stabilizes G-quadruplexes in human leukemia Jurkat cells. G-quadruplex ligand 3 localizes in the cell nucleus, serving as a fluorescent nuclear tracer for the labile iron pool .
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- HY-145776
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- HY-159123
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MAP4K
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Cancer
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KHK-6 is an inhibitor for serine/threonine kinase hematopoietic progenitor kinase 1 (HPK 1) with an IC50 of 20 nM. KHK-6 enhances CD3/CD28-induced cytokine production, enhances CD69, CD25 and HLA-DR markers on CD4+ and CD8+ T cells, and enhances T cell-mediated killing activity of SKOV3 and A549 cells .
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- HY-172396
-
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PD-1/PD-L1
VISTA
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Cancer
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PD-L1/VISTA-IN-2 (Compound S8) is an orally active bifunctional PD-L1/VISTA inhibitor with an IC50 of 1.4 μM for PD-L1 and a KD of 2.1 μM for VISTA. PD-L1/VISTA-IN-2 can activate the tumor immune microenvironment and exert anti-cancer effects .
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- HY-161392
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CRM1
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Cancer
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CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
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- HY-136252
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PROTACs
CDK
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Cancer
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BSJ-04-132 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity .
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- HY-161391
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CRM1
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Cancer
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CW0134 (Compound 12) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
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- HY-124833
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Casein Kinase
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Cancer
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Quinalizarin is a potent, selective and cell-permeable protein kinase CK2 inhibitor with an Ki of ~50 nM and an IC50 of 110 nM. Quinalizarin can induce apoptosis of certain cancer cells .
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- HY-117782
-
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Others
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Cancer
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Anticancer agent 236 (compound JP-8g) is a broad-spectrum anticancer agent that has toxic effects on several cancer cell lines with IC50 values of 6.925 μM (MDA), 6.296 μM (U937), 6.548 μM (Jurkat), 6.373 μM (Hela), and 10.381 μM (EJ) .
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- HY-P10815
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Apoptosis
Calcium Channel
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Others
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IP3RCYT is an IP3R inhibitory peptide, which can inhibit the binding of cytochrome C to IP3R with an IC50 about 100 nM. IP3RCYT regulates calcium signaling within cells. P3RCYT inhibits apoptosis in HeLa and Jurkat cells treated with Staurosporine (HY-15141) or Membrane-bound Fas ligand (FasL) .
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- HY-N0990
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Others
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Cancer
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1,5,15-Trimethylmorindol is an anthraquinone isolated from the leaves of Morinda citrifolia. 1,5,15- trimethylmorindol (25 μg/mL) does not show significant cytotoxic activity on the human T-cell leukemia cell line, Jurkat, by itself but it shows cytotoxicity (IC50 14.5-15.0 μg/mL) when combined with 0.5-1.5 μg/mL of TRAIL in the cell proliferation assay .
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- HY-144817
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 27 (DYT-1) is a tubulin polymerisation inhibitor with an IC50 of 25.6 µM. Tubulin inhibitor 27 shows anti-angiogenesis and antitumor activities .
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- HY-138113
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Interleukin Related
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Inflammation/Immunology
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Pyrrothiogatain is an inhibitor for transcription factor GATA. Pyrrothiogatain inhibits the DNA-binding activity of GATA3, inhibits the T helper 2 (Th2) cell differentiation and expression of Th2 cytokines. Pyrrothiogatain is potential in Th2 related allergic disorders .
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- HY-148454
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- HY-139875
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CDK
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Cancer
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JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC50 values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties .
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- HY-148847
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MAP4K
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Cancer
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HPK1-IN-32 is a potent and selective HPK1 inhibitor with an IC50 of 65 nM. HPK1-IN-32 can be used for the research of HPK1 related disorders or diseases .
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- HY-149232
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MAP4K
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Cancer
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HPK1-IN-35 is a potent and selective HPK1 inhibitor with an IC50 value of 3.5 nM. HPK1-IN-35 decreases the expression of p-SLP76 and promotes IL-2 secretion .
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- HY-144672
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- HY-173013
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Cyclophilin
HIV
HCV
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Infection
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TWH106 is an inhibitor for Cyclophilin (Cyp) that exhibits good affinity to CypA and CypB with KD of 53 nM and 139 nM. TWH106 inhibits the replication of HIV and HCV, exhibiting antiviral activity .
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- HY-164263
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NAPS
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Apoptosis
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Cancer
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N-Acetylphytosphingosine (NAPS) is a sphingolipid derivative. N-Acetylphytosphingosine induces mitochondria-dependent Apoptosis by activating Bak. N-Acetylphytosphingosine has antitumor activity .
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- HY-123802
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Integrin
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Cancer
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BIO7662 is a specific α4β1 antagonist. BIO7662 can be used to study α4β1 integrin-ligand interactions .
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- HY-168628
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Epigenetic Reader Domain
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Cancer
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BET-IN-27 (compound 6C) is an oral BET inhibitor with the IC50 values of 3.3 nM (BRD4-BD2)、3.4 nM (BRD4-BD1)、4.1 nM (BRD2-BD1)、20.4 nM (BRD3-BD1) and 42.0 nM (BRDT-BD1), respectively. BET-IN-27 shows anti-proliferative activity .
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- HY-19344S2
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Isotope-Labeled Compounds
Integrin
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Inflammation/Immunology
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Lifitegrast-d4-1 is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
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- HY-153598
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PROTACs
RIP kinase
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Cancer
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LD4172 is a PROTAC degrader for RIP kinase (RIPK1) with DC50 in nanomolare levels. LD4172 induces apoptosis in cell B16F10 with combination of TNF-α. LD4172 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170613); Black: linker (HY-W012241); Blue: ligand for E3 ligase VHL (HY-112078))
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- HY-N8372
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Potassium Channel
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Inflammation/Immunology
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Nalanthalide is a voltage-gated potassium channel Kv1.3 blocker (IC50=3.9 µM) and a potential immunosuppressant. Nalanthalide can be used for research on inflammatory immune diseases, such as neuroinflammation .
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- HY-146671
-
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Itk
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Cancer
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ITK inhibitor 5 (compound 27) is a potent and selective ITK inhibitor with IC50s of 5.6, 25 nM for ITK, BTK, respectively .
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- HY-163725
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- HY-117433
-
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DNA Alkylator/Crosslinker
Apoptosis
Reactive Oxygen Species
Drug Metabolite
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Inflammation/Immunology
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4-Hydroperoxy cyclophosphamide is the active metabolite form of the precursor Cyclophosphamide. 4-Hydroperoxy cyclophosphamide cross-links DNA to induce T cell apoptosis independent of caspase receptor activation, and can activate the mitochondrial death pathway by producing reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide can be used in the study of rheumatoid arthritis and autoimmune diseases .
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- HY-155219
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Methylenetetrahydrofolate Dehydrogenase (MTHFD)
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Cancer
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TH9028 is an inhibitor of MTHFD2 (IC50 = 11 nM) with IC50 values against hMTHFD2, MTHFD2L, and MTHFD1 being 7.97 nM, 27 nM, and 0.5 nM, respectively. TH9028 also exhibits anti-cancer cell proliferation activity .
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- HY-19344S1
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SAR 1118-d6; SHP-606-d6
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Isotope-Labeled Compounds
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Inflammation/Immunology
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Lifitegrast-d6 (SAR 1118-d6) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
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- HY-172107
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MAP4K
Interleukin Related
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Inflammation/Immunology
Cancer
|
|
HPK1-IN-56 (Compound A29) is a HPK1 inhibitor (IC50: 2.70 nM). HPK1-IN-56 inhibits downstream p-SLP76 (IC50: 8.1 nM in Jurkat T cells). HPK1-IN-56 induces the production of IL-2 in human PBMCs. HPK1-IN-56 has anticancer effect, enhances T-cell killing ability and the antitumor efficacy of anti-PD-1 antibody .
|
-
- HY-19344S
-
|
SAR 1118-d4; SHP-606-d4
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Lifitegrast-d4 (SAR 1118-d4) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
|
-
- HY-168770
-
|
|
RIP kinase
TNF Receptor
Apoptosis
|
Cardiovascular Disease
|
|
Cl-Necrostatin-1 is a RIPK1 inhibitor. Cl-Necrostatin-1 can also inhibit TNF-α-induced necroptosis in Jurkat cells deficient in Fas-associated death domain protein (FADD; EC50 = 180 nM), a modification that prevents caspase activation in response to death-domain receptor signaling. Cl-Necrostatin-1 can also reduce infarct size in a mouse model of middle cerebral artery occlusion (MCAO). Cl-Necrostatin-1 is used for research in cardiovascular and cerebrovascular diseases .
|
-
- HY-135078
-
|
NSC 270912
|
DNA/RNA Synthesis
|
Others
|
|
2,5-Deoxyfructosazine is a pyrazine derivative that can be found in cured tobacco and is used as a flavoring agent in the food and tobacco industry. Pyrazines, including 2,5-deoxyfructosazine, can be produced either by pyrolytic decomposition of natural compounds or by the reaction of sugars with alcoholic ammonia. 2,5-Deoxyfructosazine is also formed by the breakdown of D-glucosamine at neutral pH. Like glucosamine, 2,5-deoxyfructosazine has DNA strand breakage activity and strongly inhibits IL-2 production by Jurkat cells stimulated with phytohemagglutinin (IC50=~1.25 mM).
|
-
- HY-160214
-
|
|
Drug Derivative
|
Inflammation/Immunology
|
|
Perforin-IN-2 is a benzosulfonamide perforin inhibitor that alleviates transplant rejection during allogeneic bone marrow/stem cell transplantation. Perforin-IN-2 binds to plasma proteins with a binding rate of 99.8%. Perforin-IN-2 requires a higher concentration (> 900 μM) to achieve optimal perforin inhibition in vivo. Perforin-in-2 can effectively inhibit the lytic activity of recombinant perforin on Jurkat T (IC50=6.65 μM) leukemia cells, and also inhibit the death of K562 leukemia target cells .
|
-
- HY-163920
-
|
|
PROTACs
HDAC
|
Cancer
|
|
Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC50 of 0.27 nM in A549 cells .
|
-
- HY-110052
-
|
|
Casein Kinase
|
Cancer
|
|
TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases .
|
-
- HY-163177
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-63 (compound S17) is a potent HIV-1 inhibitor. HIV-1 inhibitor-63 inhibits integrase-Ku70 complex formation with an IC50 value of 12 µM. HIV-1 inhibitor-63 inhibits HIV-1 post-integration DNA repair .
|
-
- HY-124290A
-
|
AJM300 hydrochloride
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) hydrochloride is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl hydrochloride, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl hydrochloride prevents the development of colitis in mice .
|
-
- HY-144998
-
|
|
IKZF Family
Molecular Glues
|
Inflammation/Immunology
Cancer
|
|
NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2 .
|
-
- HY-163496
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-45 (Compound 3) is a HPK1 inhibitor, with an IC50 of 0.3 nM. HPK1-IN-45 inhibits SLP-76 phosphorylation (IC50 = 57.52 nM) and IL-2 release (IC50 = 38 nM). HPK1-IN-45 can be used for the research of cancer .
|
-
- HY-151191
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-22 is a potent Lysine-specific demethylase 1 (LSD1) inhibitor with a Ki value of 98 nM. LSD1-IN-22 has anti-proliferative activity against certain cancer cells .
|
-
- HY-169853
-
|
|
VISTA
|
Inflammation/Immunology
|
|
M351-0056 is the agonist for the immune checkpoint protein VISTA, that reduces the secretion of VISTA-induced cytokines, promotes the T-cell proliferation induced by VISTA, and exhibits immunomodulatory activity. M351-0056 ameliorates Imiquimod (HY-B0180)-induced psoriatic dermatitis in mouse models .
|
-
- HY-124290
-
|
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice .
|
-
- HY-155101
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-L1-IN-3 (Compound 4a) is a compound that targets PD-1/PD-L1, the IC50 value and EC50 value is 4.97nM and 2.70 μM for inhibit PD-L1 and Jurkat T cells, respectively. PD-L1-IN-3 can bind PD-L1 dimer to prevent PD-1 binding to PD-L1, therefore blocking PD-1 signaling. PD-L1-IN-3 can be used for lung cancer and melanoma diseases research .
|
-
- HY-116692
-
|
|
Apoptosis
Caspase
Mitochondrial Metabolism
PARP
DNA/RNA Synthesis
|
|
|
Apoptosis inducer 34 (Compound 4) is a small molecule compound that induces apoptosis by directly activating the intrinsic apoptotic pathway. Apoptosis inducer 34 promotes Apaf-1 oligomerization to form mature apoptosomes, thereby activating caspase-9 and caspase-3. It significantly activates the apoptotic pathway in Jurkat cells by enhancing the cytochrome c-dependent apoptotic signaling pathway, inducing PARP cleavage and chromosomal DNA fragmentation. Furthermore, Apoptosis inducer 34 exhibits low toxicity to normal cells, demonstrating potential for selective targeting of cancer cells. Apoptosis inducer 34 is a promising candidate for studying cancer related to apoptotic pathways .
|
-
- HY-B0914
-
|
Undecylenic acid
|
Fungal
Amyloid-β
Reactive Oxygen Species
Proteasome
Bacterial
|
Infection
Neurological Disease
Endocrinology
Cancer
|
|
10-Undecenoic acid (Undecylenic acid) is an antifungal agent. 10-Undecenoic acid inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid has neuroprotective effects. 10-Undecenoic acid has anticancer effects on a variety of tumors. 10-Undecenoic acid inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa .
|
-
- HY-N15185
-
|
(-)-Pyrenophorin
|
Herbicide
|
Cancer
|
|
Pyrenophorin ((-)-Pyrenophorin) is a fungal metabolite that has been found in D. avenae and has phytotoxic activity. Pyrenophorin shows strong cytotoxicity against several cancer cell lines with IC50 values ranging from 0.07 to 7.8 μM .
|
-
- HY-162644
-
|
|
PD-1/PD-L1
PARP
|
Cancer
|
|
Antitumor agent-170 (Compound C6) exhibits inhibitory activities against PD-1/PD-L1 interaction and PARP7, with IC50 of 0.342 μM and 7.05 nM. Antitumor agent-170 exhibits a high affinity to human PD-L1, with a Ki of 9.31 nM. Antitumor agent-170 restores the T cell function and increases IFN-γ secretion. Antitumor agent-170 exhibits antitumor efficacy against melanoma in mouse models and good pharmacokinetic characteristics .
|
-
- HY-108691
-
|
|
Itk
Btk
CXCR
PD-1/PD-L1
LAG-3
|
Cancer
|
|
PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM. PF-06465469 also inhibits BTK. PF-06465469 inhibits cell migration in response to CXCL12. PF-06465469 decreases PD-1 and LAG-3 expression. PF-06465469 can be used to study leukemia and T-cell lymphoma .
|
-
- HY-155874
-
|
|
CDK
|
Cancer
|
|
ZNL-05-044 is a CDK11 inhibitor with an IC50s of 0.23 μM and 0.27 μM against CDK11A and CDK11B, respectively (NanoBRET assay). ZNL-05-044 leads to G2/M cell cycle arrest and impairs RNA splicing .
|
-
- HY-160944
-
|
|
Sirtuin
|
Cancer
|
|
hsa62 is a dual inhibitor for SIRT1 and SIRT2, with IC50 of 1.3 and 5.5 μM, respectively .
|
-
- HY-163444
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 15 (Compound 3) induces cell apoptosis and cell cycle arrest at G2/M phase. Apoptosis inducer 15 is cytotoxicitic without causing DNA fragmentation .
|
-
- HY-153583
-
|
|
HDAC
|
Cancer
|
|
HDAC8-IN-4 is a selective inhibitor of HDAC8. HDAC8-IN-4 inhibits HDAC8 and HDAC3 with IC50s of 0.15 and 12 μM .
|
-
- HY-143270
-
-
- HY-N3119
-
|
|
Apoptosis
|
Cancer
|
|
Paeoniflorigenone, isolated as an active ingredient from the root of moutan cortex, induces apoptosis selectively in the cancer cell lines and exhibits antiproliferative effect .
|
-
- HY-151369
-
|
|
RIP kinase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
AV123 (compound 12) is a non-cytotoxic RIPK1 inhibitor (IC50=12.12 µM). AV123 blocks the TNF-α-induced necroptotic (EC50=1.7 μM) but not the apoptotic cell death. AV123 can be used in the study of necrotic chronic conditions such as ischemia-reperfusion injury of the brain, heart and kidney, inflammatory diseases, neurodegenerative diseases and infectious diseases .
|
-
- HY-B0914B
-
|
Undecylenic acid (copper)
|
Fungal
Bacterial
Amyloid-β
Reactive Oxygen Species
Proteasome
|
Infection
Neurological Disease
Endocrinology
Cancer
|
|
10-Undecenoic acid copper (Undecylenic acid copper) is an antifungal agent. 10-Undecenoic acid copper inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid copper has neuroprotective effects. 10-Undecenoic acid copper has anticancer effects on a variety of tumors. 10-Undecenoic acid copper inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid copper inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa .
|
-
- HY-169093
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078) .
|
-
- HY-110382
-
|
c-di-GMP disodium; cyclic diguanylate disodium; 5GP-5GP disodium
|
STING
Endogenous Metabolite
|
Cancer
|
|
Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research .
|
-
- HY-141877
-
MS4322
1 Publications Verification
YS43-22
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-107780B
-
|
c-di-GMP diammonium; cyclic diguanylate diammonium; 5GP-5GP diammonium
|
STING
Endogenous Metabolite
|
Cancer
|
|
Cyclic-di-GMP diammonium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP diammonium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP diammonium can be used in cancer research .
|
-
- HY-101761A
-
|
|
PAI-1
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-N8287
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Oxaline is a fungal alkaloid that can be isolated from Penicillium oxalicum. Oxaline inhibits tubulin polymerization, resulting in cell cycle arrest at the M phase .
|
-
- HY-108352
-
|
VCE 004
|
Topoisomerase
|
Cancer
|
|
HU 331 (HU 331) is a highly specific Topoisomerase II inhibitor with anticancer activity. HU 331 has shown promising inhibitory effects on human cancer cell lines in vitro and human tumor xenografts in nude mice in vivo .
|
-
- HY-107780A
-
|
c-di-GMP sodium; cyclic diguanylate sodium; 5GP-5GP sodium
|
STING
Endogenous Metabolite
|
Cancer
|
|
Cyclic-di-GMP sodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP sodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP sodium can be used in cancer research .
|
-
- HY-107780
-
|
c-di-GMP; cyclic diguanylate; 5GP-5GP
|
STING
Endogenous Metabolite
|
Cancer
|
|
Cyclic-di-GMP is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP can be used in cancer research .
|
-
- HY-171034
-
|
|
Interleukin Related
TNF Receptor
PAK
|
Inflammation/Immunology
|
|
PQA-18 is a unique PAK2 inhibitor (IC50: 10 nM). PQA-18 has immunosuppressing effects. PQA-18 suppresses IL2, IL4, IL6, and TNFα. PQA-18 inhibits the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens as well as alleviates dermatitis in mice .
|
-
- HY-P10415
-
|
hSA(408–423) peptide
|
CXCR
|
Infection
Inflammation/Immunology
Cancer
|
|
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
|
-
- HY-148174
-
|
|
DGK
|
Cancer
|
|
JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation .
|
-
- HY-146389
-
|
|
MDM-2/p53
P-glycoprotein
|
Cancer
|
|
Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma .
|
-
- HY-153567
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
|
|
Immune cell migration-IN-2 is a potent immune cell migration inhibitor with an EC50 of 13.5 nM in a T-cell adhesion assay. Immune cell migration-IN-2 is extracted from patent WO2019001171, example 11, can be used for dry-eye and other retinal diseases research . Immune cell migration-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-151426
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 83 is a potent anticancer agent, inhibits LOX IMVI cells growth with a GI50 value of 0.15 mM. Anticancer agent 83 reduces mitochondrial membrane potential and induces DNA damage to induces leukemia cells apoptosis .
|
-
- HY-156578
-
|
|
DGK
HIV
|
Infection
Cancer
|
|
DGKα-IN-8 (Example 51) is a DGKα inhibitor (IC50=22.491 nM; EC50=0.256 nM). DGKα-IN-8 can be used to study cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection .
|
-
- HY-N9388R
-
|
|
p38 MAPK
|
Infection
Inflammation/Immunology
|
|
Andrograpanin (Standard) is the analytical standard of Andrograpanin. This product is intended for research and analytical applications. Andrograpanin, a bioactive compound from Andrographis paniculata, exhibits anti-inflammatory and anti-infectious properties .
|
-
- HY-130854
-
|
|
E3 Ligase Ligand-Linker Conjugates
Autophagy
Apoptosis
|
Cancer
|
|
Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A) .
|
-
- HY-148933
-
-
- HY-B0464R
-
|
|
Bcl-2 Family
Caspase
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Hydralazine (hydrochloride) (Standard) is the analytical standard of Hydralazine (hydrochloride). This product is intended for research and analytical applications. Hydralazine hydrochloride is an antihypertensive agent. Hydralazine hydrochloride can inhibit mitochondrial fission and human peritoneal mesothelial cell proliferation. Hydralazine hydrochloride has immunomodulation and anti-migratory effect. Hydralazine hydrochloride activates the intrinsic pathway of apoptosis and causes DNA damage .
|
-
- HY-W320239
-
-
- HY-14174
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MRK-560 is an orally active, brain barrier-penetrated γ-Secretase inhibitor, reducing Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL) .
|
-
- HY-161335
-
|
|
MAP4K
Interleukin Related
IFNAR
|
Cancer
|
|
HPK1-IN-43 (compound 9f) is a HPK1 kinase inhibitor with the IC50 value of 0.32 nM. HPK1-IN-43 inhibits the phosphorylation of the downstream protein SLP-76 and enhances the secretion of interleukin-2 (IL-2) and interferon-γ (IFN-γ). HPK1-IN-43 can be used in cancer research .
|
-
- HY-148391
-
|
SBF-1
|
DNA/RNA Synthesis
|
Cancer
|
|
23-Oxa-OSW-1 (SBF-1), a derivative of OSW 1 (HY-101213), is a potent osterol-binding protein (OSBP) inhibitor. 23-Oxa-OSW-1 has antitumor activity .
|
-
- HY-B0464
-
|
|
Bcl-2 Family
Caspase
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Hydralazine hydrochloride is an antihypertensive agent. Hydralazine hydrochloride can inhibit mitochondrial fission and human peritoneal mesothelial cell proliferation. Hydralazine hydrochloride has immunomodulation and anti-migratory effect. Hydralazine hydrochloride activates the intrinsic pathway of apoptosis and causes DNA damage .
|
-
- HY-N9388
-
-
- HY-13701
-
-
- HY-13701R
-
|
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
Nelarabine (Standard) is the analytical standard of Nelarabine. This product is intended for research and analytical applications. Nelarabine (506U78) is a nucleoside analogue and can be used for the research of T cell acute lymphoblastic leukemia (T-ALL) .
|
-
- HY-168493
-
|
|
FLT3
VEGFR
HDAC
STAT
PERK
|
Cancer
|
|
FLT3/VEGFR2-IN-1 (Compound 26) is a FLT3/VEGFR2/HDAC inhibitor with IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM for FLT3, VEGFR2, and HDAC1, respectively. FLT3/VEGFR2-IN-1 can inhibit the phosphorylation of STAT3 and ERK1/2 and the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 has anti-tumor activity and can be used for the research of acute myeloid leukemia .
|
-
- HY-117513
-
|
|
Proteasome
Apoptosis
|
Cancer
|
|
CEP1612 is a dipeptidyl proteasome inhibitor with the IC50 of 60 nM. CEP1612 induces p21(WAF1)and p27(KIP1) expression and cell apoptosis. CEP1612 shows anticancer activity in vivo .
|
-
- HY-18974
-
-
- HY-147838
-
|
|
NAMPT
|
Cancer
|
|
Nampt-IN-9 (Compound 8) is a potent NAMPT inhibitor with anticancer activities. Nampt-IN-9 can be used for pancreatic ductal adenocarcinoma research .
|
-
- HY-P99445
-
|
APG101; CAN008
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Asunercept (APG101; CAN008) is a soluble CD95-Fc fusion protein targeting CD95L. Asunercept disrupts CD95/CD95L signaling by selectively binding to CD95L. Asunercept can be used in the research of glioblastoma multiforme (GBM), myelodysplastic syndrome (MDS), and graft-versus-host disease (GvHD) .
|
-
- HY-149773S
-
|
|
MAP4K
|
Inflammation/Immunology
Cancer
|
|
HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC50 of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity .
|
-
- HY-137325A
-
|
|
Calcium Channel
|
Metabolic Disease
|
|
2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
|
-
- HY-146672
-
|
|
Itk
|
Cancer
|
|
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
|
-
- HY-136250A
-
|
|
PROTACs
CDK
|
Cancer
|
|
BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 triTFA is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and has anti-cancer activity .
|
-
- HY-14389
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM . LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research .
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-
- HY-120075
-
|
|
Apoptosis
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Cancer
|
|
TJ191 is a potent and specific anti-cancer agent that targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells. TJ191 has no affects on the proliferation of other cancer cells or normal fibroblasts or immune cells. TJ191 can be used for cancer research .
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- HY-169318
-
-
- HY-12521
-
|
|
CRAC Channel
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Inflammation/Immunology
|
|
GSK-5498A is a selective CARC channel inhibitor (IC50: 1 μM). GSK-5498A inhibits mediators release from mast cells and pro-inflammatory cytokines release from T cells. GSK-5498A can be used in the research of inflammatory disorders .
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-
- HY-136250
-
|
|
PROTACs
CDK
|
Cancer
|
|
BSJ-03-204 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity .
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- HY-143461
-
|
|
Casein Kinase
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Cancer
|
|
CK2 inhibitor 3 is a potent CK2 inhibitor with IC50 value of 280 nM. CK2 inhibitor 3 inhibits endocellular CK2, significantly affects viability of tumour cells and shows remarkable selectivity on a panel of 320 kinases .
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-
- HY-169317
-
-
- HY-149917
-
|
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PROTACs
Itk
|
Cancer
|
|
ITK degrader 1 is a highly selective degrader of interleukin-2-inducible T-cell kinase (ITK; DC50=3.6 nM in vivo in mice), with good plasma exposure levels. ITK degrader 1 induces rapid, and prolonged ITK degradation and suppresses IL-2 secretion (EC50=35.2 nM, Jurkat cells) stimulated by anti-CD3 antibodyin vivo. ITK degrader 1 consists of target protein ligand (red part) ITK ligand 1 (HY-168387), PROTAC linker (black part) Piperidine-C2-piperazine-Boc (HY-168388) and E3 ubiquitinase ligand (blue part) Thalidomide 5-fluoride (HY-W087383). E3 ubiquitinase and PROTAC linker can form Thalidomide-piperidine-C2-piperazine-Boc (HY-168389) .
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-
- HY-124798
-
|
|
mTOR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity .
(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
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- HY-14942A
-
|
RTA 744; WP 744; WP 769 hydrochloride
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Apoptosis
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Cancer
|
|
Berubicin hydrochloride (RTA 744) is a Doxorubicin (HY-15142A) analogue. Berubicin hydrochloride triggers apoptosis and cell killing in NB cells by activating proapoptotic mediators. Berubicin hydrochloride has proapoptotic and anti-leukemia activities. Berubicin hydrochloride can be used for cancer research .
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-
- HY-13496
-
|
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
JNJ-28312141 is an inhibitor for colony-stimulating factor-1 receptor (CSF-1R or FMS), with an IC50 of 0.69 nM. JNJ-28312141 inhibits proliferation of BDBM, MV-4-11, M-o7e, TF-1 with an IC50s of 2.6, 21, 41 and 150 nM, respectively. JNJ-28312141 exhibits anti-inflammatory activity in mouse arthritis model .
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-
- HY-146209
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
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Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity .
|
-
- HY-N7085
-
|
5,7-Dimethoxycoumarin; Limettin
|
JNK
p38 MAPK
ERK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
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-
- HY-160018
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. BAY-155 leads to a strong expression down-regulation of the MEIS1 gene and up-regulation of CD11b and MNDA genes. BAY-155 shows anti-proliferative effects in AML/ALL (acute myeloid/lymphoblastic leukemia) models .
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-
- HY-134050
-
|
Apt-1
|
RIP kinase
Autophagy
Apoptosis
Beclin1
Necroptosis
|
Inflammation/Immunology
|
|
Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin .
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-
- HY-151425
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), shows excellent selectivity over indoleamine-2,3-dioxygenase (IDO), with an IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo .
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-
- HY-B0072
-
-
- HY-148369
-
|
|
PROTACs
Deubiquitinase
Apoptosis
MDM-2/p53
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Cancer
|
|
U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells .
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- HY-W011303
-
-
- HY-W011303R
-
-
- HY-B0971
-
|
Prophenpyridamine maleate; Tripoton maleate; Pheniramine maleate
|
Histamine Receptor
Apoptosis
|
Inflammation/Immunology
Endocrinology
|
|
Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
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- HY-B0971A
-
|
Prophenpyridamine; Tripoton; Pheniramine solution
|
Histamine Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
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- HY-14543
-
-
| Cat. No. |
Product Name |
Type |
-
- HY-B1046
-
|
|
Chromogenic Assays
|
|
Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research .
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-
- HY-B1046R
-
|
|
Chromogenic Assays
|
|
Clofazimine (Standard) is the analytical standard of Clofazimine. This product is intended for research and analytical applications. Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC50 = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10415
-
|
hSA(408–423) peptide
|
CXCR
|
Infection
Inflammation/Immunology
Cancer
|
|
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
|
-
- HY-P5870
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
KTX-Sp2 is a potassium channel toxin. KTX-Sp2 effectively blocks three types of exogenous voltage-gated potassium channels: Kv1.1, Kv1.2 and Kv1.3. Ktx-Sp2 inhibits endogenous Kv1.3 and suppresses Ca 2+ signaling in Jurkat T cells. Ktx-Sp2 inhibits IL-2 secretion from activated Jurkat T cells .
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-
- HY-P3083
-
|
|
PKC
|
Inflammation/Immunology
|
|
N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor with an IC50 value of 75 μM. N-Myristoyl-Lys-Arg-Thr-Leu-Arg inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat .
|
-
- HY-P10838
-
|
|
PD-1/PD-L1
Apoptosis
|
Inflammation/Immunology
|
|
PL120131 is a PD-1/PD-L1 inhibitory peptide that can interfere with the interaction of PD-1/PD-L1 by binding to PD-1. PL120131 is capable of inhibiting the PD-1-mediated apoptotic signaling pathway, protecting Jurkat cells and primary lymphocytes from apoptosis. PL120131 aids in the antitumor activity of cytotoxic T lymphocytes (CTLs) .
|
-
- HY-P10815
-
|
|
Apoptosis
Calcium Channel
|
Others
|
|
IP3RCYT is an IP3R inhibitory peptide, which can inhibit the binding of cytochrome C to IP3R with an IC50 about 100 nM. IP3RCYT regulates calcium signaling within cells. P3RCYT inhibits apoptosis in HeLa and Jurkat cells treated with Staurosporine (HY-15141) or Membrane-bound Fas ligand (FasL) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99445
-
|
APG101; CAN008
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Asunercept (APG101; CAN008) is a soluble CD95-Fc fusion protein targeting CD95L. Asunercept disrupts CD95/CD95L signaling by selectively binding to CD95L. Asunercept can be used in the research of glioblastoma multiforme (GBM), myelodysplastic syndrome (MDS), and graft-versus-host disease (GvHD) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-19344S2
-
|
|
|
Lifitegrast-d4-1 is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
|
-
-
- HY-19344S1
-
|
|
|
Lifitegrast-d6 (SAR 1118-d6) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
|
-
-
- HY-19344S
-
|
|
|
Lifitegrast-d4 (SAR 1118-d4) is deuterium labeled Lifitegrast. Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM. Lifitegrast can be used for researching dry eye disease .
|
-
-
- HY-149773S
-
|
|
|
HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC50 of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity .
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-
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