Search Result
Results for "
THP1
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-131454
-
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STING
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Inflammation/Immunology
Cancer
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SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity [1].
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- HY-100688
-
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Dihydroorotate Dehydrogenase
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Cancer
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ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models [1] .
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- HY-104073
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-
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- HY-131454A
-
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STING
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Inflammation/Immunology
Cancer
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SR-717 free acid is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 free acid is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity [1].
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-
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- HY-156415
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-
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- HY-120048
-
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NBC19 is an NLRP3 inflammasome inhibitor with an IC50 of 60 nM in differentiated THP1 cells. NBC19 inhibits nigericin- and ATP-induced IL-1β release with IC50s of 80 nM and 850 nM, respectively [1].
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- HY-N12720
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Others
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Cancer
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Cynanoside J is a C21 steroidal glycosides that can be obtained from Cynanchum taihangense. The IC50 values of Cynanoside J for HL-60, THP1, and Caco2 are 6.38, 5.82, and 6.76 μM, respectively. Cynanoside J can be used in cancer research [1].
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- HY-123270
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-
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- HY-N12469
-
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Others
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Others
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Gypsogenin 3-O-glucuronide is a glucuronide that can be isolated from Gypsophila. Gypsogenin 3-O-glucuronide has cytotoxic effect on THP-1 cells [1].
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- HY-162658
-
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HDAC
Apoptosis
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Cancer
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Leuxinostat is an inhibitor for HDAC with IC50 of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models [1].
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- HY-N8390
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Others
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Cancer
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3-Epidehydropachymic acid, a lanostane triterpenoid, shows totoxicity effect against human acute monocytic leukemia cell line THP-1 (IC50=52.51 μM) [1].
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- HY-144168A
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STING
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Inflammation/Immunology
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STING agonist-8 dihydrochloride (compound 5-AB) is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells [1].
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-
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- HY-132221
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-
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- HY-167877
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p38 MAPK
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Inflammation/Immunology
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PS-166276 is a highly potent and less cytotoxic inhibitor of p38. PS166276 has an IC50 of 28 nM at p38 kinase and 170 nM in the THP-1 TNFα assay [1].
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- HY-N12186
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Others
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Inflammation/Immunology
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Sibiricine (Compound 8) is an isoquinoline alkaloid derived from the medicinal plant Corydalis crispa. Sibiricine has significant anti-inflammatory activity on TNF-α production by LPS-activated THP-1 cells [1].
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- HY-168554
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STING
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Inflammation/Immunology
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STING-IN-10 (P8) is a dual STING degrader and inhibitor with a DC50 value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity [1].
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- HY-144168
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STING
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Inflammation/Immunology
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STING agonist-8 is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells (WO2021239068A1, compound 5-AB) [1].
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- HY-157554
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- HY-162588
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- HY-148645
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STING
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Inflammation/Immunology
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STING modulator-4 (compound AIH05) is a competitive STING modulator with a Ki of 0.0933 μM for R232H STING. STING modulator-4 has an EC50 of >10 μM for p-IRF3 in THP-1 cell [1].
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- HY-122941
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Others
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Inflammation/Immunology
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Viscidulin II (FL6) is a flavone. Viscidulin II can be isolated from the root of Scutellaria baicalensis. Viscidulin II significantly suppresses P. acnes-induced IL-8 and IL-1β production in THP-1 cells [1].
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- HY-N8304
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(+)-Shegansu B; Parvifolol D
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Interleukin Related
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Inflammation/Immunology
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Shegansu B is an inhibitor of IL-1β. Shegansu B 6 inhibits IL-1β expression on LPS-induced THP-1 cells with 64.74% inhibition. Shegansu B has anti-inflammatory activity [1].
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- HY-122008
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Bacterial
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Infection
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Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) arginine is a broad-spectrum antistaphylococcal agent. Levonadifloxacin arginine has antimicrobial activity against methicillin-susceptible Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus and reduces phagocytosis of MRSA and MSSA strains by monocytic THP-1.
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- HY-15544
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CCR
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Inflammation/Immunology
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CCR1 antagonist 10 (example 1) is a potent and orally active CCR1 antagonist. CCR1 antagonist 10 inhibits 125I-MIP-1α binding to THP-1 cell membranes with an Ki value of 2.3 nM [1].
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- HY-158711
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STING
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Cancer
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STING agonist-38 (compound 58) is a potent agonist of STING, with the EC50 of 0.05 μM in THP1 cells. STING agonist-38 has certain oral bioactivity [1].
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- HY-145861
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Histone Demethylase
Apoptosis
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Cancer
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LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells [1].
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- HY-146581
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Cathepsin
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Inflammation/Immunology
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Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively [1].
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- HY-146580
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Cathepsin
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Inflammation/Immunology
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Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC50 values of 101.5 and 86.5 nM, respectively [1].
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- HY-108670
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P2X Receptor
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Inflammation/Immunology
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AZ11645373 is a highly selective and potent antagonist at human but not rat P2X7 receptors，AZ11645373 inhibits ATP-evoked IL-1β release from lipopolysaccharide-activated THP-1 cells , with an IC50 value of 90 nM [1].
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- HY-149816
-
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Interleukin Related
TNF Receptor
NF-κB
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Inflammation/Immunology
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Anti-inflammatory agent 41 (13a) significantly inhibit lipopolysaccharide (LPS)-induced expression of the proinflammatory cytokines IL-6 and TNF-α on J774A.1, THP-1 and LX-2 cells, and inhibits the activation of the NF-κB pathway [1].
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- HY-14926B
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(S)-(-)-Nadifloxacin arginine; WCK 771 arginine
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Bacterial
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Infection
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Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) arginine is a broad-spectrum antistaphylococcal agent. Levonadifloxacin arginine has antimicrobial activity against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus and reduces phagocytosis of MRSA and MSSA strains by monocytic THP-1 cells [1].
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- HY-14926A
-
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(S)-(-)-Nadifloxacin (arginine) hydrate; WCK-771A (arginine) hydrate
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Antibiotic
Bacterial
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Infection
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Levonadifloxacin (arginine) hydrate is a broad-spectrum anti-staphylococcal agent. Levonadifloxacin (arginine) hydrate shows antibacterial activity against Methicillin (HY-121544)-susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant S. aureus (MRSA) strains, with a reduction of which phagocytized in THP-1 monocytes [1].
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- HY-161671
-
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nAChR
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Neurological Disease
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GAT2711 (compound 3h) is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells and exhibits analgesic activity in α7 knockout mice [1].
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- HY-158379
-
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Parasite
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Infection
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Antiparasitic agent-22 (Compound 24) is a pan antiparasitic agent, that inhibits T. Brucei, L. infantum, L. tropica promastigotes (IC50 of 2.41, 5.95, 8.98 μM), L. infantum amastigotes (IC50 of 8.18 μM) and P. falciparum W2 strain (IC50 of 0.155 μM). Antiparasitic agent-22 exhibits low cytotoxicity against THP1, with CC50 of 64.16 μM [1].
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- HY-14926
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(S)-(-)-Nadifloxacin; WCK 771
|
Antibiotic
Bacterial
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Infection
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Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) is a broad-spectrum anti-staphylococcal agent. Levonadifloxacin shows antibacterial activity against Methicillin (HY-121544)-susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant S. aureus (MRSA) strains, with a reduction of which phagocytized in THP-1 monocytes [1].
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- HY-148606
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STING
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Cancer
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STING modulator-3 is a STING inhibitor. STING modulator-3 inhibits R232 STING with an Ki value of 43.1 nM in scintillation proximity assay. STING modulator-3 has no effect on IRF-3 activation or TNF-β induction in THP-1 cells [1].
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- HY-18739
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PMA; TPA; Phorbol myristate acetate
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PKC
SphK
NF-κB
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Inflammation/Immunology
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Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator [1] . Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells .
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- HY-149781
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STING
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Cancer
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STING agonist-34 (Compound 12L) is a potent STING agonist with an IC50 value of 1.15 μM and an EC50 of 0.38 μM in THP1 cells. STING agonist-34 could be used in cancer research [1].
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- HY-161687
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Src
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Cancer
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Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively [1].
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- HY-148643
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STING
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Inflammation/Immunology
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STING modulator-5 (compound 38) is a STING modulator with a pIC50 value of 9.5. STING modulator-5 antagonizes peripheral blood mononuclear cells (PBMC) with a pIC50 value of 8.1. STING modulator-5 is a antagonist of THP-1 cells, it can be used for immunological disease research [1].
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- HY-W080443
-
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Others
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Others
Cancer
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O-allylvanillin is O-allylchalcone derivative with anti-cancer effects [1]. O-allylvanillin inhibits THP-1, HL60, Hep-G2, MCF-7 cells growth with IC50 values of 74.76 μM, 63.52 μM, 90.99 μM, and 90.11 μM, respectively [1].
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- HY-161325
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Parasite
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Infection
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Antileishmanial agent-26 (Compound 69) is a guanidine-containing compound with anti-Leishmania donovani activity. Its IC50 value against Leishmania donovani is 5.67 μM, and its CC50 value against THP-1 is 3.79 μM. Antileishmanial agent-26 can be used in the research of tropical diseases [1].
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- HY-116926
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Antibiotic
Bacterial
DNA/RNA Synthesis
Topoisomerase
Apoptosis
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Infection
Cancer
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Deoxynybomycin is an antibiotic, that can be isolated from Streptomyces, and antibacterial activity against Staphylococcus aureus. Deoxynybomycin is the inhibitor for DNA gyrase and Topoisomerase I. Deoxynybomycin induces expression of p21/WAF1, exhibits cytotoxicity and induces apoptosis in cancer cells Saos-2, TMK-1, and THP-1 [1] .
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- HY-122623A
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Apoptosis
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Cancer
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DB818 dihydrochloride is the dihydrochloride salt form of DB818 (HY-122623). DB818 dihydrochloride is an inhibitor for Homeobox A9 (HOXA9). DB818 dihydrochloride reduces the formation of HOXA9-DNA complexes, inhibits the growth and induces apoptosis in AML cell lines OCI/AML3, MV4-11, and THP-1 [1].
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- HY-131945
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CU-115
2 Publications Verification
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells [1].
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- HY-147506
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs [1].
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- HY-155463
-
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NOD-like Receptor (NLR)
Interleukin Related
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Inflammation/Immunology
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NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM [1].
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- HY-P2036A
-
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Toll-like Receptor (TLR)
MMP
HSV
Antibiotic
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Infection
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FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection [1]. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells .
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-
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- HY-151132
-
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IsoQC-IN-1
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CD47
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Cancer
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Glutaminyl cyclases-IN-1 (IsoQC-IN-1) is a potent glutaminyl cyclases (QC) inhibitor with IC50 values of 12 nM and 73 nM for human QC and isoQC, respectively. Glutaminyl cyclases-IN-1 can selectively interfere with the interaction of CD47/SIRPα through isoQC inhibition, and enhances the increased phagocytic activity of both THP-1 and U937 macrophages [1].
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-
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- HY-155151
-
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RIP kinase
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Inflammation/Immunology
|
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RIPK2/3-IN-1 is a potent dual RIPK2/3 kinases inhibitor with IC50 values of 3 nM and 117 nM, respectively. RIPK2/3-IN-1 is against RIPK2 with IC50 value 14 nM in 14-TriLAN-Gly/NOD1 THP-1 cell-based NF-κB reporter assay [1].
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- HY-163280
-
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NAMPT
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Neurological Disease
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JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. JGB-1-155 counteracts the oxidative stress, through upregulating the NAD + in THP-1 human monocytes. JGB-1-155 attenuates TNFα-induced ROS in HT-22 cells [1].
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- HY-129340
-
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Acyltransferase
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Cardiovascular Disease
|
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AS-183 is an inhibitor of cholesterol acyltransferase (ACAT) (IC50=0.94 µM). AS-183 also inhibits the formation of cholesterol esters in HepG2, CaCo2 and THP-1 cells with IC50 values of 18.1, 25.5 and 34.5 µM, respectively. AS-183 can be used in the study of atherosclerosis and hypercholesterolemia [1].
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- HY-164765
-
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NLRP3-IN-56 (compound 062) is a NLRP3 inhibitor. NLRP3-IN-56 potently inhibits the level of IL-1β secretion by THP-1 cells with an IC50 of 9.7 nM. NLRP3-IN-56 can be used for the study of NLRP3-mediated symptoms and/or diseases [1].
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-
- HY-N7489
-
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Parasite
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Infection
Inflammation/Immunology
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β-Hederin, a saponin isolated from Hedera helix L.(Araliaceae), possesses antileishmanial activity. β-Hederin exhibits IC50 values of 1.5 μM, 68 nM and 4.57 μM in L. Mexicana promastigotes, L. mexicana amastigotes and THP1 cells, respectively [1] .
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- HY-146283
-
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Histone Demethylase
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Cancer
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LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively [1].
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- HY-146284
-
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Histone Demethylase
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Cancer
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LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively [1].
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- HY-135453
-
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Bacterial
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Infection
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(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines [1].
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- HY-159718
-
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NOD-like Receptor (NLR)
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Inflammation/Immunology
|
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NLRP3-IN-46 (Compound 3k) activates neuro-immunomodulatory cholinergic anti-inflammatory pathway, and thus inhibits NLRP3 inflammasome activation. NLRP3-IN-46 inhibits Uric acid sodium (HY-B2130A)-induced IL-1β production in THP-1 cells, and can be used in gouty arthritis research [1].
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- HY-146285
-
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Histone Demethylase
Histone Methyltransferase
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Cancer
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LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively [1].
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- HY-123942
-
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Toll-like Receptor (TLR)
TNF Receptor
p38 MAPK
NF-κB
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Inflammation/Immunology
Cancer
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Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses [1] .
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- HY-162647
-
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PI3K
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Inflammation/Immunology
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PI3Kδ-IN-22 (Compound 26) is a selective inhibitor for PI3Kδ with pKi of 9.3. PI3Kδ-IN-22 inhibits PI3Kδ-AKT signaling pathway in THP-1 cells, with pIC50 of 9.4. PI3Kδ-IN-22 exhibits good pharmacokinetic characters in rats [1].
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- HY-130481
-
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PROTAC Linkers
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Cancer
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Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells [1]. Propargyl-PEG4-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-131040
-
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NOD-like Receptor (NLR)
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Inflammation/Immunology
|
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NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor (IC50= 574 nM) that acts independently of Ca 2+. NLRP3-IN-NBC6 inhibits Nigericin (HY-127019)-induced inflammasome activation in THP-1 cells and Imiquimod (HY-B0180)-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].
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- HY-153673
-
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IRAK
PROTACs
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Cancer
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PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively [1].
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- HY-155245
-
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CDK
Bcl-2 Family
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Cancer
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A09-003 is a CDK-9 inhibitor (IC50: 16 nM). A09-003 inhibits leukemia cell proliferation (IC50: 1.90, 0.86, 2.49, 1.84, 0.48 μM for BDCM, Molm-14, THP-1, U937, MV4-11 cells). A09-003 induces apoptosis and decreases Mcl-1 expression through Thr163 dephosphorylation [1].
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- HY-162122
-
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PPAR
|
Inflammation/Immunology
|
|
PPARα/γ agonist 3 (Compound 4) is a dual agonist of PPARα/γ. PPARα/γ agonist 3 has anti-inflammatory activity, significantly reducing inflammatory markers such as IL-6 and MCP-1 on THP-1 macrophages through NF-κB activation. PPARα/γ agonist 3 can be used in the study of metabolic syndrome and metabolic dysfunction-related fatty liver disease (MAFLD) [1].
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- HY-N3887
-
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Haplophytin B; Haplophytine B
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Others
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Infection
|
|
Evoxine (Haplophytin B) is a compound that selectively inhibits CO2-induced immunosuppression and has activity in inhibiting the expression of interleukin-6 and chemokine CCL2 in human THP-1 macrophages. Evoxine shows antimicrobial activity against a wide range of bacteria, especially performing well in minimum inhibitory concentration (MIC) tests against Escherichia coli, Bacillus subtilis, and Staphylococcus aureus. Evoxine extracts may find application in crude drug preparations in West Africa, provided that their in vivo toxicity results are negative [1].
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- HY-156622
-
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HMC-C-01-A; MBS2320
|
Mitochondrial Metabolism
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Cancer
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Leramistat (HMC-C-01-A; MBS2320) is a mitochondrial complex 1 inhibitor, involving in cell metabolism immune metabolism regulation. Leramistat also inhibits ATP production in Thp1 human monocytes (IC50: 0.63 μM). Leramistat inhibits atopic dermatitis and other skin diseases autoimmune diseases, inflammatory diseases, cancer; and also inhibits osteoclast mediated disease [1] .
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-
- HY-127102
-
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DDD01305143
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Parasite
Proteasome
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Infection
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GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties [1] .
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- HY-158434
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IRAK
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Inflammation/Immunology
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IRAK1-IN-1 (compound B8) is an orally active IRAK1 inhibitor. IRAK1-IN-1 inhibits the release of IL-6 with the IC50 values of 4.57 μM and 6.51 μM on mouse cells J774A. 1 and human cells THP-1, respectively. IRAK1-IN-1 alleviats LPS (HY-D1056)-induced acute lung injury (ALI) and DSS(HY-116282C)-induced colitis in mice [1].
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- HY-144226
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NOD-like Receptor (NLR)
AIM2
Pyroptosis
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Inflammation/Immunology
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NLRP3/AIM2-IN-3 (compound 59) is a potent inhibitor with differential species specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. NLRP3/AIM2-IN-3 shows inhibitory efficacy against pyroptosis in THP-1 macrophages stimulated with LPS/nigericin, with an IC50 of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disturbs the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization [1].
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- HY-168089
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NLRP3-IN-49 (compound Z48) is a potent and specific NLRP3 inhibitor (IC50=0.26 μM in THP-1 cells, IC50=0.21 μM in mouse bone marrow macrophages). NLRP3-IN-49 can directly bind to NLRP3 protein (Kd=1.05 μM), effectively preventing the assembly and activation of NLRP3 inflammasome, thereby exhibiting anti-inflammatory properties. NLRP3-IN-49 can be used in the study of inflammatory bowel disease [1].
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- HY-162874
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STING
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Inflammation/Immunology
Cancer
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diABZI-V/C-DBCO (Compound 3) is a potent STING agonist. diABZI-V/C-DBCO can release diABZI-amine upon activation by cathepsin B to activate STING, leading to the production of interferons and other immune-stimulatory molecules, thereby enhancing the immune system's response to tumors. The EC50 values for diABZI-V/C-DBCO and diABZI-amine in activating STING in THP1-Dual cells are 1.47 and 0.144 nM, respectively, and in primary mouse splenocytes, the EC50 values are 7.7 and 0.17 μM, respectively. diABZI-V/C-DBCO can be used in cancer immunotherapy research [1].
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- HY-100401A
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CS-505
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Acyltransferase
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Cardiovascular Disease
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Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively [1]. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
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- HY-100401
-
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CS-505 free base
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Acyltransferase
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Cardiovascular Disease
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Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively [1]. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
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- HY-159719
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NF-κB
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Inflammation/Immunology
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NLRP3-IN-51 (Compound 3q) is a potent cholinergic anti-inflammatory pathway (CAP) activators. ANLRP3-IN-51 inhibits Monosodium urate (MSU) (HY-B2130A)-induced IL-1β production in THP-1 cells, indicating its potential against gout arthritis. NLRP3-IN-51 inhibits MSU induced phosphorylation of NF-κB p65, without any inhibitory effect against NLRP3, pro-caspase 1, or the self-cleavage and activation of caspase-1 of the second signaling. Therefore, NLRP3-IN-51 inhibits the initial phase of NLRP3 through CAP activation [1].
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- HY-149522
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Bcl-2 Family
Apoptosis
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Cancer
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BCL6-IN-10 (Compound WK499) is a BCL6 inhibitor. BCL6-IN-10 interrupts the binding of BCL6 to SMRT protein. BCL6-IN-10 induces cell apoptosis, cell cycle arrest and DNA damage. BCL6-IN-10 inhibits AML cell proliferation (IC50s: 0.91, 1.63, 1.026, 7.42, 0.87, 0.85μM for OCl-AML3, THP1, MOLM13, HL60, KG1, NB4 cell respectively) [1].
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- HY-162772
-
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Isocitrate Dehydrogenase (IDH)
Apoptosis
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Cancer
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IDH1/2-IN-1 (Compound 6b) serves as a dual inhibitor of IDH1(R132H)/IDH2(R140Q) with IC50 values of 0.22 μM and 1.6 μM, respectively. IDH1/2-IN-1 effectively inhibits tumor growth by suppressing tumor cell proliferation and enhancing host defense through the activation of antioxidant enzymes. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis, demonstrating robust antitumor activity. IDH1/2-IN-1 holds potential for research in leukemia [1].
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- HY-137320
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STING
|
Cancer
|
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diABZI-C2-NH2, an active analogue containing a primary amine functionality, is a STING agonist [1].
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- HY-W327122
-
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Others
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Cancer
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BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM [1].
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- HY-160944
-
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Sirtuin
|
Cancer
|
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hsa62 is a dual inhibitor for SIRT1 and SIRT2, with IC50 of 1.3 and 5.5 μM, respectively [1].
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- HY-163707
-
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Apoptosis
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Cancer
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UR778Br targets the GTPase-activating protein-related domain (GRD domain) of IQGAP1 proteins. UR778Br inhibits the proliferation of human acute myeloid leukemia (AML), arrests the cell cycle at the G2/M phase, and induces apoptosis. UR778Br inhibits colony formation of primary and AML cells, without significant impacts on normal bone marrow cells [1].
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- HY-151560
-
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Dihydroorotate Dehydrogenase
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Cancer
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hDHODH-IN-11 is a potent human dihydroorotate dehydrogenase (hDHODH) inhibitor with an IC50 value of 7.2 nM. hDHODH-IN-11 has low cytotoxicity. hDHODH-IN-11 can be used in research of acute myeloid leukemia (AML) [1].
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- HY-128583
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G150
4 Publications Verification
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Cyclic GMP-AMP Synthase
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Inflammation/Immunology
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G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory [1].
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- HY-136351
-
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Autophagy
|
Cancer
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THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines [1].
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- HY-150025
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DNA Methyltransferase
Apoptosis
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Cancer
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(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882 [1].
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- HY-136241
-
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NAMPT
Caspase
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Cancer
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OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD + dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies [1].
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2036A
-
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Toll-like Receptor (TLR)
MMP
HSV
Antibiotic
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Infection
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FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection [1]. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
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Classification |
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- HY-130481
-
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PROTAC Synthesis
Alkynes
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Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells [1]. Propargyl-PEG4-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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