Search Result
Results for "ActivatedCD8+ T Cell Inhibitors" in MCE Product Catalog:
9700
Inhibitors & Agonists
30
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-131140
-
BD750
|
JAK
STAT
|
Cancer
Inflammation/Immunology
|
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
|
-
- HY-136498
-
T-705RMP
|
Drug Metabolite
|
Infection
|
T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC50 of 601 μM.
|
-
- HY-19352
-
-
- HY-125930
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T-2513
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
|
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- HY-13624A
-
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13624
-
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P2251
-
T-peptide
|
Microtubule/Tubulin
|
|
T-peptide is a peptide derived from microtubule binding repeat of Tau protein. T-peptide self-assembles into 30-55 nm paired helical filaments (PHFs) even in the absense of inducers. T-peptide is cytotoxic in multiple cell lines including cortical neurons, cerebellar granular neurons, neuroblastoma cells, kidney fibroblasts and HEK293 cells. T-peptide co-localizes with pathological hyperphosphorylated forms of tau in vitro.
|
-
- HY-120356A
-
T-1101 tosylate
TAI-95 tosylate
|
Apoptosis
|
Cancer
|
T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG
|
-
- HY-12072
-
Lck Inhibitor
|
Src
|
Inflammation/Immunology
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-N6792
-
T-2 Toxin
T-2 Mycotoxin
|
Apoptosis
DNA/RNA Synthesis
|
Metabolic Disease
|
T-2 Toxin (T-2 Mycotoxin) is a toxic trichothecene mycotoxin produced by various Fusarium species in feedstuffs and cereal grains, LD50 values of T-2 Toxin in mice and rats are 5.2 and 1.5 mg/kg BW a,respectively . T-2 Toxin (T-2 Mycotoxin) can be transformed into a variety of metabolite, the typical metabolites of T-2 toxin in animals are HT-2 toxin and T-2-triol, which are hydrolysates. T-2 Toxin (T-2 Mycotoxin) is an inhibitor of protein synthesis resulting from binding peptidyltransferase, which is an integral part of the 60s ribosomal subunit. T-2 Toxin (T-2 Mycotoxin) inhibits the synthesis of DNA and RNA, interferes with the metabolism of membrane phospholipids, and increases the level of liver lipid peroxides. T-2 Toxin (T-2 Mycotoxin) induces apoptosis in the immune system, gastrointestinal tissues, and fetal tissues.
|
-
- HY-U00439
-
-
- HY-32219
-
T863
|
Acyltransferase
|
Metabolic Disease
|
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells.
|
-
- HY-W015764
-
T-1105
|
Influenza Virus
|
Infection
|
T-1105, a novel broad-spectrum viral polymerase inhibitor, structural analogue of T-705, inhibits the polymerases of RNA viruses after being converted to ribonucleoside triphosphate (RTP) metabolite. T-1105 has antiviral activity against various RNA viruses, including Zika virus (ZIKV), influenza virus, arenaviruses, bunyaviruses, West Nile virus (WNV), yellow fever virus (YFV), and foot-and-mouth disease virus (FMDV). T-1105 can be formed by nicotinamide mononucleotide adenylyltransferase.
|
-
- HY-P1404
-
R8-T198wt
|
Pim
|
Cancer
|
R8-T198wt is a cell-permeable carboxyl-terminal p27 Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase.
|
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- HY-102045
-
-
- HY-125832
-
PBDB-T
|
Others
|
Others
|
PBDB-T is a wide bandgap polymer donor in Perylene diimide (PDI)-based polymer solar cells (PSCs).
|
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- HY-103085
-
-
- HY-122635A
-
T-448
|
Histone Demethylase
|
Neurological Disease
|
T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
|
-
- HY-135791
-
-
- HY-135803
-
T-705RTP
|
DNA/RNA Synthesis
Influenza Virus
SARS-CoV
|
Infection
|
T-705RTP is a selective and GTP-competitive influenza virus RNA polymerase inhibitor with an IC50 of 0.14 μM and a Ki of 1.52 μM. T-705RTP is the active triphosphate metabolite of T-705 and has potent anti-influenza virus activity.
|
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- HY-12270
-
T-5224
|
MMP
|
Others
|
T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
|
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- HY-134771
-
YM-341619
AS1617612
|
STAT
|
Inflammation/Immunology
|
YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC50 of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 (IC50=0.28 nM) without affecting Th1 cell differentiation. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma.
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- HY-18522
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AA26-9
|
Phospholipase
|
Metabolic Disease
|
AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
|
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- HY-129055
-
Isoeleutherin
|
Fungal
|
Inflammation/Immunology
|
Isoeleutherin is a naphthopyran derivative isolated from E. americana Merr. Et Heyne with anti-fungal, anti-viral, and anti-tumor activities. Isoeleutherin plays an important role in selective modulation of T helper cell-mediated immune responses.
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- HY-U00028
-
-
- HY-102011
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BMS-1166
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-109520
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Glatiramer acetate
|
Others
|
Inflammation/Immunology
|
Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression.
|
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- HY-13563
-
Batabulin
T138067
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.
|
-
- HY-13563A
-
Batabulin sodium
T138067 sodium
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Batabulin sodium (T138067 sodium) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin sodium affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.
|
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- HY-18676
-
OSU-T315
|
Integrin
Autophagy
Apoptosis
|
Cancer
|
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
|
-
- HY-110177
-
SP-100030
|
NF-κB
|
Inflammation/Immunology
|
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-N6720
-
T-2 Triol
|
Endogenous Metabolite
|
Metabolic Disease
|
T-2 Triol is a trichothecene mycotoxin derived by the metabolism of T-2 toxin. It is less toxic than T-2 toxin. T-2 Triol major metabolites are evaluated in broiler chickens with Half-lives (t1/2λz), Peak plasma concentrations (Cmax) and Tmax values of 9.6 mins, 563 ng/ml , 2.5 mins, respectively.
|
-
- HY-10626
-
T0901317
|
LXR
FXR
ROR
Apoptosis
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
|
-
- HY-N6721
-
T-2 Tetraol
|
Others
|
Infection
|
T-2 Tetraol is a metabolite of T-2 toxin, and also a trichothecene mycotoxin, with less toxicity and is unable to induce apoptosis.
|
-
- HY-16906
-
T338C Src-IN-2
|
Src
|
Cancer
|
T338C Src-IN-2 is a potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM; also inhibits T338C/V323A and T338C/V323S with IC50 of 57 nM/19 nM.
|
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- HY-14925
-
-
- HY-B0959
-
-
- HY-B0724B
-
-
- HY-122635
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T-448 free base
|
Histone Demethylase
|
Neurological Disease
|
T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
|
-
- HY-108313
-
T-00127_HEV1
|
PI4K
|
Infection
|
T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM.
|
-
- HY-P0052
-
-
- HY-14768
-
Favipiravir
T-705
|
DNA/RNA Synthesis
Influenza Virus
SARS-CoV
|
Infection
|
Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
|
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- HY-135956
-
-
- HY-19744
-
T6167923
|
MyD88
|
Inflammation/Immunology
|
T6167923 is a potent and selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with an 50 of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
|
-
- HY-121638
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CU-3
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
|
-
- HY-100518
-
T-26c
|
MMP
|
Inflammation/Immunology
|
T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes.
|
-
- HY-16905
-
T338C Src-IN-1
|
Src
|
Cancer
|
T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
|
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- HY-111595
-
-
- HY-P1115
-
AKTide-2T
|
Akt
|
Others
|
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
|
-
- HY-113962
-
7α,25-Dihydroxycholesterol
7α,25-OHC
|
EBI2/GPR183
Endogenous Metabolite
|
Inflammation/Immunology
|
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.
|
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- HY-P0272
-
Peptide T
|
HIV
|
Infection
|
Peptide T is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
|
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- HY-114272A
-
-
- HY-114271A
-
-
- HY-13202
-
-
- HY-103033
-
T.cruzi-IN-1
|
Parasite
|
Infection
|
T.cruzi-IN-1 is a potent Trypanosoma cruzi inhibitor with an IC50 of 8 nM. T.cruzi-IN-1, a 4-trifluoromethyl substituted analog, has the potential for both the acute and chronic stages of Chagas disease.
|
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- HY-140414
-
-
- HY-18341
-
-
- HY-101458
-
-
- HY-101458A
-
-
- HY-P1115A
-
AKTide-2T TFA
|
Akt
|
Others
|
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
|
-
- HY-P0052A
-
-
- HY-P0272A
-
Peptide T TFA
|
HIV
|
Infection
|
Peptide T (TFA) is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
|
-
- HY-17002
-
Suplatast (Tosilate)
IPD 1151T
|
Interleukin Related
|
Inflammation/Immunology
|
Suplatast Tosilate (IPD 1151T) is an orally active Th2 cytokine inhibitor which can inhibit both IL-4 and IL-5 production from Th2 cells and suppress IgE synthesis. Suplatast Tosilate is an anti-allergic agent. Suplatast Tosilate has antiasthmatic, anti-inflammatory and antifibrotic activity.
|
-
- HY-115470
-
CLK-IN-T3
|
CDK
DYRK
|
Cancer
|
CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity.
|
-
- HY-100612
-
T16Ainh-A01
|
Chloride Channel
|
Others
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
|
-
- HY-18341B
-
L-Thyroxine sodium
Levothyroxine sodium; T4 sodium
|
Thyroid Hormone Receptor
|
Endocrinology
|
L-Thyroxine sodium (Levothyroxine sodium) is a synthetic hormone for the research of hypothyroidism. DIO enzymes convert biologically active thyroid hormone (Triiodothyronine,T3) from L-Thyroxine (T4).
|
-
- HY-131183
-
PROTAC PD-1/PD-L1 degrader-1
|
PROTAC
PD-1/PD-L1
|
Inflammation/Immunology
|
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 degrader, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
|
-
- HY-112296
-
T025
|
CDK
|
Cancer
|
T025 is an orally available and highly potent Cdc2-like kinase (CLK) inhibitor with Kds of 4.8, 0.096, 6.5, and 0.61 nM for CLK1, CLK2, CLK3, and CLK4, respectively.
|
-
- HY-B0724A
-
-
- HY-13821
-
Epoxomicin
BU-4061T
|
Proteasome
Apoptosis
|
Cancer
Inflammation/Immunology
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
|
-
- HY-18676B
-
-
- HY-110353
-
CU-T12-9
|
Toll-like Receptor (TLR)
|
Cancer
Infection
Inflammation/Immunology
|
CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
|
-
- HY-130676
-
CLK-IN-T3N
|
CDK
|
Cancer
|
CLK-IN-T3N, the negative control of CLK-IN-T3 (HY-115470), is a chemical probe for CDC-like kinase (CLK).
|
-
- HY-N4010
-
Iriflophenone
|
Others
|
Cancer
|
Iriflophenone, isolated from Aquilaria sinensis, stimulates MCF-7 and T-47D human breast cancer cells proliferation.
|
-
- HY-101184
-
-
- HY-129624A
-
Bisindolylmaleimide VIII acetate
Ro 31-7549 acetate; Bis VIII acetate
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
|
-
- HY-101467A
-
Trilaciclib hydrochloride
G1T28 hydrochloride
|
CDK
|
Cancer
|
Trilaciclib hydrochloride (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
|
-
- HY-113924
-
-
- HY-113974
-
trans-AUCB
t-AUCB
|
Epoxide Hydrolase
|
Cancer
|
trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.
|
-
- HY-B0116
-
-
- HY-B0116A
-
-
- HY-136427
-
KRM-III
|
Others
|
Inflammation/Immunology
|
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
|
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- HY-132088
-
-
- HY-112272
-
Lerociclib
G1T38
|
CDK
|
Cancer
|
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
|
-
- HY-115463
-
EB-3D
|
AMPK
Apoptosis
|
Cancer
|
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
|
-
- HY-N4053
-
Heraclenin
|
Others
|
Inflammation/Immunology
|
Heraclenin, a natural furanocoumarin, isolated from the root parts of the plant Prangos pabularia. Heraclenin significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
|
-
- HY-115400
-
1V209
TLR7 agonist T7
|
Toll-like Receptor (TLR)
|
Cancer
|
1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.
|
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- HY-132117
-
-
- HY-132067
-
-
- HY-132022
-
-
- HY-132066
-
-
- HY-132056
-
-
- HY-W096076
-
-
- HY-132118
-
-
- HY-132057
-
-
- HY-132062
-
-
- HY-132034
-
-
- HY-132081
-
-
- HY-132044
-
-
- HY-132071
-
-
- HY-140783
-
-
- HY-132100
-
-
- HY-132061
-
-
- HY-140386
-
-
- HY-132054
-
-
- HY-140384
-
-
- HY-132060
-
-
- HY-132079
-
-
- HY-132080
-
-
- HY-132084
-
-
- HY-132064
-
-
- HY-132101
-
-
- HY-132025
-
-
- HY-112272A
-
Lerociclib dihydrochloride
G1T38 dihydrochloride
|
CDK
|
Cancer
|
Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
|
-
- HY-112823
-
Almonertinib
HS-10296
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
|
-
- HY-112823B
-
Almonertinib hydrochloride
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
|
-
- HY-122716
-
PTGR2-IN-1
|
Others
|
Others
|
PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.
|
-
- HY-119339
-
SX-682
|
CXCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
|
-
- HY-131005
-
-
- HY-135103
-
Tauro-β-muricholic acid sodium
T-βMCA sodium
|
FXR
|
Cancer
|
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
|
-
- HY-19617A
-
EGFR-IN-1 hydrochloride
|
EGFR
|
Cancer
|
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
|
-
- HY-106199
-
-
- HY-129974
-
-
- HY-N6626
-
-
- HY-140434
-
-
- HY-140054
-
-
- HY-140436
-
-
- HY-140417
-
-
- HY-132089
-
-
- HY-140429
-
-
- HY-140419
-
-
- HY-140424
-
-
- HY-140431
-
-
- HY-140422
-
-
- HY-140437
-
-
- HY-140418
-
-
- HY-140378
-
-
- HY-19617B
-
EGFR-IN-1 TFA
|
EGFR
|
Cancer
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
|
-
- HY-19617
-
EGFR-IN-1
|
EGFR
|
Cancer
|
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
|
-
- HY-18959
-
CWP232228
|
β-catenin
Wnt
|
Cancer
|
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
|
-
- HY-W096165
-
-
- HY-140405
-
-
- HY-140753
-
-
- HY-130254
-
Src Inhibitor 3
|
Src
|
Cancer
Inflammation/Immunology
|
Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling.
|
-
- HY-114170
-
ML604440
|
Proteasome
|
Inflammation/Immunology
|
ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
|
-
- HY-N6729
-
HT-2 Toxin
|
Others
|
Metabolic Disease
|
HT-2 Toxin is an active, deacetylated metabolite of the T-2 toxin. HT-2 toxin inhibits protein synthesis and cell proliferation in plants.
|
-
- HY-79256
-
MMAF-OMe
Monomethyl auristatin F methyl ester
|
ADC Cytotoxin
|
Cancer
|
MMAF-Ome, an antitubulin agent, belongs to ADC. MMAF-Ome inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4 -) cell lines, respectively.
|
-
- HY-15405
-
Teriflunomide
A77 1726
|
Others
|
Inflammation/Immunology
|
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
|
-
- HY-140874
-
-
- HY-130422
-
Tos-PEG4-t-butyl ester
Tos-PEG4-Boc
|
PROTAC Linker
|
Cancer
|
Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker, which refers to the PEG composition. Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) can be used in the synthesis of a series of PROTACs, such as BI-3663 (HY-111546). BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation, and inhibits PTK2 with an IC50 of 18 nM.
|
-
- HY-129492
-
GNF4877
|
DYRK
GSK-3
|
Metabolic Disease
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
|
-
- HY-136895
-
AZ12672857
|
Prostaglandin Receptor
|
Cancer
|
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).
|
-
- HY-N4119
-
Neoeriocitrin
|
AChE
|
Neurological Disease
|
Neoeriocitrin, isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor.
|
-
- HY-135813
-
LtaS-IN-1
|
Bacterial
|
Infection
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- HY-W096080
-
-
- HY-140592
-
-
- HY-W096082
-
-
- HY-111446
-
-
- HY-140584
-
-
- HY-100891
-
-
- HY-121879
-
-
- HY-102022
-
α-Galactosylceramide
α-GalCer; KRN7000
|
Others
|
Cancer
Inflammation/Immunology
|
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).
|
-
- HY-100894
-
Biotin-VAD-FMK
|
Caspase
|
Cancer
|
Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.
|
-
- HY-112125A
-
-
- HY-130608
-
Mutated EGFR-IN-3
|
EGFR
|
Cancer
|
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
|
-
- HY-106934
-
Peldesine
BCX 34
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-106934A
-
Peldesine dihydrochloride
BCX 34 dihydrochloride
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-12461
-
WS6
|
Others
|
Inflammation/Immunology
|
WS6 is a novel small molecule that promotes β cell proliferation in rodent and human primary islets with EC50 of 0.28 uM(R7T1 cell viability).
|
-
- HY-100429
-
CAN508
|
CDK
|
Cancer
|
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
|
-
- HY-16558
-
Butein
2’,3,4,4’-tetrahydroxy Chalcone
|
EGFR
Autophagy
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
Butein, isolated from Dalbergia odorifera T. Chen, is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
|
-
- HY-U00439A
-
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-N7634
-
Tectol
|
Farnesyl Transferase
Parasite
|
Cancer
Infection
|
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM.
|
-
- HY-125957
-
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-129767
-
CMLD012612
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity.
|
-
- HY-N4171
-
Dihydrocucurbitacin B
|
Others
|
Inflammation/Immunology
|
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity.
|
-
- HY-136522
-
S2116
|
Histone Demethylase
Apoptosis
|
Cancer
|
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
|
-
- HY-136523
-
S2157
|
Histone Demethylase
Apoptosis
|
Cancer
|
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
|
-
- HY-140999
-
-
- HY-129769
-
CMLD012073
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
CMLD012073 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012073 inhibits the growth of NIH/3T3 cells with an IC50 of 10 nM. CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A).
|
-
- HY-140564
-
-
- HY-140928
-
-
- HY-140921
-
-
- HY-140094
-
-
- HY-15707
-
-
- HY-12972
-
Mavelertinib
PF-06747775
|
EGFR
|
Cancer
|
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
|
-
- HY-N1506
-
Ganodermanontriol
|
Others
|
Cancer
|
Ganodermanontriol, a sterol isolated from Ganoderma lucidum, induces anti-inflammatory activity in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells through the expression of HO-1. Ganodermanontriol exhibits hepatoprotective activity.
|
-
- HY-12521
-
GSK-5498A
|
CRAC Channel
|
Inflammation/Immunology
|
GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
|
-
- HY-128726
-
-
- HY-18337
-
-
- HY-15440
-
Temsavir
BMS-626529
|
HIV
|
Infection
|
Temsavir (BMS-626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
|
-
- HY-140873
-
-
- HY-140870
-
-
- HY-19373
-
-
- HY-140092
-
-
- HY-125881
-
ASP1126
|
LPL Receptor
|
Inflammation/Immunology
|
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile.
|
-
- HY-113618A
-
RO2959 hydrochloride
|
CRAC Channel
Interleukin Related
|
Cardiovascular Disease
|
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
|
-
- HY-17631A
-
-
- HY-14622
-
Necrostatin 2
|
RIP kinase
|
Cancer
|
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.
|
-
- HY-18667
-
-
- HY-109108
-
-
- HY-100365
-
Remetinostat
SHP-141
|
HDAC
|
Cancer
|
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma.
|
-
- HY-114388
-
QM385
|
Others
|
Inflammation/Immunology
|
QM385 is a potent sepiapterin reductase (SPR) inhibitor with an IC50 of 1.49 nM, which blocks T-cell proliferation and autoimmunity at nanomolar potency and with good oral bioavailability.
|
-
- HY-113618B
-
RO2959 monohydrochloride
|
CRAC Channel
Interleukin Related
|
Cardiovascular Disease
|
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
|
-
- HY-N6734
-
K-252b
|
PKC
|
Infection
|
K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely .
|
-
- HY-15898
-
-
- HY-109108A
-
-
- HY-112816
-
MA242
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy.
|
-
- HY-112514
-
1,3,6,8-Tetrahydroxynaphthalene
1,3,6,8-THN; T4HN
|
Others
|
Others
|
1,3,6,8-Tetrahydroxynaphthalene (T4HN) is an indispensable precursor to DHN (1,8-Dihydroxynaphthalene) melanin and is an unique symmetrical compound of polyketide origin.
|
-
- HY-128971
-
LHVS
|
Cathepsin
Parasite
|
Infection
|
LHVS is a potent, non-selective cysteine protease inhibitor. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion.
|
-
- HY-124416
-
ML604086
|
CCR
|
Inflammation/Immunology
Endocrinology
|
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations.
|
-
- HY-14171
-
Bexarotene
LGD1069
|
RAR/RXR
Autophagy
|
Cancer
|
Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
|
-
- HY-19344
-
Lifitegrast
SAR 1118; SHP-606
|
Integrin
|
Inflammation/Immunology
|
Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
|
-
- HY-136583
-
28-Epirapamycin
|
Others
|
Others
|
28-Epirapamycin is an impurity of Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells.
|
-
- HY-W012037
-
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-124617A
-
AMXT-1501 tetrahydrochloride
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines.
|
-
- HY-50730
-
Asparagusic acid
|
Parasite
|
Infection
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-W008859
-
Tetrac
Tetraiodothyroacetic acid; 3,3',5,5'-Tetraiodothyroacetic acid
|
Integrin
Endogenous Metabolite
|
Cancer
|
Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities.
|
-
- HY-123159
-
AKI603
|
Aurora Kinase
|
Cancer
|
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
|
-
- HY-115292
-
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-19713
-
LJI308
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation.
|
-
- HY-137497
-
KRAS inhibitor-9
|
Ras
Apoptosis
|
Cancer
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-19985
-
-
- HY-17009
-
Iguratimod
T614
|
COX
|
Inflammation/Immunology
|
Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.
|
-
- HY-136110
-
-
- HY-108317
-
ABL127
|
Others
|
Cancer
|
ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
|
-
- HY-N6681
-
-
- HY-118047
-
-
- HY-112125
-
KRN2
|
Others
|
Inflammation/Immunology
|
KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis.
|
-
- HY-B2145
-
Ilaprazole sodium
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-126675A
-
AS2863619
|
CDK
STAT
|
Inflammation/Immunology
|
AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
|
-
- HY-126250
-
NPD-1335
|
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
|
NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death.
|
-
- HY-B0190A
-
-
- HY-B0190
-
-
- HY-B0190B
-
-
- HY-B1156
-
Cephradine
Cefradine; SQ-11436
|
Bacterial
TOPK
Antibiotic
|
Infection
|
Cephradine (Cefradine) is the first-generation broad-spectrum cephalosporin antibiotic, which also acts as an inhibitor of TOPK (T-LAK cell-originated protein kinase) and suppresses skin inflammation induced by excessive solar ultraviolet.
|
-
- HY-11011
-
A-770041
|
Src
|
Inflammation/Immunology
|
A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
|
-
- HY-101664
-
Ilaprazole
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-50722
-
NNC 55-0396
NNC 55-0396 dihydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.
|
-
- HY-15440A
-
Fostemsavir
BMS-663068
|
HIV
|
Infection
|
Fostemsavir (BMS-663068) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir (BMS-663068) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
|
-
- HY-N7119
-
Cimicifugoside
|
Others
|
Inflammation/Immunology
|
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity. Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function.
|
-
- HY-126675
-
AS2863619 free base
|
CDK
STAT
|
Inflammation/Immunology
|
AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
|
-
- HY-113965
-
CUR61414
|
Hedgehog
Smo
Apoptosis
|
Inflammation/Immunology
|
CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells.
|
-
- HY-N4058
-
Helichrysetin
|
Apoptosis
|
Cancer
|
Helichrysetin, isolated from the flowers of Helichrysum odoratissimum, is an ID2 (inhibitor of DNA binding 2) inhibitor, and suppresses DCIS (ductal carcinoma in situ) formation. Helichrysetin possess strong inhibitory effects on cell growth and is capable of inducing apoptosis in A549 cells.
|
-
- HY-17561
-
G-418 disulfate
Geneticin sulfate; Antibiotic G-418 sulfate
|
Bacterial
Antibiotic
|
Infection
|
G-418 disulfate (Geneticin sulfate), is an aminoglycoside antibiotic, inhibits protein synthesis in eukaryotes and prokaryotes. G-418 disulfate is commonly used as a selective agent for eukaryotic cells.
|
-
- HY-16023A
-
Acolbifene
EM-652; SCH 57068
|
Estrogen Receptor/ERR
|
Cancer
|
Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist with an IC50 of of 0.110 nM in T-47D cells. Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties.
|
-
- HY-16023
-
Acolbifene hydrochloride
EM-652 hydrochloride; SCH 57068 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
Acolbifene (EM-652) hydrochloride, the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist with an IC50 of of 0.110 nM in T-47D cells. Acolbifene (EM-652) hydrochloride possesses potent and pure anticarcinogenic properties.
|
-
- HY-131344
-
mTOR inhibitor-8
|
mTOR
Autophagy
|
Cancer
|
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
|
-
- HY-101918
-
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-138072
-
EMI1
|
EGFR
|
Cancer
|
EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC).
|
-
- HY-108742A
-
Abaloparatide TFA
BA 058 TFA; BIM 44058 TFA
|
Thyroid Hormone Receptor
|
Metabolic Disease
Endocrinology
|
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue selected to be a potent and selective activator of the PTHR1 signaling pathway. Abaloparatide TFA enhances Gs/cAMP signaling (EC50 of 0.3 nM) and β-arrestin recruitment (EC50 of 0.9 nM) in MC3T3-E1 osteoblast cells.
|
-
- HY-112615
-
NAMPT inhibitor-linker 1
|
NAMPT
Drug-Linker Conjugates for ADC
|
Cancer
|
NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
|
-
- HY-16787
-
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-114266
-
-
- HY-W015445
-
SD-169
|
p38 MAPK
|
Metabolic Disease
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
|
-
- HY-N7087
-
Tulipalin A
α-Methylene butyrolactone
|
Drug Metabolite
|
|
Tulipalin A (α-Methylene butyrolactone) is a toxic glycoside isolated from the tulip bulbs. Tulipalin A is a causative allergen that induces Allergic contact dermatitides. Tulipalin A (α-Methylene butyrolactone) at low dose affects the functionality of immune cells, such as Jurkat T cells.
|
-
- HY-16984
-
GNE-4997
|
Itk
|
Inflammation/Immunology
|
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.
|
-
- HY-15440B
-
Fostemsavir Tris
BMS-663068 Tris
|
HIV
|
Infection
|
Fostemsavir Tris (BMS-663068 (Tris)) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir Tris (BMS-663068 (Tris)) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4 + T cells.
|
-
- HY-120210
-
XY018
|
ROR
|
Cancer
Inflammation/Immunology
|
XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).
|
-
- HY-N1255
-
Scoulerine
(-)-Scoulerine; Discretamine
|
Microtubule/Tubulin
Beta-secretase
Apoptosis
|
Cancer
|
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
|
-
- HY-18728
-
-
- HY-17473
-
Embelin
Embelic acid; Emberine; NSC 91874
|
IAP
NF-κB
Apoptosis
Autophagy
|
Cancer
|
Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
|
-
- HY-N6583
-
Licoflavonol
|
Bacterial
|
Infection
|
Licoflavonol, a minor flavone from the roots of Glycyrrhiza uralensis, is an inhibitor of the Salmonella type III secretion system (T3SS).
|
-
- HY-W032013
-
-
- HY-12420
-
JNJ-47117096 hydrochloride
MELK-T1 hydrochloride
|
MELK
FLT3
|
Cancer
|
JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.
|
-
- HY-U00441
-
DPBQ
|
MDM-2/p53
Apoptosis
|
Cancer
|
DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
|
-
- HY-N7122
-
Thymopentin
|
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
Thymopentin is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs).
|
-
- HY-N7122A
-
Thymopentin acetate
|
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
|
Thymopentin acetate is a biologically active peptide secreted mainly by the epithelial cells of thymic cortex and medulla. Thymopentin acetate is an effective immunomodulatory agent with a short plasma half-life of 30 seconds. Thymopentin acetate enhances the generation of T-cell lineage derived from human embryonic stem cells (hESCs).
|
-
- HY-18303
-
AMG-47a
|
Src
VEGFR
p38 MAPK
JAK
|
Inflammation/Immunology
|
AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
|
-
- HY-B1324
-
-
- HY-101255
-
ODQ
|
Guanylate Cyclase
Apoptosis
|
Cancer
|
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
|
-
- HY-101522
-
CHMFL-EGFR-202
|
EGFR
BMX Kinase
Btk
MEK
|
Cancer
|
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
|
-
- HY-110086
-
RWJ 50271
|
Integrin
|
Inflammation/Immunology
|
RWJ 50271 is an selective and orally active inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC50 of 5.0 μM (HL60 cells). RWJ 50271 inhibits LFA-1/ICAM-1-mediated cell adhesion.
|
-
- HY-N7038
-
Phytohemagglutinin
PHA-M
|
Others
|
Inflammation/Immunology
|
Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, accumulates in the parenchyma cells of the cotyledons. Phytohemagglutinin is a T-cell activator. Stimulation of human mononuclear leukocytes by Phytohemagglutinin induces the expression of ChAT mRNA, and potentiated ACh synthesis.
|
-
- HY-135805
-
JBJ-04-125-02
|
EGFR
|
Cancer
|
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.
|
-
- HY-128947
-
CL2 Linker
|
ADC Linker
|
Cancer
|
CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours).
|
-
- HY-111356
-
IIIM-290
|
CDK
|
Cancer
|
IIIM-290 is a potent and oral CDK inhibitor with IC50s of 90 and 94 nM for CDK2/A and CDK9/T1.
|
-
- HY-107390A
-
AX-024 hydrochloride
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-107390
-
AX-024
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-10446
-
Pralatrexate
|
Antifolate
Apoptosis
|
Cancer
|
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.
|
-
- HY-119881
-
-
- HY-W009245
-
Bz-RS-iSer(3-Ph)-OMe
|
HIV
|
Infection
|
Bz-RS-iSer(3-Ph)-OMe (compound 2), a Taxol derivative, inhibits HSV replication cycle at low cytotoxicity, blocks mitotic divisions of Vero cells, influences M-MSV induced tumor size and affects immune response by inhibiting PHA-induced T lymphocyte proliferation.
|
-
- HY-12467
-
OTS964 hydrochloride
|
TOPK
CDK
Apoptosis
|
Cancer
|
OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
|
-
- HY-N0774
-
Isofraxidin
|
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
|
-
- HY-102052
-
DCEBIO
|
Potassium Channel
|
Inflammation/Immunology
|
DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl - secretion in T84 colonic cells. DCEBIO stimulates Cl - secretion via the activation of hIK1 K + channels and the activation of an apical membrane Cl - conductance.
|
-
- HY-120504
-
N-Acetyltyramine
|
Bacterial
|
Cancer
Infection
|
N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells.
|
-
- HY-N6857
-
Armepavine
|
NF-κB
|
Inflammation/Immunology
|
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades.
|
-
- HY-16689
-
VU 0240551
|
Potassium Channel
|
Others
|
VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission.
|
-
- HY-12680
-
PRN694
|
Itk
|
Inflammation/Immunology
|
PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo.
|
-
- HY-12316
-
20(S)-Hydroxycholesterol
20α-Hydroxycholesterol
|
Smo
Endogenous Metabolite
|
Cancer
|
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
|
-
- HY-N8441
-
Neriifolin
17β-Neriifolin
|
Na+/K+ ATPase
Apoptosis
|
Cancer
Inflammation/Immunology
|
Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells[2.
|
-
- HY-135336A
-
-
- HY-122872
-
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- HY-101467
-
Trilaciclib
G1T28
|
CDK
|
Cancer
|
Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
|
-
- HY-105019A
-
Melflufen hydrochloride
Melphalan flufenamide hydrochloride
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
|
-
- HY-105019
-
Melflufen
Melphalan flufenamide
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells.
|
-
- HY-122295
-
Dehydroleucodine
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Dehydroleucodine is a sesquiterpene lactone isolated from Gynoxys verrucosa. Dehydroleucodine is a mast cell stabilizer that inhibits tmast cell degranulation induced by compound 48/80. Dehydroleucodine inudces cells apoptosis, and has gastric ulcer inhibition and antileukemic effects.
|
-
- HY-19779
-
JTT 551
|
Phosphatase
|
Metabolic Disease
|
JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively; JTT 551 can be used in the research of type 2 diabetes mellitus.
|
-
- HY-15583
-
-
- HY-18341A
-
-
- HY-N1403
-
Tigogenin
|
Others
|
Metabolic Disease
|
Tigogenin, one of steroidal sapogenins, is widely used for synthesizing steroid drugs. Tigogenin inhibits adipocytic differentiation and induces osteoblastic differentiation in mouse bone marrow stromal cells.
|
-
- HY-P1052
-
Myelin Basic Protein(87-99)
|
Others
|
Inflammation/Immunology
|
Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS).
|
-
- HY-122181A
-
OTS186935 trihydrochloride
|
Histone Methyltransferase
|
Cancer
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells.
|
-
- HY-13811
-
NSC697923
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
|
-
- HY-P3139
-
TPP-1
|
PD-1/PD-L1
|
Cancer
|
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function.
|
-
- HY-101030
-
MBM-17
|
Apoptosis
|
Cancer
|
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
|
-
- HY-A0003B
-
Lenalidomide hemihydrate
CC-5013 hemihydrate
|
Ligand for E3 Ligase
Apoptosis
|
Cancer
|
Lenalidomide hemihydrate (CC-5013 hemihydrate) is a derivative of Thalidomide and an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-A0003
-
Lenalidomide
CC-5013
|
Ligand for E3 Ligase
Apoptosis
|
Cancer
Inflammation/Immunology
|
Lenalidomide (CC-5013) is a derivative of Thalidomide and an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-A0003A
-
Lenalidomide hydrochloride
CC-5013 hydrochloride
|
Ligand for E3 Ligase
|
Cancer
Inflammation/Immunology
|
Lenalidomide hydrochloride (CC-5013 hydrochloride) is a derivative of Thalidomide and an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-122470
-
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-124958
-
NDMC101
|
NF-κB
Dipeptidyl Peptidase
|
Metabolic Disease
Inflammation/Immunology
|
NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene express. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
|
-
- HY-136123
-
Tubulin inhibitor 8
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
|
-
- HY-136122
-
Tubulin inhibitor 7
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
|
-
- HY-136121
-
Tubulin inhibitor 6
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
|
-
- HY-15217
-
-
- HY-107994
-
-
- HY-18621A
-
OTS514 hydrochloride
|
TOPK
Apoptosis
|
Cancer
|
OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells. OTS514 hydrochloride induces cell cycle arrest and apoptosis.
|
-
- HY-101096
-
-
- HY-N0041
-
Ginsenoside Rb3
Gypenoside IV
|
NF-κB
COX
NO Synthase
|
Cancer
Inflammation/Immunology
|
Ginsenoside Rb3 is extracted from steamed Panax notoginseng. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
|
-
- HY-N4113
-
Glycycoumarin
|
Autophagy
|
Cancer
|
Glycycoumarin is a major bioactive coumarin of licorice. Glycycoumarin inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway. Glycycoumarin exerts anti-liver cancer activity by directly targeting T-LAK cell-originated protein kinase .
|
-
- HY-101775A
-
-
- HY-15164A
-
Icotinib
BPI-2009
|
EGFR
|
Cancer
|
Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q.
|
-
- HY-15164
-
Icotinib Hydrochloride
BPI-2009H
|
EGFR
|
Cancer
|
Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q.
|
-
- HY-N3415
-
Kumatakenin
|
Apoptosis
|
Cancer
|
Kumatakenin, a flavonoid that is isolated from cloves shows the effect of inducing apoptosis in ovarian cancer cells.
|
-
- HY-N7695
-
Physalin B
|
Apoptosis
Autophagy
|
Cancer
|
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro.
|
-
- HY-P3139A
-
TPP-1 TFA
|
PD-1/PD-L1
|
Cancer
|
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function.
|
-
- HY-100579
-
Ferrostatin-1
|
Ferroptosis
Fungal
|
Cancer
|
Ferrostatin-1, a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1, a synthetic antioxidant, acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibit cell death. Antifungal Activity.
|
-
- HY-18621
-
OTS514
|
TOPK
Apoptosis
|
Cancer
|
OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.
|
-
- HY-14171S
-
Bexarotene D4
LGD1069 D4
|
RAR/RXR
Autophagy
|
Cancer
|
Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
|
-
- HY-N2599
-
Taraxerol acetate
|
COX
Apoptosis
|
Cancer
|
Taraxerol acetate is a COX-1 and COX-2 inhibitor with IC50 values of 116.3 μM and 94.7 μM, respectively. Taraxerol acetate the has the anticancer potential and induces cell apoptosis.
|
-
- HY-100360
-
MS049
|
Histone Methyltransferase
|
Cancer
|
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
|
-
- HY-100360A
-
MS049 dihydrochloride
|
Histone Methyltransferase
|
Cancer
|
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells.
|
-
- HY-112616
-
NAMPT inhibitor-linker 2
|
NAMPT
Drug-Linker Conjugates for ADC
|
Cancer
|
NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
|
-
- HY-B0795
-
MHY1485
|
mTOR
Autophagy
|
Cancer
|
MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
|
-
- HY-16981
-
SB-332235
|
CXCR
|
Inflammation/Immunology
|
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells.
|
-
- HY-121638A
-
(5Z,2E)-CU-3
|
Apoptosis
|
Cancer
|
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
|
-
- HY-122534
-
Mensacarcin
|
Mitochondrial Metabolism
ADC Cytotoxin
Apoptosis
|
Cancer
|
Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-124771
-
RH01386
|
Others
|
Metabolic Disease
|
RH01386 is a small molecule that can prevent ER stress-induced β cell dysfunction and death, and inhibits proapoptotic gene expression. RH01386 restores ER stress-impaired glucose-stimulated insulin secretion responses. RH01386 has the potential for type 2 diabetes treatment.
|
-
- HY-12026
-
WZ4002
|
EGFR
|
Cancer
|
WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750 and EGFR E746_A750/T790M, respectively.
|
-
- HY-114268
-
BRD-K98645985
|
HIV
|
Infection
|
BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without T cell activation or toxicity.
|
-
- HY-N4215
-
11(α)-Methoxysaikosaponin F
|
Others
|
Inflammation/Immunology
|
11(α)-Methoxysaikosaponin F is a triterpenoid saponin isolated from Bupleurum marginatum Wall.ex DC(ZYCH) which is a promising therapeutic for liver fibrosis. 11(α)-Methoxysaikosaponin F has an IC50 of 387.7 nM with viability of hepatic stellate cells-T6 (HSCs-T6). Triterpenoid saponins have numerous targets, important network positions, and strong inhibitory activity.
|
-
- HY-111149A
-
PS372424 hydrochloride
|
CXCR
|
Inflammation/Immunology
|
PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation.
|
-
- HY-111149
-
PS372424
|
CXCR
|
Inflammation/Immunology
|
PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 prevents human T-cell migration in a humanized model of arthritic inflammation.
|
-
- HY-11007
-
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-14454
-
TPh A
Triphenyl Compound A
|
Others
|
Cancer
|
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
|
-
- HY-129390
-
Orelabrutinib
ICP-022
|
Btk
|
Cancer
|
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
|
-
- HY-19992
-
3-Bromopyruvic acid
Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP
|
Hexokinase
Apoptosis
Autophagy
|
Cancer
|
3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities.
|
-
- HY-101030A
-
MBM-17S
|
Apoptosis
|
Cancer
|
MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.
|
-
- HY-122590
-
Glabrescione B
|
Gli
|
Cancer
|
Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.
|
-
- HY-116090
-
Conoidin A
|
Parasite
|
Infection
Neurological Disease
Cardiovascular Disease
|
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
|
-
- HY-19356
-
Rocaglamide
Roc-A
|
NF-κB
HSP
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
|
-
- HY-15814
-
HG-7-85-01
|
Bcr-Abl
PDGFR
c-Kit
Src
JAK
Apoptosis
|
Cancer
|
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
|
-
- HY-12001
-
WZ-3146
|
EGFR
|
Cancer
|
WZ3146 is a mutant selective EGFR inhibitor with IC50s of
2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
|
-
- HY-13686
-
PQ401
|
IGF-1R
Apoptosis
|
Cancer
|
PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.
|
-
- HY-13917A
-
PND-1186 hydrochloride
VS-4718 hydrochloride; SR-2516 hydrochloride
|
FAK
Apoptosis
|
Cancer
|
PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.
|
-
- HY-13917
-
PND-1186
VS-4718; SR-2516
|
FAK
Apoptosis
|
Cancer
|
PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.
|
-
- HY-113903
-
(+)-Isopulegol
|
Parasite
|
Infection
|
(+)-Isopulegol is a terpenoid found in Mentha canadensis L. (+)-Isopulegol shows phagostimulatory activity towards adults of S. granarius and T. confusum. (+)-Isopulegol is a feeding attractant for adults of T. confusum and T. granarium larvae.
|
-
- HY-135858
-
SARS-CoV-IN-3
|
SARS-CoV
Parasite
HIV
|
Infection
|
SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells.
|
-
- HY-P0023
-
Cyclo(-RGDfK)
|
Integrin
|
Cancer
|
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-15729
-
Rociletinib
CO-1686; AVL-301; CNX-419
|
EGFR
|
Cancer
|
Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
|
-
- HY-14957
-
Ozenoxacin
T-3912
|
Bacterial
|
Infection
|
Ozenoxacin is a nonfluorinated quinolone antibacterial, which shows potent activities against the main microorganisms isolated from skin and soft tissue infections.
|
-
- HY-138540
-
1-Dodecylimidazole
N-Dodecylimidazole
|
Fungal
|
Cancer
|
1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity.
|
-
- HY-135745
-
Sulfentrazone
|
Others
|
Others
|
Sulfentrazone is a phenyl triazolinone herbicide used for control of certain broadleaf and grass weed species. Sulfentrazone inhibits protoporphyrinogen oxidase, resulting in the disruption of lipid cell membranes.
|
-
- HY-16062
-
ARQ 621
|
Kinesin
|
Cancer
|
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
|
-
- HY-133511
-
MLS000544460
|
Phosphatase
|
Cancer
|
MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity.
|
-
- HY-18681
-
Voxelotor
GBT 440
|
Others
|
Cardiovascular Disease
|
Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment.
|
-
- HY-50101A
-
Mavorixafor trihydrochloride
AMD-070 trihydrochloride
|
CXCR
HIV
|
Infection
Endocrinology
|
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
|
-
- HY-N6939
-
-
- HY-50101
-
Mavorixafor
AMD-070
|
CXCR
HIV
|
Infection
Endocrinology
|
Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
|
-
- HY-114436
-
MRTX-1257
|
Ras
|
Cancer
|
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
|
-
- HY-P0023A
-
Cyclo(-RGDfK) TFA
|
Integrin
|
Cancer
|
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-13897
-
CNX-2006
|
EGFR
|
Cancer
|
CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFR T790M.
|
-
- HY-129550
-
BI-4020
|
EGFR
|
Cancer
|
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties.
|
-
- HY-15408
-
Trelagliptin
SYR-472
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
Trelagliptin (SYR-472) is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).
|
-
- HY-N0732
-
Jolkinolide B
|
Apoptosis
|
Cancer
|
Jolkinolide B, a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud, is known to induce apoptosis in cancer cells.
|
-
- HY-118355
-
ALLM
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
|
-
- HY-118630
-
Vacuolin-1
|
PIKfyve
Autophagy
|
Cancer
|
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca 2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation.
|
-
- HY-15408A
-
Trelagliptin succinate
SYR-472 succinate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
Trelagliptin (SYR-472) succinate is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).
|
-
- HY-15729A
-
Rociletinib hydrobromide
CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide
|
EGFR
|
Cancer
|
Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
|
-
- HY-108618
-
BC11-38
|
Phosphodiesterase (PDE)
|
Endocrinology
|
BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.
|
-
- HY-112126
-
KRN5
|
Others
|
Inflammation/Immunology
|
KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis.
|
-
- HY-15225
-
Telomestatin
|
Telomerase
ADC Cytotoxin
|
Cancer
|
Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Telomestatin is an ADC cytotoxin and can be used for cancer research.
|
-
- HY-50896
-
Erlotinib
CP-358774; NSC 718781; OSI-774
|
EGFR
Autophagy
|
Cancer
|
Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer.
|
-
- HY-N7006
-
-
- HY-15597
-
Salinomycin
Procoxacin
|
Bacterial
Wnt
β-catenin
Mitophagy
Autophagy
Apoptosis
Antibiotic
|
Cancer
|
Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells.
|
-
- HY-N5021
-
Anhydrosafflor yellow B
AHSYB
|
Others
|
Neurological Disease
|
Anhydrosafflor yellow B (AHSYB) is a quinochalcone C-glycoside isolated from Carthamus tinctorius. Anhydrosafflor yellow B inhibits ADP-induced platelet aggregation, exhibits significant anti-oxidative effects in vitro, and possesses certain activity against H2O2-induced cytotoxicity in cultured PC12 cells and primary neuronal cells.
|
-
- HY-B0517
-
Mepivacaine
|
Sodium Channel
|
Neurological Disease
|
Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
|
-
- HY-137471
-
RBPJ Inhibitor-1
RIN1
|
Notch
|
Cancer
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
|
-
- HY-135276
-
Targaprimir-96
|
MicroRNA
Apoptosis
|
Cancer
|
Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
|
-
- HY-19644
-
GSK2256294A
GSK 2256294
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.
|
-
- HY-70002S
-
-
- HY-103269
-
BAI1
|
Bcl-2 Family
Apoptosis
|
Cancer
|
BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
|
-
- HY-P1034
-
DAPTA
D-Ala-peptide T-amide; Adaptavir
|
CCR
HIV
|
Infection
Endocrinology
|
DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities.
|
-
- HY-114495
-
Caerulomycin A
Cerulomycin; Caerulomycin
|
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.
|
-
- HY-19747
-
HPOB
|
HDAC
Apoptosis
|
Cancer
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.
|
-
- HY-135955
-
-
- HY-14374
-
GPP78
CAY10618
|
NAMPT
Autophagy
|
Cancer
Inflammation/Immunology
|
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.
|
-
- HY-136312
-
17-DMAP-GA
|
Others
|
Cancer
|
17-DMAP-GA, a Geldanamycin (HY-15230) analogue, is an inhibitor of HSP90. 17-DMAP-GA causes cell cycle abnormalities.
|
-
- HY-10985
-
Marizomib
Salinosporamide A; NPI-0052
|
Proteasome
|
Cancer
|
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
|
-
- HY-19826
-
-
- HY-N6076
-
Tenuifoliside A
|
ERK
|
Neurological Disease
|
Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
|
-
- HY-W028690
-
DNMDP
|
Phosphodiesterase (PDE)
|
Cancer
|
DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity.
|
-
- HY-121508
-
(E/Z)-IT-603
|
NF-κB
|
Cancer
Inflammation/Immunology
|
(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases.
|
-
- HY-135008
-
J14
|
Reactive Oxygen Species
|
Cancer
|
J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death.
|
-
- HY-129937A
-
GNE-987
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
GNE-987 is a highly active chimeric BET degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
|
-
- HY-133570
-
17-AEP-GA
|
HSP
ADC Cytotoxin
|
Cancer
|
17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
|
-
- HY-131394
-
5-Hydroxymethyl-2’-deoxycytidine
5hmdC
|
Others
|
Cancer
|
5-Hydroxymethyl-2’-deoxycytidine (5hmdC) is an oxidation derivative of 5-methyl-2'-deoxycytidine (5-mdC) in DNA. 5-Hydroxymethyl-2’-deoxycytidine may serve as a marker of irreversibly damaged cells.
|
-
- HY-W004282
-
Undecanoic acid
Undecanoate; Hendecanoic acid
|
Fungal
Endogenous Metabolite
|
Infection
|
Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum.
|
-
- HY-136528
-
RA-9
|
Deubiquitinase
Apoptosis
|
Cancer
|
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.
|
-
- HY-103349
-
PETCM
|
Caspase
Apoptosis
|
Cancer
|
PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.
|
-
- HY-101519
-
BETd-260
ZBC 260
|
PROTAC
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BETd-260 (ZBC 260) is a potent PROTAC BET degrader, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
- HY-W011303
-
Phytosphingosine
|
Apoptosis
|
Cancer
|
Phytosphingosine is a phospholipid and has anti-cancer activities. Phytosphingosine induces cell apoptosis via caspase 8 activation and Bax translocation in cancer cells.
|
-
- HY-129578
-
-
- HY-B0847
-
Propiconazole
|
Fungal
Reactive Oxygen Species
|
Infection
|
Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS).
|
-
- HY-N0671
-
Rhapontin
Rhaponiticin
|
Apoptosis
|
Cancer
|
Rhapontin (Rhaponiticin), a component of rhubarb (Rheum officinale Baillon), induces apoptosis resulting in suppression of proliferation of human stomach cancer KATO III cells.
|
-
- HY-10591
-
-
- HY-111360
-
SPL-707
|
γ-secretase
|
Inflammation/Immunology
|
SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
|
-
- HY-125729
-
-
- HY-14291
-
-
- HY-136453
-
-
- HY-130616
-
EGFR-IN-11
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
|
-
- HY-P3143A
-
BMSpep-57 hydrochloride
|
PD-1/PD-L1
|
Cancer
|
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs.
|
-
- HY-100888
-
Simurosertib
TAK-931
|
CDK
|
Cancer
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity.
|
-
- HY-111838A
-
ZZW-115 hydrochloride
|
Apoptosis
|
Cancer
|
ZZW-115 hydrochloride is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 hydrochloride induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
|
-
- HY-111838
-
ZZW-115
|
Apoptosis
|
Cancer
|
ZZW-115 is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
|
-
- HY-133556
-
IQZ23
|
AMPK
|
Metabolic Disease
|
IQZ23 inhibits adipocyte differentiation via AMPK pathway activation. IQZ23 exerts a high efficacy in decreasing the triglyceride level (EC50=0.033 μM) in 3T3-L1 adipocytes. IQZ23 could be used for the research of obesity and related metabolic disorders.
|
-
- HY-16936
-
JH-II-127
|
LRRK2
|
Neurological Disease
|
JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.
|
-
- HY-10346
-
AV-412
MP412
|
EGFR
|
Cancer
|
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
|
-
- HY-101029
-
MBM-55
|
Apoptosis
|
Cancer
|
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
|
-
- HY-128600
-
ERD-308
|
PROTAC
Estrogen Receptor/ERR
|
Cancer
|
ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).
|
-
- HY-P1191
-
JIP-1(153-163)
T1-JIP
|
JNK
|
Others
|
JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).
|
-
- HY-108391
-
C8-Ceramide
N-Octanoyl-D-erythro-sphingosine
|
Apoptosis
PKC
Autophagy
|
Cancer
Inflammation/Immunology
|
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
|
-
- HY-130122
-
MG-277
|
PROTAC
Apoptosis
|
Cancer
|
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.
|
-
- HY-U00220
-
-
- HY-N1039A
-
Manool
|
Others
|
Cancer
|
Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle.
|
-
- HY-N7707
-
Sandacanol
|
Apoptosis
|
Cancer
|
Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells.
|
-
- HY-N2534
-
Karanjin
|
AMPK
Apoptosis
|
Cancer
|
Karanjin is a major active furanoflavonol constituent of Fordia cauliflora. Karanjin induces GLUT4 translocation in skeletal muscle cells by increasing AMPK activity. Karanjin can induce cancer cell death through cell cycle arrest and enhance apoptosis.
|
-
- HY-B0517A
-
Mepivacaine hydrochloride
|
Sodium Channel
|
Neurological Disease
|
Mepivacaine hydrochloride is an amide-type local anesthetic agent. Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
|
-
- HY-113953
-
Z-Asp-CH2-DCB
|
Caspase
|
Inflammation/Immunology
|
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.
|
-
- HY-N3523
-
3-O-Beta-D-Glucopyranosylplatycodigenin
|
Others
|
Cancer
|
3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC50 of 13.36 μM.
|
-
- HY-128860
-
Mutated EGFR-IN-2
|
EGFR
|
Cancer
|
Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
|
-
- HY-101489A
-
GZD856 formic
|
PDGFR
Bcr-Abl
Apoptosis
|
Cancer
|
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
|
-
- HY-101489
-
GZD856
|
PDGFR
Bcr-Abl
Apoptosis
|
Cancer
|
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
|
-
- HY-14521
-
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-14521B
-
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-100490
-
Rilmenidine
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
|
-
- HY-127170
-
3-Hydroxycoumarin
|
Others
|
Others
|
3-hydroxycoumarin is a potent and redox inhibitor of human 15-LOX-1. 3-hydroxycoumarin is recently demonstrated to protect sea urchin reproductive cells against ultraviolet B damage.
|
-
- HY-14291A
-
-
- HY-100213
-
EAI045
|
EGFR
|
Cancer
|
EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
|
-
- HY-129601
-
MYCi975
NUCC-0200975
|
c-Myc
|
Cancer
Inflammation/Immunology
|
MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good tolerability, increases tumor immune cell infiltration, and sensitizes tumors to anti-PD1 immunotherapy.
|
-
- HY-W013274
-
CPTH2
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).
|
-
- HY-15036
-
Diclofenac
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-15038
-
Diclofenac potassium
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac potassium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-12892
-
SKI-178
|
SPHK
Apoptosis
|
Cancer
|
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
|
-
- HY-113204
-
-
- HY-101867
-
AU1235
|
Bacterial
|
Cancer
Infection
|
AU1235, an adamantyl urea, is a potent MmpL3 inhibitor. The Mycobacterium tuberculosis protein MmpL3 performs an essential role in cell wall synthesis, since it effects the transport of trehalose monomycolates across the inner membrane.
|
-
- HY-13984
-
Mutant EGFR inhibitor
|
EGFR
|
Cancer
|
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
|
-
- HY-135856
-
SARS-CoV-IN-2
|
SARS-CoV
Parasite
HIV
|
Infection
|
SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities.
|
-
- HY-108741
-
Plecanatide
|
Guanylate Cyclase
|
Inflammation/Immunology
|
Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.
|
-
- HY-124675
-
MYCMI-6
NSC354961
|
c-Myc
Apoptosis
|
Cancer
|
MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis.
|
-
- HY-131058
-
Muscotoxin A
|
ADC Cytotoxin
|
Cancer
|
Muscotoxin A is an ADC cytotoxin. Muscotoxin A is a cytotoxic lipopeptide that permeabilizes mammalian cell membranes and induces necrotic cell death.
|
-
- HY-15036A
-
Diclofenac diethylamine
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-15037
-
Diclofenac Sodium
GP 45840
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-121282A
-
Mepazine hydrochloride
Pecazine hydrochloride
|
MALT1
Apoptosis
|
Cancer
|
Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis.
|
-
- HY-D0226
-
Quinizarin
1,4-Dihydroxyanthraquinone
|
DNA/RNA Synthesis
Fungal
|
Cancer
Infection
|
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth.
|
-
- HY-121282
-
Mepazine
Pecazine
|
MALT1
Apoptosis
|
Cancer
|
Mepazine (Pecazine) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.
|
-
- HY-B0640A
-
-
- HY-100219
-
CB1151
|
VD/VDR
|
Cancer
|
CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM.
|
-
- HY-129388B
-
CC-90011 benzenesulfonate
LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
|
-
- HY-14373
-
CB30865
ZM 242421
|
NAMPT
|
Cancer
|
CB30865 (ZM 242421) is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with potent cytotoxicity. CB30865 is highly potent against a variety of human tumour cell lines (IC50 values in the 1-10 nM range).
|
-
- HY-N0128
-
Sclareol
|
Apoptosis
|
Cancer
|
Sclareol is isolated from Salvia sclarea with anticarcinogenic activity. Sclareol shows strong cytotoxic activity against mouse leukemia (P-388), human epidermal carcinoma (KB) cells and human leukemia cell lines. Sclareol induces cell apoptosis.
|
-
- HY-101029A
-
MBM-55S
|
Ribosomal S6 Kinase (RSK)
DYRK
Apoptosis
|
Cancer
|
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.
|
-
- HY-104066
-
Theliatinib
HMPL-309
|
EGFR
|
Cancer
|
Theliatinib (HMPL-309) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases. Anti-tumor activity.
|
-
- HY-10346A
-
AV-412 free base
MP-412 free base
|
EGFR
|
Cancer
|
AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
|
-
- HY-101058
-
-
- HY-B0640
-
-
- HY-P3143
-
BMSpep-57
|
PD-1/PD-L1
|
Cancer
|
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs.
|
-
- HY-102011A
-
BMS-1166 hydrochloride
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-P1854
-
β-Amyloid (1-9)
|
Amyloid-β
|
Neurological Disease
|
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism .
|
-
- HY-B0768A
-
-
- HY-N2373
-
-
- HY-101076
-
L-690488
|
Phosphatase
|
Metabolic Disease
|
L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor. L-690488 has more effective cell penetration than L-690330.
|
-
- HY-137295
-
Ingenol 3,20-dibenzoate
|
PKC
Apoptosis
|
Inflammation/Immunology
|
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells.
|
-
- HY-129388
-
CC-90011 Methylbenzenesulfonate
LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Cancer
|
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
|
-
- HY-70002
-
-
- HY-113914
-
9-ING-41
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.
|
-
- HY-P1066
-
Apelin-17(human, bovine)
|
HIV
|
Infection
|
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-122181B
-
OTS186935 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.
|
-
- HY-12029
-
WZ8040
|
EGFR
|
Cancer
|
WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal.
|
-
- HY-136373
-
Metazachlor
|
Others
|
Others
|
Metazachlor is a herbicide of the chloroacetamide class. Metazachlor is an inhibitor of the synthesis of long chain fatty acids and has an effect on cell division or tissue differentiation in the germinating and emerging weed target species.
|
-
- HY-120139
-
KMH-233
|
Others
|
Cancer
|
KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).
|
-
- HY-14674
-
CP-724714
|
EGFR
Apoptosis
|
Cancer
|
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
|
-
- HY-B2028
-
Propargite
|
Parasite
|
Infection
|
Propargite is a pesticide used to kill mites. Propargite induces β-cell necrosis preceded by DNA damage. Propargite induces MIN6 cell death with an IC50 of 1 μM.
|
-
- HY-119906
-
Conglobatin
FW-04-806
|
HSP
Apoptosis
|
Cancer
|
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.
|
-
- HY-108847
-
Etanercept
|
TNF Receptor
|
Inflammation/Immunology
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
|
-
- HY-18981
-
Decursin
(+)-Decursin
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
Decursin ((+)-Decursin) is a cytotoxic agent and a potent protein kinase C activator from the Root of Angelica gigas. Decursin inhibits tumor growth, migration, and invasion in gastric cancer by down-regulating CXCR7 expression. Decursin inhibits the growth of HepG2 cells via Hippo/YAP signaling pathway.
|
-
- HY-16196
-
ENMD-1198
IRC-110160
|
Microtubule/Tubulin
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
|
-
- HY-111415
-
EGFR-IN-5
|
EGFR
|
Cancer
|
EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR L858R, EGFR L858R/T790M, and EGFR L858R/T790M/C797S, respectively.
|
-
- HY-123390
-
DB07107
|
Bcr-Abl
Akt
|
Cancer
|
DB07107 is a potent drug resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
|
-
- HY-128589
-
CHMFL-KIT-033
|
c-Kit
|
Cancer
|
CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM.
|
-
- HY-131911
-
-
- HY-N0899
-
-
- HY-15398A
-
5,6-trans-Vitamin D3
5,6-trans-Cholecalciferol; 5,6-trans-Colecalciferol
|
VD/VDR
|
Metabolic Disease
|
5,6-trans-Vitamin D3 (5,6-trans-Cholecalciferol;5,6-trans-Colecalciferol) is a photoproduct of vitamin D3. Vitamin D3 is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
|
-
- HY-P1066A
-
Apelin-17(human, bovine) TFA
|
HIV
|
Infection
|
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-N7496
-
Odoroside A
|
Apoptosis
|
Cancer
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
|
-
- HY-122181
-
OTS186935
|
Histone Methyltransferase
|
Cancer
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells.
|
-
- HY-108640
-
HLI373
|
MDM-2/p53
Parasite
Apoptosis
|
Cancer
Infection
|
HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
|
-
- HY-108640A
-
HLI373 dihydrochloride
|
MDM-2/p53
Parasite
Apoptosis
|
Cancer
Infection
|
HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
|
-
- HY-125531
-
Dactylorhin A
|
Others
|
Others
|
Dactylorhin A, a succinate derivative ester, is isolated from rhizomes of Gymnadenia conopsea. Dactylorhin A exhibits moderate inhibitory effects on NO production effects in RAW 264.7 macrophage cells.
|
-
- HY-108601A
-
Ro 32-0432 hydrochloride
|
PKC
|
Inflammation/Immunology
Neurological Disease
|
Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
|
-
- HY-15178
-
Oglemilast
GRC 3886
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
|
-
- HY-19834
-
Fenebrutinib
GDC-0853
|
Btk
|
Cancer
|
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
|
-
- HY-N3026
-
Soyasaponin Ab
|
Others
|
Metabolic Disease
|
Soyasaponin Ab is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
|
-
- HY-N3027
-
Soyasaponin Aa
|
Others
|
Metabolic Disease
|
Soyasaponin Aa is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).
|
-
- HY-19947
-
PF-06291874
Glucagon receptor antagonists-4
|
Glucagon Receptor
|
Metabolic Disease
|
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM).
|
-
- HY-129851
-
NTP42
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca 2+] mobilization following stimulation of cells with the alternative TP agonist U46609. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).
|
-
- HY-104037
-
Cintirorgon
LYC-55716
|
ROR
|
Cancer
|
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
|
-
- HY-117433
-
-
- HY-130997
-
-
- HY-125209A
-
TH5427 hydrochloride
|
DNA/RNA Synthesis
|
Cancer
|
TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells.
|
-
- HY-N4114
-
Picrocrocin
|
Apoptosis
|
Cancer
|
Picrocrocin, an apocarotenoid found in the flowers of Cochliobolus sativus. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanoma cells.
|
-
- HY-N0069
-
Solamargine
Solamargin; δ-Solanigrine
|
P-glycoprotein
Apoptosis
|
Cancer
|
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.
|
-
- HY-116304
-
1G244
|
Dipeptidyl Peptidase
Apoptosis
|
Cancer
|
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
|
-
- HY-135855
-
SARS-CoV-IN-1
|
SARS-CoV
Parasite
|
Infection
|
SARS-CoV-IN-1 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-1 shows anti-Coronavirus activity with an EC50 of 4.9 μM in Vero cells. SARS-CoV-IN-1 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 15.4 and 133.2 nM; and IC90s of 25.7 and 459.1 nM; respectively. Antimalarial and antiviral activities.
|
-
- HY-N6042
-
-
- HY-101406
-
-
- HY-N4253
-
Kudinoside D
|
Others
|
Metabolic Disease
|
Kudinoside D is a main natural component of triterpenoid saponin derived from Ilex kudingcha. Kudinoside D suppresses adipogenesis through modulation of the AMPK pathway in 3T3-L1 adipocytes.
|
-
- HY-15553A
-
-
- HY-136594
-
BODIPY aminoacetaldehyde
BAAA
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for both murine and human aldehyde dehydrogenase (ALDH). BODIPY aminoacetaldehyde consists of an aminoacetaldehyde moiety bonded to the BODIPY fluorochrome and can be used to label stem cells.
|
-
- HY-101939
-
RP-001
|
LPL Receptor
|
Neurological Disease
|
RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
|
-
- HY-101939A
-
RP-001 hydrochloride
|
LPL Receptor
|
Neurological Disease
|
RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5.
|
-
- HY-N0595
-
Genistin
Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
Metabolic Disease
|
Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway.
|
-
- HY-13756A
-
-
- HY-110147A
-
SSM3 tetraTFA
|
Others
|
Infection
|
SSM3 tetraTFA is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro.
|
-
- HY-126251
-
CDK9-IN-7
|
CDK
Apoptosis
|
Cancer
|
CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
|
-
- HY-12830
-
M-110
|
Pim
|
Cancer
|
M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
|
-
- HY-W011916
-
Muramic acid
|
Bacterial
|
Others
|
Muramic acid is a component in many Gram-positive bacterial cell walls, as marker for Gram-positive bacteria.
|
-
- HY-11009
-
CGP60474
|
CDK
PKC
|
Cancer
|
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.
|
-
- HY-18773
-
Oct3/4-inducer-1
|
Oct3/4
|
Inflammation/Immunology
|
Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells.
|
-
- HY-131042
-
NNMTi
|
Others
|
Metabolic Disease
|
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues. NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice.
|
-
- HY-18819
-
BCR-ABL-IN-2
|
Bcr-Abl
|
Cancer
|
BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1 native and ABL1 T315I, respectively.
|
-
- HY-10339
-
-
- HY-131010
-
Flutax-2
|
Microtubule/Tubulin
|
Cancer
|
FLUTAX-2 is an active fluorescent derivative of Taxol. FLUTAX-2 binds to polymerized α,β-tubulin dimers. FLUTAX-2 is able to stabilize microtubules of intact T. gallinae and T. foetus trophozoites[1].
|
-
- HY-112234
-
L-Sepiapterin
Sepiapterin
|
Endogenous Metabolite
|
Cancer
|
L-Sepiapterin (Sepiapterin) is a precursor of the endothelial nitric oxide synthase (eNOS) cofactor tetrahydrobiopterin (BH4). L-Sepiapterin improves endothelial dysfunction in small mesenteric arteries from db/db mice, and induces angiogenesis. L-Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70 S6K-dependent VEGFR-2 expression.
|
-
- HY-13603
-
Crolibulin
EPC2407
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity.
|
-
- HY-12378
-
BQ-123
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
|
-
- HY-B1021
-
Vincamine
|
GPR40
|
Metabolic Disease
Cardiovascular Disease
|
Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.
|
-
- HY-13756
-
-
- HY-100746
-
STF-62247
|
Autophagy
|
Cancer
|
STF-62247 is an autophagy inducer that selectively cytotoxic to VHL-deficient renal cell carcinoma (IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively).
|
-
- HY-108741A
-
Plecanatide acetate
|
Guanylate Cyclase
|
Inflammation/Immunology
|
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis.
|
-
- HY-114191
-
-
- HY-114191A
-
-
- HY-15553
-
Mibefradil
Ro 40-5967
|
Calcium Channel
|
Cardiovascular Disease
|
Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca 2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.
|
-
- HY-P9921
-
Trastuzumab emtansine
Ado-Trastuzumab emtansine; PRO132365; T-DM 1
|
EGFR
|
Cancer
|
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer.
|
-
- HY-125801
-
3-Oxo-5β-cholanoic acid
Dehydrolithocholic acid; 3-oxoLCA
|
ROR
|
Inflammation/Immunology
|
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
|
-
- HY-100608
-
BMS453
BMS-189453
|
RAR/RXR
|
Cancer
|
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
|
-
- HY-15160A
-
TAK-960 hydrochloride
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
|
-
- HY-15160B
-
TAK-960 dihydrochloride
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
|
-
- HY-15160
-
TAK-960
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
|
-
- HY-137478A
-
KB-0742 dihydrochloride
|
CDK
|
Cancer
|
KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.
|
-
- HY-11062
-
Icilin
AG-3-5
|
TRP Channel
|
Cancer
Neurological Disease
|
Icilin (AG-3-5) is an agonist of nonselective cation channel TRPM8, with antiproliferative activity. Icilin activates currents only in wild type TRPM8 and in the presence of Ca 2+. Icilin can induce G1 arrest in prostate cancer cells.
|
-
- HY-78869
-
Mutated EGFR-IN-1
Osimertinib analog
|
EGFR
|
Cancer
|
Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
|
-
- HY-P1191A
-
JIP-1(153-163) TFA
T1-JIP TFA
|
JNK
|
Others
|
JIP-1(153-163) TFA (TI-JIP TFA) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).
|
-
- HY-12378A
-
BQ-123 TFA
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
|
-
- HY-12646A
-
Rhosin
|
Ras
Apoptosis
|
Cancer
|
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
|
-
- HY-12646
-
Rhosin hydrochloride
|
Ras
Apoptosis
|
Cancer
|
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
|
-
- HY-103661
-
BI-6C9
|
Mitochondrial Metabolism
Apoptosis
|
Neurological Disease
|
BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons.
|
-
- HY-15160C
-
TAK-960 monohydrochloride
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
|
-
- HY-N8098
-
Pulchinenoside E2
|
Others
|
Cancer
|
Pulchinenoside E2 (Compound 8) is a triterpene saponin isolated from the roots of Pulsatilla chinensis. Pulchinenoside E2 shows cytotoxic to HL-60 cells with an IC50 value of 2.6 µg/mL.
|
-
- HY-115452
-
G5-7
|
JAK
Apoptosis
|
Cancer
|
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
|
-
- HY-N7669
-
-
- HY-N0569
-
-
- HY-101261
-
ATPA
|
iGluR
|
Neurological Disease
|
ATPA is a selective glutamate receptor GluR5 activator with EC50s of 0.66, 9.5, 1.4, 23, 32, 18, and 14 μM for GluR5wt, GluR5(S741M), GluR5(S721T), GluR5(S721T, S741M), GluR5(S741A), GluR5(S741L), and GluR5(S741V), respectively.
|
-
- HY-15473A
-
MLN120B dihydrochloride
ML120B dihydrochloride
|
IKK
|
Cancer
Inflammation/Immunology
|
MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
|
-
- HY-N3446
-
IVHD-valtrate
|
Apoptosis
|
Cancer
|
IVHD-valtrate, an active Valeriana jatamansi derivative, is against human ovarian cancer cells in vitro and in vivo. IVHD-valtrate induces cancer cells apoptosis and arrests the ovarian cancer cells in the G2/M phase. IVHD-valtrate has the potential to be a novel chemotherapeutic agent for the human ovarian cancer research.
|
-
- HY-135774
-
6-Hydroxybenzbromarone
|
Drug Metabolite
Phosphatase
|
Cardiovascular Disease
|
6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting.
|
-
- HY-114356
-
BPI-9016M
|
c-Met/HGFR
|
Cancer
|
BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma.
|
-
- HY-119198
-
NSC745885
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
|
-
- HY-19642
-
Glesatinib
MGCD265
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
|
-
- HY-19642A
-
Glesatinib hydrochloride
MGCD265 hydrochloride
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
|
-
- HY-103178
-
MRE3008F20
|
Adenosine Receptor
|
Cancer
|
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
|
-
- HY-112668
-
-
- HY-W011338
-
Benzyl butyl phthalate
|
Aryl Hydrocarbon Receptor
|
Cancer
|
Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs).
|
-
- HY-W040329
-
-
- HY-124798
-
-
- HY-18340
-
(R)-CR8
CR8, (R)-Isomer
|
CDK
Apoptosis
|
Cancer
Neurological Disease
|
(R)-CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.
|
-
- HY-18340A
-
(R)-CR8 trihydrochloride
CR8, (R)-Isomer trihydrochloride
|
CDK
Apoptosis
|
Cancer
Neurological Disease
|
(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.
|
-
- HY-15504A
-
RGB-286638 free base
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-15504
-
RGB-286638
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-12066
-
-
- HY-100490B
-
Rilmenidine phosphate
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-16399
-
Pladienolide B
|
Apoptosis
|
Cancer
|
Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.
|
-
- HY-N0647
-
Silychristin
|
Others
|
Endocrinology
|
Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM.
|
-
- HY-103697
-
Gardiquimod
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-118341
-
Clitocine
|
Apoptosis
Bcl-2 Family
|
Cancer
|
Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity.
|
-
- HY-12319
-
Cardiogenol C
|
β-catenin
Wnt
|
Cancer
|
Cardiogenol C is a potent cell-permeable pyrimidine inducer which prompts the differentiation of ESCs into cardiomyocytes (EC50=100 nM). Cardiogenol C also acts cardiomyogenic on already lineage-committed progenitor cell types with a limited degree of plasticity. Cardiogenol C is a useful cardiomyogenic agent and can be used as a tool to improve cardiac repair by cell transplantation therapy in animal models.
|
-
- HY-12319A
-
Cardiogenol C hydrochloride
|
β-catenin
Wnt
|
Cardiovascular Disease
|
Cardiogenol C hydrochloride is a potent cell-permeable pyrimidine inducer which prompts the differentiation of ESCs into cardiomyocytes (EC50=100 nM). Cardiogenol C hydrochloride also acts cardiomyogenic on already lineage-committed progenitor cell types with a limited degree of plasticity. Cardiogenol C hydrochloride is a useful cardiomyogenic agent and can be used as a tool to improve cardiac repair by cell transplantation therapy in animal models.
|
-
- HY-130709
-
PROTAC CDK2/9 Degrader-1
|
PROTAC
CDK
|
Cancer
|
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.
|
-
- HY-12502B
-
-
- HY-12502
-
-
- HY-19721
-
-
- HY-113408
-
-
- HY-101616
-
-
- HY-135982
-
GPR81 agonist 1
|
Others
|
Metabolic Disease
|
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a.
|
-
- HY-129099
-
N-Desmethyltamoxifen
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
|
Cancer
|
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
|
-
- HY-129099A
-
N-Desmethyltamoxifen hydrochloride
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
|
Cancer
|
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
|
-
- HY-128781
-
-
- HY-N7262
-
Hydroxyvalerenic acid
|
Others
|
Cancer
|
Hydroxyvalerenic acid is isolated from Verbena officinalis, has a low toxicity with IC50 values of 123 and 165 μM against GLC4 and COLO 320 cells, respectively.
|
-
- HY-15838
-
ID-8
|
DYRK
|
Cancer
|
ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs.
|
-
- HY-13894
-
Tyrphostin AG1296
AG1296
|
PDGFR
c-Kit
FLT3
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
|
-
- HY-136526
-
BCR-ABL-IN-3
|
Bcr-Abl
|
Cancer
|
BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC50 of ≤100 nM for Ba/F3Bcr-Abl T3151. BCR-ABL-IN-3 has anti-cancer activity.
|
-
- HY-119370
-
CHMFL-ABL-121
|
Bcr-Abl
Apoptosis
|
Cancer
|
CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.
|
-
- HY-N4000
-
Digitonin
|
Others
|
Cancer
|
Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth. Digitonin is an natural detergent.
|
-
- HY-N3119
-
Paeoniflorigenone
|
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-133128
-
FM26
|
ROR
|
Cancer
|
FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.
|
-
- HY-P1432
-
K-(D-1-Nal)-FwLL-NH2
|
GHSR
|
|
K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
|
-
- HY-P1064
-
Apelin-36(human)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-135680
-
I-OMe-Tyrphostin AG 538
I-OMe-AG 538
|
IGF-1R
|
Cancer
Metabolic Disease
|
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
|
-
- HY-70068
-
-
- HY-44178
-
-
- HY-10251
-
BMS-599626
AC480
|
EGFR
|
Cancer
|
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
|
-
- HY-13297
-
PYZD-4409
|
E1/E2/E3 Enzyme
|
Cancer
|
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
|
-
- HY-126666
-
PNU-159682 carboxylic acid
|
ADC Cytotoxin
|
Cancer
Inflammation/Immunology
|
PNU-159682 carboxylic acid (compound 53) is a potent ADCs cytotoxin and encodes a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid has protein fold and diverse functions, such as cell adhesion, cell-cell signalling, glycoprotein turnover, and roles in inflammation and immune response.
|
-
- HY-13024
-
Rebastinib
DCC-2036
|
Bcr-Abl
FLT3
Src
Apoptosis
|
Cancer
|
Rebastinib (DCC-2036) is a non-ATP-competitive Bcr-Abl inhibitor for Abl1 WT and Abl1 T315I with IC50 of 0.8 nM and 4 nM, also inhibits SRC, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit.
|
-
- HY-103697A
-
Gardiquimod diTFA
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-N7690
-
3,5,7,3′,4′-Pentamethoxyflavone
|
Others
|
Metabolic Disease
|
3,5,7,3′,4′-Pentamethoxyflavone is a polymethoxyflavonoid that can be extracted from Kaempferia parviflora. 3,5,7,3′,4′-Pentamethoxyflavone can induce adipogenesis on 3T3-L1 preadipocytes by regulating transcription factors at an early stage of differentiation.
|
-
- HY-B1057S2
-
Nefopam D3
Fenazoxine D3
|
β-catenin
|
Neurological Disease
|
Nefopam D3 (Fenazoxine D3) is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells.
|
-
- HY-P1126
-
Dolastatin 15
DLS 15
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin.
|
-
- HY-A0067
-
Oxybenzone
Benzophenone 3
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
|
Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
|
-
- HY-B0902A
-
Rufloxacin hydrochloride
MF-934 hydrochloride
|
Bacterial
|
Infection
|
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
|
-
- HY-B0097
-
Floxuridine
5-Fluorouracil 2'-deoxyriboside
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
Apoptosis
|
Cancer
Infection
|
Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.
|
-
- HY-15772A
-
Osimertinib mesylate
AZD-9291 mesylate; Mereletinib mesylate
|
EGFR
|
Cancer
|
Osimertinib mesylate (AZD-9291 mesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
|
-
- HY-101870B
-
INCB053914 phosphate
|
Pim
|
Cancer
|
INCB053914 phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. INCB053914 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
|
-
- HY-136057
-
iFSP1
|
Ferroptosis
|
Cancer
|
iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A).
|
-
- HY-16918
-
Heptamidine
SBi4211
|
Others
|
Cancer
Inflammation/Immunology
|
Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).
|
-
- HY-N2993
-
Polyporenic acid C
|
Apoptosis
|
Cancer
|
Polyporenic acid C is a lanostane-type triterpenoid isolated from P. cocos. Polyporenic acid C induces cell apoptosis through the death receptor-mediated apoptotic pathway without the involvement of the mitochondria. Polyporenic acid C is promising agent for lung cancer therapy.
|
-
- HY-N6036
-
Ganoderic acid F
|
Others
|
Cancer
|
Ganoderic acid F is a ganoderic acid. Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum stress.
|
-
- HY-B0497B
-
-
- HY-P1064A
-
Apelin-36(human) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-13775
-
XL019
|
JAK
Apoptosis
|
Cancer
|
XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
|
-
- HY-12502A
-
-
- HY-131055
-
Mytoxin B
|
ADC Cytotoxin
PI3K
Apoptosis
|
Cancer
|
Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002 (HY-10108). Mytoxin B induces cell apoptosis via PI3K/Akt pathway.
|
-
- HY-121537
-
CAY10404
|
COX
Akt
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.
|
-
- HY-131296
-
5-A-RU-PABC-Val-Cit-Fmoc
|
Others
|
Inflammation/Immunology
|
5-A-RU-PABC-Val-Cit-Fmoc is the prodrug of 5-A-RU. 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
|
-
- HY-15730
-
Poziotinib
HM781-36B; NOV120101
|
EGFR
Apoptosis
|
Cancer
|
Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.
|
-
- HY-123076
-
Pifithrin-α, p-Nitro, Cyclic
PFN-α
|
MDM-2/p53
|
Neurological Disease
|
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
|
-
- HY-113846
-
CMP-5 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|
-
- HY-113498
-
Sphingomyelin
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
Sphingomyelin is a eukaryotic sphingolipid and one of the major constituents of cell membranes and particularly abundant in the myelin sheath that surrounds neuronal axons. Sphingomyelin plays an important role in cell processes, the regulation of inflammatory responses, and signal transduction. Sphingomyelin metabolism is associated with various central nervous system diseases and Niemann–Pick disease.
|
-
- HY-100490A
-
Rilmenidine hemifumarate
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-128587
-
Mevociclib
SY-1365
|
CDK
|
Cancer
|
Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
|
-
- HY-125035
-
LCH-7749944
GNF-PF-2356
|
PAK
Apoptosis
|
Cancer
|
LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis.
|
-
- HY-N0226
-
Epiberberine
|
AChE
Beta-secretase
|
Metabolic Disease
Neurological Disease
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberinecan be used for the research of diabetic disease.
|
-
- HY-N0226A
-
Epiberberine chloride
|
AChE
Beta-secretase
Reactive Oxygen Species
|
Metabolic Disease
Neurological Disease
|
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Epiberberine has the potential effect in the research of diabetic disease.
|
-
- HY-16918A
-
Heptamidine dimethanesulfonate
SBi4211 dimethanesulfonate
|
Others
|
Cancer
Inflammation/Immunology
|
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).
|
-
- HY-13919
-
Napabucasin
|
STAT
|
Cancer
|
Napabucasin is a STAT3 inhibitor which blocks stem cell activity in cancer cells.
|
-
- HY-B1776
-
Spermidine
|
Endogenous Metabolite
|
Metabolic Disease
|
Spermidine maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine significantly decreases the H2O2 and O2 .- contents.
|
-
- HY-107846
-
Xylan
|
Others
|
Others
|
Xylan represents the main hemicellulose component in the secondary plant cell walls of flowering plants. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose.
|
-
- HY-B1776A
-
Spermidine trihydrochloride
|
Others
|
Metabolic Disease
|
Spermidine trihydrochloride maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine trihydrochloride significantly decreases the H2O2 and O2 .- contents.
|
-
- HY-100734
-
-
- HY-19694
-
BRD7552
|
Others
|
Endocrinology
|
BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function.
|
-
- HY-10183
-
-
- HY-15772
-
Osimertinib
AZD-9291; Mereletinib
|
EGFR
|
Cancer
|
Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
|
-
- HY-79077
-
Osimertinib dimesylate
AZD-9291 dimesylate; Mereletinib dimesylate
|
EGFR
|
Cancer
|
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
|
-
- HY-133654
-
2,3,3-Tribromopropenoic acid
|
Others
|
Others
|
2,3,3-Tribromopropenoic acid is a 2,3,3-Tribromo product based on propenoic acid. 2,3,3-Tribromopropenoic acid is a polar aromatic brominated disinfection byproduct during chlorination in water and shows cytotoxic potency in mammalian cell chronic cytotoxicity experiments.
|
-
- HY-16219
-
Gadoxetate Disodium
Gd-EOB-DTPA Disodium; ZK 139834
|
Others
|
Cancer
|
Gadoxetate Disodium (Gd-EOB-DTPA Disodium) is a contrast agent in magnetic resonance imaging (MRI) of the hepatobiliary system, which accumulates in normal, functioning hepatocytes. Gadoxetate Disodium (Gd-EOB-DTPA Disodium) is used to evaluate focal liver lesions, such as hepatocellular carcinoma or liver metastasis on T1-weighted imaging.
|
-
- HY-13801
-
Fexinidazole
HOE 239
|
Parasite
|
Infection
|
Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal drug. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC50s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.
|
-
- HY-W052512
-
Antitrypanosomal agent 1
|
Parasite
|
Infection
|
Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor with an IC50 of 3.3 μM. Antitrypanosomal agent 1 inhibits glutathione reductase (GR) (IC50=64.8 μM) and T. brucei (EC50=1 μM). Antitrypanosomal agent 1 has anti-trypanosomal activity.
|
-
- HY-75564
-
Cyclo(Ala-Gly)
|
Endogenous Metabolite
|
Cancer
|
Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM.
|
-
- HY-12755
-
ML141
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.
|
-
- HY-120137
-
CMP-5
|
Histone Methyltransferase
|
Cancer
|
CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|
-
- HY-128206
-
I3MT-3
HMPSNE
|
Hippo (MST)
|
Metabolic Disease
|
I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.
|
-
- HY-108556
-
RWJ-56110
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
|
-
- HY-106571
-
-
- HY-N1957
-
Gamma-Mangostin
γ-Mangostin
|
5-HT Receptor
|
Metabolic Disease
|
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 µM) .
|
-
- HY-132073
-
-
- HY-Y0248A
-
-
- HY-121087
-
BCI-215
|
Phosphatase
|
Cancer
|
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.
|
-
- HY-15666
-
GZD824
HQP1351
|
Bcr-Abl
|
Cancer
|
GZD824 (HQP1351) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity.
|
-
- HY-19832
-
SC66
|
Akt
Apoptosis
|
Cancer
|
SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
- HY-114410
-
CCI-006
|
Mitochondrial Metabolism
|
Cancer
|
CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells.
|
-
- HY-134130
-
Integrin modulator 1
|
Integrin
|
Inflammation/Immunology
|
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
|
-
- HY-50514
-
AT9283
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
|
-
- HY-N2230
-
N-p-trans-Coumaroyltyramine
|
AChE
|
Infection
Neurological Disease
|
N-p-trans-Coumaroyltyramine is a cinnamoylphenethyl amide isolated from polygonum hyrcanicum, acts as an acetylcholinesterase (AChE) inhibitor with an an IC50 of 122 μM. N-p-trans-Coumaroyltyramine exhibits anti-trypanosomal activity with an IC50 of 13.3 µM for T. brucei rhodesiense.
|
-
- HY-10261A
-
Afatinib dimaleate
BIBW 2992MA2
|
EGFR
Autophagy
|
Cancer
|
Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
|
-
- HY-W010791
-
Adenosine 5'-diphosphate sodium salt
|
Endogenous Metabolite
|
Others
|
Adenosine 5'-diphosphate (ADP) sodium salt is a nucleoside diphosphate, which is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate sodium salt induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
|
-
- HY-W010918
-
Adenosine 5'-diphosphate
Adenosine diphosphate; ADP
|
Endogenous Metabolite
|
Others
|
Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
|
-
- HY-13306
-
Pyrintegrin
|
Integrin
|
Metabolic Disease
|
Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.
|
-
- HY-N7255
-
Cycloartenol
|
p38 MAPK
Apoptosis
|
Cancer
|
Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development.
|
-
- HY-19331
-
WZB117
|
GLUT
|
Cancer
|
WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
|
-
- HY-103637
-
Vimirogant
VTP-43742
|
ROR
|
Inflammation/Immunology
|
Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research.
|
-
- HY-103637A
-
Vimirogant hydrochloride
VTP-43742 hydrochloride
|
ROR
|
Inflammation/Immunology
|
Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.
|
-
- HY-U00087
-
Tosylchloramide sodium trihydrate
|
Bacterial
|
Infection
|
Tosylchloramide sodium trihydrate (Chloramine T sodium trihydrate) is a disinfectant agent widely used in laboratories, kitchens and hospitals. It is also used as a biocide in air fresheners and deodorants.
|
-
- HY-113338
-
-
- HY-N1713
-
-
- HY-W015399
-
4-Methylcinnamic acid
|
Fungal
|
Infection
|
4-Methylcinnamic acid, a Cinnamic acid analog, can be used as a intervention catalyst for overcoming antifungal tolerance. 4-Methylcinnamic acid can improve the potency of cell wall-disrupting agents.
|
-
- HY-N2028
-
Demethylwedelolactone
|
Others
|
Cancer
|
Demethylwedelolactone is a naturally occurring coumestan isolated from Eclipta alba. Demethylwedelolactone is a potent trypsin inhibitor with an IC50 of 3.0 μM. Demethylwedelolactone suppresses cell motility and cell invasion of breast cancer cell.
|
-
- HY-W011404
-
Tributyrin
Glyceryl tributyrate
|
Apoptosis
|
Metabolic Disease
|
Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
|
-
- HY-129529
-
6-Hydroxyluteolin 7-glucoside
|
Others
|
Inflammation/Immunology
|
6-Hydroxyluteolin 7-glucoside is a flavonoid from Tanacetum parthenium and T. vulgare. 6-Hydroxyluteolin 7-glucoside inhibits the major pathways of arachidonate metabolism in leukocytes. 6-Hydroxyluteolin 7-glucoside has anti-inflammatory effect.
|
-
- HY-10261
-
Afatinib
BIBW 2992
|
EGFR
Autophagy
|
Cancer
|
Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
|
-
- HY-112608
-
CHMFL-PI3KD-317
|
PI3K
|
Cancer
|
CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
|
-
- HY-13915
-
NSC348884
|
Apoptosis
|
Cancer
|
NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.
|
-
- HY-P1185
-
Antagonist G
|
Vasopressin Receptor
Apoptosis
|
Cancer
|
Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
|
-
- HY-123905
-
LIN28 inhibitor LI71
|
MicroRNA
|
Cancer
|
LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells.
|
-
- HY-116894
-
Rotundifuran
|
Apoptosis
|
Cancer
|
Rotundifuran, a labdane type diterpene, is isolated from Vitex rotundifolia. Rotundifuran can inhibit the cell cycle progression and induce apoptosis in human myeloid leukaemia cells.
|
-
- HY-19619
-
m-3M3FBS
|
Phospholipase
Apoptosis
|
Cancer
|
m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis.
|
-
- HY-P1185A
-
-
- HY-10046
-
-
- HY-140510
-
-
- HY-10388
-
-
- HY-50908
-
Ridaforolimus
MK-8669; Deforolimus; AP23573
|
mTOR
Autophagy
|
Cancer
|
Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
|
-
- HY-N7019
-
19-Hydroxybufalin
|
Others
|
Cancer
|
19-Hydroxybufalin is a bufadienolide, inhibits epithelial-mesenchymal transition and attenuates the migration and invasion of PC3 cells.
|
-
- HY-125965
-
BioA-IN-13
|
Bacterial
|
Infection
|
BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.
|
-
- HY-B0862
-
Pendimethalin
|
Others
|
Others
|
Pendimethalin is an herbicide that controls annual grasses and certain broadleaf weeds. Pendimethalin inhibits cell division and cell elongation.
|
-
- HY-W013699
-
Chlorhexidine diacetate
|
Bacterial
Antibiotic
|
Infection
|
Chlorhexidine diacetate is a biguanide disinfectant with rapid bactericidal activity against both Gram-positive and Gram-negative organism. The antibacterial effect of chlorhexidine diacetate is related to its action on the bacterial cell membrane and to precipitation of intracellular contents.
|
-
- HY-B0986
-
Hexylresorcinol
4-Hexylresorcinol
|
Parasite
Bacterial
Apoptosis
Glucosidase
|
Cancer
Infection
Metabolic Disease
|
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
|
-
- HY-P1201
-
Cyclosomatostatin
|
Somatostatin Receptor
|
Cancer
|
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-113950
-
-
- HY-15518
-
LCL161
|
IAP
|
Cancer
|
LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
|
-
- HY-17362
-
Vancomycin hydrochloride
|
Bacterial
Autophagy
Antibiotic
|
Infection
Cancer
|
Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria. Vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis.
|
-
- HY-100395
-
F16
|
Apoptosis
|
Cancer
|
F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
|
-
- HY-10583
-
Y-27632 dihydrochloride
|
ROCK
Apoptosis
|
Cancer
|
Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
|
-
- HY-108556A
-
RWJ-56110 dihydrochloride
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
|
-
- HY-119944
-
JND3229
|
EGFR
|
Cancer
|
JND3229 is a highly potent and fourth-generation EGFR C797S reversible inhibitor with IC50 value of 5.8 nM, and also potently suppressed EGFR L858R/T790M and EGFR WT with IC50 values of 30.5 and 6.8 nM.
|
-
- HY-N5072
-
Desmethylglycitein
4',6,7-Trihydroxyisoflavone
|
CDK
PI3K
PKC
|
Cancer
|
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.
Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
|
-
- HY-B1378
-
-
- HY-N7798
-
Pennogenin
|
Others
|
Inflammation/Immunology
|
Pennogenin is a bioactive component which can be isolated from T. govanianum rhizomes. Pennogenin exhibits significant in vitro inhibitory effect on release of ROS.
|
-
- HY-W008344
-
2-Chloroadenosine
|
Others
|
Others
|
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.
|
-
- HY-109566
-
-
- HY-N0438
-
Pimpinellin
|
Apoptosis
|
Cancer
|
Pimpinellin is a constituent of Cyrtomium fortumei (J.). Pimpinellin inhibits the growth of tumor cells via the induction of tumor cell apoptosis.
|
-
- HY-114313
-
-
- HY-100036
-
MK-4101
|
Smo
Apoptosis
Hedgehog
|
Cancer
|
MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.
|
-
- HY-100195
-
SAR-020106
|
Checkpoint Kinase (Chk)
|
Cancer
|
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer drugs.
|
-
- HY-P1065
-
Apelin-36(rat, mouse)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- HY-P1201A
-
Cyclosomatostatin TFA
|
Somatostatin Receptor
|
Cancer
|
Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-112314
-
AZD0424
|
Src
Bcr-Abl
Apoptosis
|
Cancer
|
AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
|
-
- HY-W019870A
-
Glufosinate
|
Others
|
Neurological Disease
|
Glufosinate, a phosphinic acid analogue of glutamic acid, is a herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate exerts neurotoxic activity.
|
-
- HY-138537
-
NF-κB-IN-1
|
IKK
|
Cancer
|
NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.
|
-
- HY-122502
-
Pyrazofurin
|
DNA/RNA Synthesis
|
Cancer
|
Pyrazofurin, a pyrimidine nucleoside analogue with antineoplastic activity, inhibits cell proliferation and DNA synthesis in cells by inhibiting uridine 5'-phosphate (UMP) synthase. Pyrazofurin is an active, sensitive orotate-phosphoribosyltransferase inhibitor with IC50s between 0.06-0.37 µM in the three squamous cell carcinoma (SCC) cell lines Hep-2, HNSCC-14B and HNSCC-14C.
|
-
- HY-121018
-
Daltroban
BM-13505; SKF 96148
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury.
|
-
- HY-15826
-
-
- HY-15666A
-
GZD824 dimesylate
HQP1351 dimesylate
|
Bcr-Abl
|
Cancer
|
GZD824 dimesylate (HQP1351 dimesylate) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 dimesylate has antitumor activity.
|
-
- HY-12826
-
IMB-XH1
|
Bcl-2 Family
Bacterial
|
Cancer
|
IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1). IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively.
|
-
- HY-135784
-
OSMI-2
|
Acyltransferase
|
Metabolic Disease
|
OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.
|
-
- HY-U00177
-
GDP366
|
Survivin
|
Cancer
|
GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
|
-
- HY-15184
-
Elaiophylin
Azalomycin B; Gopalamicin; Efomycin E
|
Autophagy
|
Cancer
|
Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
|
-
- HY-114926
-
KT185
|
MAGL
|
Neurological Disease
|
KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
|
-
- HY-112716
-
-
- HY-19637
-
SW044248
|
Topoisomerase
|
Cancer
|
SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
|
-
- HY-136383
-
AZA1
Rac1/Cdc42-IN-1
|
Ras
Apoptosis
|
Cancer
|
AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.
|
-
- HY-P0119A
-
-
- HY-P0119
-
-
- HY-111815A
-
-
- HY-19835
-
LY2922470
|
GPR40
|
Metabolic Disease
|
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
|
-
- HY-15771A
-
Tirabrutinib hydrochloride
ONO-4059 hydrochloride; GS-4059 hydrochloride
|
Btk
|
Cancer
|
Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.
|
-
- HY-10126
-
Barasertib-HQPA
AZD2811; INH-34; AZD1152-HQPA
|
Aurora Kinase
Apoptosis
|
Cancer
|
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.
|
-
- HY-N1419
-
Vaccarin
|
AMPK
|
Metabolic Disease
|
Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.
|
-
- HY-15861
-
Targapremir-210
TGP-210
|
MicroRNA
Apoptosis
|
Cancer
|
Targapremir-210 (TGP-210) is a potent and selective miR-210 inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM).
|
-
- HY-16697
-
CID 16020046
|
GPR55
|
Cancer
|
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.
|
-
- HY-110193
-
SPP-86
|
RET
|
Cancer
|
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
|
-
- HY-21141
-
Cysteine protease inhibitor-2
|
Cathepsin
|
Cancer
|
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
|
-
- HY-15648F
-
GSK-J4 hydrochloride
|
Histone Demethylase
|
Cancer
|
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.
|
-
- HY-112062
-
POL1-IN-1
|
DNA/RNA Synthesis
|
Cancer
|
POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.
|
-
- HY-135805A
-
(Rac)-JBJ-04-125-02
|
EGFR
|
Cancer
|
(Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M.
|
-
- HY-15772S
-
Osimertinib D6
AZD-9291 D6; Mereletinib D6
|
EGFR
|
Cancer
|
Osimertinib D6 (AZD-9291 D6) is a deuterium labeled Osimertinib. Osimertinib is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
|
-
- HY-W012009
-
2'-Deoxy-2'-fluorocytidine
|
Influenza Virus
|
Infection
|
2'-Deoxy-2'-fluorocytidine, an nucleoside analog, is a potent inhibitor of Crimean-Congo hemorrhagic fever virus (CCHFV) replication. 2′-deoxy-2′-fluorocytidine can act synergistically with T705 to increase the potency of both compounds antiviral effects on CCHFV replication.
|
-
- HY-18213
-
EGFR-IN-9
|
EGFR
|
Cancer
|
EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.
|
-
- HY-N2008
-
-
- HY-133780
-
Afatinib impurity 11
|
EGFR
Autophagy
|
Cancer
|
Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively.
|
-
- HY-112301
-
Pralsetinib
BLU-667
|
RET
|
Cancer
|
Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively.
|
-
- HY-126020
-
Bractoppin
|
DNA/RNA Synthesis
RAD51
|
Cancer
|
Bractoppin is a potent and selective drug-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response.
|
-
- HY-12743A
-
-
- HY-12743
-
K-7174
|
Others
|
Inflammation/Immunology
|
K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
|
-
- HY-114503
-
NSAH
|
DNA/RNA Synthesis
|
Cancer
|
NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively.
|
-
- HY-101055
-
Kinetin riboside
N6-Furfuryladenosine
|
Apoptosis
|
Cancer
|
Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM.
|
-
- HY-101524
-
-
- HY-W019870
-
Glufosinate ammonium
|
Others
|
Neurological Disease
|
Glufosinate ammonium, a phosphinic acid analogue of glutamic acid, is an herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate ammonium exerts neurotoxic activity.
|
-
- HY-P1065A
-
Apelin-36(rat, mouse) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- HY-15295
-
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-108716
-
CBS9106
SL-801
|
CRM1
Apoptosis
|
Cancer
|
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells.
|
-
- HY-103489
-
PI-273
|
PI4K
Apoptosis
|
Cancer
|
PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
|
-
- HY-10388A
-
-
- HY-100007
-
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-15304
-
-
- HY-P0151
-
-
- HY-12797
-
GF 15
|
Others
|
Cancer
|
GF 15 is a potent inhibitor of centrosomal clustering in tumor cells.
|
-
- HY-103359
-
Ceranib1
|
Others
|
Cancer
|
Ceranib1 is a ceramidase inhibitor. Ceranib1 inhibits ceramidase activity toward an exogenous ceramide analog, induces the accumulation of multiple ceramide species, decreases levels of sphingosine and S1P. Ceranib1 inhibits the proliferation of ovarian cancer cells.
|
-
- HY-112914
-
-
- HY-10127
-
Barasertib
AZD1152
|
Aurora Kinase
Apoptosis
|
Cancer
|
Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.
|
-
- HY-15694
-
SMIP004
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
|
-
- HY-135785
-
OSMI-3
|
Acyltransferase
|
Metabolic Disease
|
OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.
|
-
- HY-15004
-
AUZ 454
K03861
|
CDK
|
Cancer
|
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
|
-
- HY-118224
-
BPH-715
|
Parasite
|
Infection
|
BPH-715 is a bisphosphonate, inhibits Plasmodium liver-stage growth, with an IC50 of 10 μM for Plasmodium exoerythrocytic forms in HepG2 cells.
|
-
- HY-114322
-
VZ185
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
VZ185 is a potent, fast, and selective VHL based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively.
|
-
- HY-N2292
-
Kinsenoside
|
Keap1-Nrf2
Apoptosis
|
Inflammation/Immunology
|
Kinsenoside is a main active component isolated from plants of the genus Anoectochilus, and exhibits many biological activities and pharmacological effects. Kinsenoside rescues the nucleus pulposus cells (NPCs) viability under oxidative stress and protects against apoptosis, senescence and mitochondrial dysfunction in a Nrf2-dependent way.
|
-
- HY-Y0445A
-
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-10846
-
-
- HY-15700
-
-
- HY-16662
-
Oncrasin-1
|
Ras
Apoptosis
|
Cancer
|
Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation
of PKCι in nucleus of sensitive cells but not in resistant cells.
|
-
- HY-17511
-
Potassium oxonate
Potassium azaorotate; Potassium otastat
|
Others
|
Metabolic Disease
|
Potassium oxonate is an inhibitor of uricase, inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.
|
-
- HY-N6745
-
Citreoviridin
|
Na+/K+ ATPase
Apoptosis
|
Infection
Cardiovascular Disease
|
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner. Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells.
|
-
- HY-119738
-
OSMI-1
|
Acyltransferase
|
Metabolic Disease
|
OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.
|
-
- HY-12458
-
Pyrindamycin A
|
DNA/RNA Synthesis
|
Cancer
Infection
|
Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
|
-
- HY-B1548
-
Benznidazol
Ro 07-1051; Ro 71051
|
Parasite
|
Infection
|
Benznidazol (Ro 07-1051) is an antiparasitic medication, with an IC50 of 20.35 μM for Colombian T. cruzi strains, and has been used in the treatment of Chagas disease.
|
-
- HY-112723
-
-
- HY-110115
-
TC-Mps1-12
|
Mps1
|
Cancer
|
TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM.
|
-
- HY-B0817
-
Pyridaben
|
Parasite
|
Infection
|
Pyridaben is a METI acaricide that inhibits mitochondrial electron transport at complex I (METI; Ki = 0.36 nmol/mg protein in rat brain mitochondria). Pyridaben is active against a variety of mites, inducing 100% mortality of C. malaccensis, D. farina, and T. putrescentia when administered via filter paper contact at doses of 25, 100, and 200 mg/mL, respectively.
|
-
- HY-128778
-
DBPR112
|
EGFR
|
Cancer
|
DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy.
|
-
- HY-N0162
-
Luteolin
Luteoline; Luteolol; Digitoflavone
|
Keap1-Nrf2
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
|
Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
|
-
- HY-N1931
-
Epifriedelanol
|
Others
|
Cancer
|
Epifriedelanol is a triterpenoid isolated from the root bark of Ulmus davidiana, with antitumor activity. Epifriedelanol inhibits cellular senescence in human primary cells.
|
-
- HY-124632
-
WJ460
|
Others
|
Cancer
|
WJ460 is a potent myoferlin (MYOF) inhibitor, which interacts directly with MYOF and exerts anti-metastatic activity in the nanomolar range in breast cancer cells.
|
-
- HY-N6602
-
α-Solanine
|
Apoptosis
|
Cancer
|
α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in potatoes, has been observed to inhibit growth and induce apoptosis in cancer cells.
|
-
- HY-A0068
-
Aurothioglucose
Gold thioglucose
|
Others
|
Cancer
|
Aurothioglucose (Gold thioglucose) is a well known active-site inhibitor of TrxR1, inhibited TrxR1 activity in HeLa cell cytosol but had no effect on the viability of the cells.
|
-
- HY-N6862
-
Lucideric acid A
|
MMP
|
Cancer
|
Lucideric acid A is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
|
-
- HY-13668
-
-
- HY-N2420
-
Flavokawain A
|
Apoptosis
|
Cancer
|
Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer.
|
-
- HY-N6727
-
Gliotoxin
Aspergillin
|
Apoptosis
PKA
NF-κB
Bacterial
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
|
-
- HY-18944
-
FIT-039
|
CDK
HSV
CMV
DNA/RNA Synthesis
|
Infection
|
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
|
-
- HY-N0504
-
-
- HY-10222
-
Ixabepilone
BMS-247550; Aza-epothilone B
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
|
-
- HY-135383B
-
(Z)-Pitavastatin calcium
|
Others
|
Metabolic Disease
|
(Z)-Pitavastatin calcium is the Z-Isomer of Pitavastatin hemicacium. Pitavastatin calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin calcium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.
|
-
- HY-N6782
-
Oligomycin
|
ATP Synthase
Fungal
Antibiotic
|
Cancer
Infection
|
Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
|
-
- HY-131187
-
BMS-1166-N-piperidine-COOH
|
Ligand for Target Protein for PROTAC
|
Cancer
|
BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-10498
-
Lexibulin
CYT-997
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells.
|
-
- HY-10498A
-
Lexibulin dihydrochloride
CYT-997 dihydrochloride
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
Lexibulin dihydrochloride (CYT-997 dihydrochloride) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin dihydrochloride induces cell apoptosis and induces mitochondrial ROS generation in GC cells.
|
-
- HY-B1596
-
-
- HY-18965
-
-
- HY-100498
-
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-18679
-
TC-N 22A
|
mGluR
|
Neurological Disease
|
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
|
-
- HY-N0171A
-
-
- HY-138239
-
WEE1-IN-3
|
Wee1
|
Cancer
|
WEE1-IN-3 is a potent Wee1 kinase inhibitor with an IC50 of <10 nM. WEE1-IN-3 has anticancer activities.
|
-
- HY-121497
-
3-Methoxybenzamide
3-MBA
|
PARP
Bacterial
|
Cancer
|
3-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells. 3-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum).
|
-
- HY-17371
-
Oxaliplatin
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Autophagy
|
Cancer
|
Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
|
-
- HY-121802
-
Dynarrestin
|
Hedgehog
|
Cancer
|
Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells.
|
-
- HY-13721
-
Phenoxodiol
Idronoxil; Dehydroequol; Haginin E
|
Caspase
Apoptosis
Topoisomerase
|
Cancer
|
Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner.
|
-
- HY-16658B
-
Z-VAD-FMK
Z-VAD(OH)-FMK
|
Caspase
|
Cancer
|
Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM.
|
-
- HY-N6744
-
Chaetoglobosin A
|
Apoptosis
|
Cancer
Infection
|
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration.
|
-
- HY-77813
-
-
- HY-111425
-
SSE15206
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
|
-
- HY-120215
-
KT203
|
MAGL
|
Metabolic Disease
|
KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
|
-
- HY-N6860
-
Lucidenic acid C
|
MMP
|
Cancer
|
Lucidenic acid C is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
|
-
- HY-100636
-
Gefitinib N-oxide
|
EGFR
|
Cancer
|
Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
|
-
- HY-120177
-
KT182
|
MAGL
|
Others
|
KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
|
-
- HY-12873
-
RBC8
|
Ras
|
Cancer
|
RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
|
-
- HY-B0497
-
Niclosamide
BAY2353
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
|
-
- HY-127002A
-
Squarunkin A hydrochloride
|
Src
|
Cancer
|
Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.
|
-
- HY-119222
-
GSK256073
|
GPR109A
|
Metabolic Disease
|
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
|
-
- HY-140156
-
-
- HY-140616
-
-
- HY-141328
-
-
- HY-140154
-
-
- HY-141327
-
-
- HY-140155
-
-
- HY-126679
-
Apoptolidin
|
ATP Synthase
Apoptosis
|
Cancer
|
Apoptolidin is a polyketide isolated from Nocardiopsis bacteria. Apoptolidin is a selective mitochondrial F1FO ATPase inhibitor. Apoptolidin is an apoptosis inducer and induces apoptotic cell death in cells transformed with the adenovirus type 12 oncogenes including ElA (IC50=10-17 ng/ml) but not in normal cells.
|
-
- HY-134582
-
dCBP-1
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
|
-
- HY-106420
-
-
- HY-P1629
-
Temporin A
|
Bacterial
Fungal
Antibiotic
|
Infection
|
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans).
|
-
- HY-P0069A
-
-
- HY-P1286
-
-
- HY-B0313
-
-
- HY-B1300
-
-
- HY-21972
-
-
- HY-18632A
-
-
- HY-15648B
-
GSK-J4
|
Histone Demethylase
Apoptosis
|
Cancer
|
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
|
-
- HY-B0793
-
AZ-5104
|
EGFR
|
Cancer
|
AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFR L858R/T790M, EGFR L858R, EGFR L861Q, EGFR and ErbB4, respectively.
|
-
- HY-W010254
-
4′-Hydroxy-2′-methylacetophenone
|
Parasite
|
Infection
|
4′-Hydroxy-2′-methylacetophenone, an aroma compound of red wines, is isolated from cv. Bobal grape variety. 4′-Hydroxy-2′-methylacetophenone has ciliate toxicity. 4′-Hydroxy-2′-methylacetophenone inhibits the growth of T. pyriformis, with an IC50 of 0.65 mM.
|
-
- HY-B0790
-
TAI-1
|
Apoptosis
|
Cancer
|
TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
|
-
- HY-N2486
-
-
- HY-118660
-
Anhydrotetracycline hydrochloride
|
Antibiotic
Bacterial
|
Infection
|
Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells.
|
-
- HY-12425
-
-
- HY-N3558
-
Ceanothic acid
Emmolic acid
|
Others
|
Cancer
|
Ceanothic acid (Emmolic acid) is a ring-A homologue of betulinic acid. Ceanothic acid inhibits OVCAR-3, HeLa, and FS-5 cells with the cell survival of 68%, 65%, and 81%, respectively.
|
-
- HY-12842
-
UC-112
|
IAP
Apoptosis
|
Cancer
|
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
|
-
- HY-136351
-
THZ-P1-2
|
Autophagy
|
Cancer
|
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.
|
-
- HY-N1924
-
Crassicauline A
Crassicaulin A
|
Others
|
Neurological Disease
|
Crassicauline A (Crassicaulin A) is a bioactive alkaloid found in roots of Aconitum carmichaeli. Crassicauline A (Crassicaulin A) possesses feeding deterrent activity against T. castaneum adults with an EC50 of 1134.5 ppm.
|
-
- HY-120836
-
AOH1160
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells.
|
-
- HY-15609
-
-
- HY-117650A
-
RG7834
RO 7020322
|
HBV
|
Infection
|
RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells.
|
-
- HY-106101
-
Echinomycin
Quinomycin A; NSC-13502
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
|
-
- HY-120548
-
KBU2046
|
Others
|
Cancer
|
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life.
|
-
- HY-N0674A
-
Dehydrocorydaline chloride
13-Methylpalmatine chloride
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Cancer
Infection
|
Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
|
-
- HY-N0674
-
Dehydrocorydaline
13-Methylpalmatine
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Cancer
Infection
|
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
|
-
- HY-12462
-
WS3
|
Others
|
Inflammation/Immunology
|
WS3 is a novel proliferative molecule that promotes pancreatic β cell proliferation in rodent and human primary islets. WS3 can be used for the research of type 1 diabetes.
|
-
- HY-126378
-
LSP-249
|
Others
|
Inflammation/Immunology
|
LSP-249 (example 35), extracted from patent WO2016011209A1, is a plasma kallikrein inhibitor under the study for angioedema, with an EC50 less than 100 nM in cell.
|
-
- HY-N4219
-
-
- HY-15894
-
-
- HY-N1516
-
Ganoderenic acid D
|
Apoptosis
|
Cancer
|
Ganoderenic acid D is a triterpene identified from the effective compounds of Ganoderma lucidum extract (GLE). Ganoderenic acid D inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
|
-
- HY-122214
-
AC-73
|
Autophagy
|
Cancer
|
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells. AC-73 is also an anti-proliferative drug and an inducer of autophagy in leukemic cells.
|
-
- HY-A0098
-
Tunicamycin
|
Bacterial
Fungal
Influenza Virus
Antibiotic
|
Cancer
Infection
Inflammation/Immunology
|
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.Tunicamycin increases exosome release in cervical cancer cells.
|
-
- HY-101567
-
BMS-986158
|
Epigenetic Reader Domain
|
Cancer
|
BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
|
-
- HY-103002
-
SU5408
VEGFR2 Kinase Inhibitor I
|
VEGFR
|
Cardiovascular Disease
|
SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
|
-
- HY-117102
-
ANI-7
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
|
-
- HY-B0496
-
PMSF
Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride
|
Cathepsin
|
Others
|
PMSF is an irreversible serine/cysteine protease inhibitor commonly used in the preparation of cell lysates.
|
-
- HY-13307
-
JK184
|
Hedgehog
|
Cancer
|
JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
|
-
- HY-16695
-
-
- HY-100755
-
-
- HY-P1286A
-
-
- HY-129337
-
Reveromycin A
|
Antibiotic
Fungal
Apoptosis
|
Cancer
Infection
|
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
|
-
- HY-108900
-
Leu-AMS
|
Aminoacyl-tRNA Synthetase
Bacterial
|
Cancer
Infection
|
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
|
-
- HY-112256
-
-
- HY-32340
-
Lexacalcitol
KH1060
|
VD/VDR
|
Cancer
Inflammation/Immunology
|
Lexacalcitol (KH1060), a vitamin D analog, is potent regulators of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases.
|
-
- HY-14590
-
-
- HY-50895S
-
Gefitinib D8
ZD1839 D8
|
EGFR
Autophagy
|
Cancer
|
Gefitinib D8 (ZD1839 D8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
|
-
- HY-101413
-
Iberin
NSC 321801
|
Apoptosis
Endogenous Metabolite
Bacterial
|
Cancer
|
Iberin (NSC 321801), a sulfoxide analogue of sulforaphane, is a naturally occurring member of isothiocyanate family. Iberin inhibits cell survival with an IC50 of 2.3 μM in HL60 cell. Iberin induces apoptosis.
|
-
- HY-128522
-
ARS-1323-alkyne
|
Ras
|
Cancer
|
ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS G12C nucleotide state in living cells.
|
-
- HY-N0726
-
Dracorhodin perchlorate
Dracohodin perochlorate
|
Apoptosis
|
Cancer
|
Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product extracted from a natural medicine Dragon's blood. Dracorhodin perchlorate inhibits cell proliferation and induces cell cycle arrest and apoptosis.
|
-
- HY-N4285
-
-
- HY-112055
-
DIM-C-pPhOH
|
Apoptosis
|
Cancer
|
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
|
-
- HY-137658
-
Purine riboside triphosphate
PTP
|
Nucleoside Antimetabolite/Analog
|
Others
|
Purine riboside triphosphate is a triphosphate derivative of purine riboside. Purine riboside is a naturally occurring base analog which closely resembles adenosine. Purine riboside inhibits carcinogenic growth. Purine riboside strongly inhibits RNA and DNA synthesis in different cancer ascites cells.
|
-
- HY-119751
-
Hematein
|
Casein Kinase
Akt
Wnt
Apoptosis
|
Cancer
|
Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.
|
-
- HY-13065
-
Isobavachalcone
Corylifolinin; Isobacachalcone
|
Akt
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.
|
-
- HY-129065
-
Nourseothricin sulfate
Streptothricin sulfate
|
Fungal
Bacterial
Antibiotic
|
Infection
|
Nourseothricin sulfate (Streptothricin sulfate) is a broad-spectrum antibiotic that destroys the outer membrane of Gram-negative bacteria and is a dominant selective marker for Fonsecaea pedrosoi. Nourseothricin sulfate inhibits protein biosynthesis in prokaryotic cells and strongly inhibits the growth of eukaryotes like fungi and can also be used as a elective marker for a wide range of organisms including bacteria, yeast, filamentous fungi, and plant cells.
|
-
- HY-12726A
-
-
- HY-12726
-
-
- HY-N7654
-
(-)-Epipodophyllotoxin
|
Apoptosis
|
Cancer
|
(-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro.
|
-
- HY-119940
-
MC180295
(rel)-MC180295
|
CDK
|
Cancer
|
MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
|
-
- HY-116282D
-
-
- HY-116282C
-
-
- HY-116282A
-
-
- HY-N6644
-
Crocin III
|
Others
|
Cancer
Inflammation/Immunology
|
Crocin III is a crocetin from saffron (Crocus sutivus L.). Crocetins inhibit cell growth of tumor cells and has anti-inflammatory activity. Crocins serve as spices and coloring agents.
|
-
- HY-116282B
-
-
- HY-19095
-
TNP-351
|
Antifolate
|
Cancer
|
TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
|
-
- HY-120635
-
-
- HY-131036
-
MAO-IN-M30 dihydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease.
|
-
- HY-115537
-
NAE-IN-M22
|
Apoptosis
|
Cancer
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
|
-
- HY-10585A
-
Valproic acid sodium salt
Sodium Valproate
|
HDAC
Autophagy
Mitophagy
HIV
Notch
|
Cancer
|
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
|
-
- HY-100415
-
UKI-1
UKI-1C
|
PAI-1
Ser/Thr Protease
|
Infection
Cancer
|
UKI-1 (UKI-1C) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells.
|
-
- HY-N2567
-
(±)-Decursinol
|
Bacterial
|
Cancer
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-19324
-
-
- HY-19563
-
-
- HY-12053A
-
-
- HY-D0850
-
Tartaric acid disodium dihydrate
Sodium tartrate dibasic dihydrate; Sodium tartrate dihydrate
|
Phosphatase
|
Cancer
|
Tartaric acid disodium dihydrate is a Acid phosphatase inhibitor, is a sodium salt used in buffers for molecular biology and cell culture applications.
|
-
- HY-13541
-
ADH-1
|
Others
|
Cancer
|
ADH-1, an N-cadherin antagonist, inhibits N-cadherin mediated cell adhesion.
|
-
- HY-B0535
-
-
- HY-B0312
-
-
- HY-15723
-
NSC 23766
|
Ras
|
Cancer
|
NSC 23766 is a cell-permeable, reversible and specific inhibitor of Rac GTPase, used for cancer treatment.
|
-
- HY-12053
-
-
- HY-16268
-
Kartogenin
KGN
|
TGF-beta/Smad
|
Inflammation/Immunology
|
Kartogenin (KGN) is an inducer of differentiation of human mesenchymal stem cells into chondrocytes, with an EC50 of 100 nM. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program. Kartogenin can be used for the research of osteoarthritis (OA).
|
-
- HY-17406
-
Tolcapone
Ro 40-7592
|
COMT
Amyloid-β
|
Neurological Disease
|
Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-100544
-
FLLL32
|
STAT
JAK
Apoptosis
|
Cancer
|
FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
|
-
- HY-100236
-
Madrasin
DDD00107587
|
Others
|
Cancer
|
Madrasin (DDD00107587) is a splicing inhibitor that prevents formation of both splicing intermediates and products in vitro and interferes with one or more early steps in the pathway of spliceosome assembly. Madrasin also can inhibit pre-mRNA splicing in vitro and modify splicing of endogenous pre-mRNA in cells.
|
-
- HY-122571
-
Retro-2
|
Filovirus
Parasite
Autophagy
|
Cancer
Infection
|
Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC50 of 12.2 µM in HeLa cells. Retro-2 induces cell autophagy.
|
-
- HY-17372
-
Rofecoxib
MK 966
|
COX
|
Inflammation/Immunology
Cancer
|
Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
|
-
- HY-N1990
-
Gypenoside XLIX
|
PPAR
|
Inflammation/Immunology
Cardiovascular Disease
|
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
|
-
- HY-126324
-
IV-23
|
Apoptosis
|
Cancer
|
IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC).
|
-
- HY-W011434
-
Triglycidyl isocyanurate
TGIC; Teroxirone
|
MDM-2/p53
Apoptosis
|
Cancer
Inflammation/Immunology
|
Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.
|
-
- HY-15894A
-
BQ-788
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM.
|
-
- HY-W009749
-
L-Cystathionine
|
Endogenous Metabolite
Apoptosis
|
Cardiovascular Disease
|
L-Cystathionine is a nonprotein thioether and is a key amino acid associated with the metabolic state of sulfur-containing amino acids. L-Cystathionine protects against Homocysteine-induced mitochondria-dependent apoptosis of vascular endothelial cells (HUVECs). L-Cystathionine plays an important role in cardiovascular protection.
|
-
- HY-N0171B
-
Beta-Sitosterol (purity>75%)
β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)
|
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-100303A
-
FR194738
|
Others
|
Metabolic Disease
|
FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
|
-
- HY-16904
-
RI-2
|
RAD51
|
Cancer
|
RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
|
-
- HY-13813
-
Blebbistatin
|
Myosin
|
Others
|
Blebbistatin is a selective non-muscle myosin II (NMII) inhibitor, promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, and better preserves cell junctional integrity and barrier function.
|
-
- HY-100004
-
-
- HY-114305
-
A1874
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
|
-
- HY-109049
-
Adavivint
SM04690; Lorecivivint
|
Wnt
|
Inflammation/Immunology
Cancer
|
Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
|
-
- HY-16191
-
ELR510444
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
|
-
- HY-13057
-
O6BTG-octylglucoside
Glucose-conjugated MGMT inhibitor
|
DNA Methyltransferase
|
Cancer
|
O6BTG-octylglucoside is a potent O 6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
|
-
- HY-135396
-
(1S,2S)-Bortezomib
|
Proteasome
Apoptosis
|
Cancer
|
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
|
-
- HY-136833
-
-
- HY-115686
-
-
- HY-15355
-
Loviride
R 89439
|
Reverse Transcriptase
HIV
|
Infection
|
Loviride (R 89439) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), with an IC50 of 0.3 µM for reverse transcriptase from HIV-1. Loviride (R 89439) inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells.
|
-
- HY-128862
-
EGFR-IN-7
|
EGFR
|
Cancer
|
EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
|
-
- HY-128704A1
-
c-Kit-IN-3 hydrochloride
|
c-Kit
|
Cancer
|
c-Kit-IN-3 hydrochloride (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC50 of 4 nM) and a broad spectrum of drug-resistant mutants (IC50 of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.
|
-
- HY-128704
-
c-Kit-IN-3
|
c-Kit
|
Cancer
|
c-Kit-IN-3 (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.
|
-
- HY-B0228
-
-
- HY-N4238
-
Dehydrocorydaline nitrate
13-Methylpalmatine nitrate
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Cancer
Infection
|
Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline nitrate shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
|
-
- HY-129189
-
RAS GTPase inhibitor 1
|
Ras
|
Cancer
|
RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.
|
-
- HY-76474
-
BAY 61-3606
|
Syk
Apoptosis
|
Cancer
Inflammation/Immunology
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
|
-
- HY-14985
-
BAY 61-3606 dihydrochloride
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
|
-
- HY-10225
-
Belinostat
PXD101; PX105684
|
HDAC
Autophagy
|
Cancer
|
Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
|
-
- HY-100693
-
-
- HY-13541A
-
-
- HY-101071A
-
Monastrol
(±)-Monastrol
|
Kinesin
Apoptosis
|
Cancer
|
Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
|
-
- HY-18664
-
-
- HY-B0535A
-
-
- HY-19971
-
ML239
|
Others
|
Cancer
|
ML239 is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM.
|
-
- HY-N0171
-
Beta-Sitosterol (purity>80%)
β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)
|
Endogenous Metabolite
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-A0070
-
-
- HY-A0070A
-
-
- HY-12762
-
QS11
|
Others
|
Cancer
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
|
-
- HY-10218
-
Everolimus
RAD001; SDZ-RAD
|
mTOR
FKBP
Autophagy
Apoptosis
|
Cancer
|
Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
|
-
- HY-15003
-
ATH686
|
FLT3
Apoptosis
|
Cancer
|
ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects.
|
-
- HY-117819
-
TMP920
|
ROR
|
Inflammation/Immunology
|
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
|
-
- HY-100853
-
IWP-O1
|
Porcupine
Wnt
|
Cancer
|
IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.
|
-
- HY-N3023
-
3,4-Dihydroxybenzylamine hydrobromide
NSC 263475 hydrobromide
|
DNA/RNA Synthesis
|
Cancer
|
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.
|
-
- HY-107856
-
5-Fluorouridine
|
Others
|
Cancer
|
5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity. 5-fluorouridine inhibits rRNA synthesis of human colon carcinoma cells. 5-Fluorouridine exhibits cytotoxic effect on growth of L1210 cells with an IC50 of 2 nM.
|
-
- HY-102064
-
SR 57227A
|
5-HT Receptor
|
Neurological Disease
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
|
-
- HY-P1454
-
Fz7-21
Ac-LPSDDLEFWCHVMY-NH2
|
Wnt
|
Cancer
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2), a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
|
-
- HY-N1150
-
Thymidine
DThyd; NSC 21548
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Others
|
Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
|
-
- HY-128607
-
Mcl1-IN-9
|
Bcl-2 Family
|
Cancer
|
Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
|
-
- HY-N6601
-
Pomolic acid
Randialic acid A
|
Apoptosis
|
Cancer
|
Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC).
|
-
- HY-P1103
-
CTCE-9908
|
CXCR
|
Cancer
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
|
-
- HY-100321
-
-
- HY-19553
-
-
- HY-128595
-
MT-4
|
Others
|
Cancer
|
MT-4 blocks the TG2/FN complex at the interface between cancer cells and the tumor niche. MT-4 inhibits the adhesion of ovarian cancer (OC) cells to the peritoneum.
|
-
- HY-126075A
-
WS-383
|
E1/E2/E3 Enzyme
|
Cancer
|
WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
|
-
- HY-50909
-
Perifosine
KRX-0401; NSC 639966; D21266
|
Akt
Autophagy
Apoptosis
|
Cancer
|
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
|
-
- HY-N2403
-