Search Result
Results for "1 10 phenanthroline mmp Inhibitors" in MCE Product Catalog:
7783
Inhibitors & Agonists
12
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-135232
-
|
MMP-9-IN-1
|
MMP
|
Cancer
|
|
MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor, which
selectively target the hemopexin (PEX) domain of MMP-9, but not other MMPs.
|
-
- HY-114418
-
-
- HY-108672
-
|
NF157
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).
|
-
- HY-117970
-
|
MMPI-1154
|
MMP
|
Cardiovascular Disease
|
|
MMPI-1154 is a promising novel cardio-cytoprotective imidazole-carboxylic acid (ICA) MMP-2 inhibitor(IC50=6.6 μM) and can be used for the study of acute myocardial infarction. MMPI-1154 also inhibits the activity of MMP-13, MMP-1 and MMP-9 with IC50s of 1.8 μM,10 μM, and 13 μM, respectively.
|
-
- HY-19485
-
|
XL-784
|
MMP
|
Cardiovascular Disease
|
|
XL-784 is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1，MMP-2，MMP-3，MMP-8，MMP-9，MMP-13，respectively.
|
-
- HY-N1391
-
|
10-Deacetyltaxol
10-Deacetylpaclitaxel
|
Microtubule/Tubulin
|
Cancer
|
|
10-Deacetyltaxol (10-Deacetylpaclitaxel) is a taxane derivative isolated from Taxus wallichiana Zucc. 10-Deacetyltaxol (10-Deacetylpaclitaxel) promotes the polymerization of tubulin and to inhibit the depolymerization of microtubules induced by cold or by calcium ions in vitro. 10-Deacetyltaxol (10-Deacetylpaclitaxel) exhibits cytotoxicity in human glial and neuroblastoma cell-lines.
|
-
- HY-112160
-
|
XL-784 free base
|
MMP
|
Cardiovascular Disease
|
|
XL-784 free base is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1，MMP-2，MMP-3，MMP-8，MMP-9，MMP-13，respectively.
|
-
- HY-N0095
-
|
(S)-10-Hydroxycamptothecin
10-HCPT; 10-Hydroxycamptothecin
|
Topoisomerase
Apoptosis
|
Cancer
|
|
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
|
-
- HY-14550
-
-
- HY-U00439
-
-
- HY-115467
-
|
MitoBloCK-10
|
Others
|
Metabolic Disease
|
|
MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70.
|
-
- HY-N0275
-
|
(±)-10-Hydroxycamptothecin
(±)-10-HCPT
|
Topoisomerase
|
Cancer
|
|
(±)-10-Hydroxycamptothecin, an indole alkaloid isolated from Camptotheca acuminate, inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
|
-
- HY-15580
-
-
- HY-101865
-
|
KKL-10
|
Bacterial
|
Infection
|
|
KKL-10 is a small-molecule ribosome rescue inhibitor with broad-spectrum antimicrobial activity against bacteria.
|
-
- HY-N2434
-
|
[10]-Shogaol
|
COX
|
Cancer
|
|
[10]-Shogaol is an antioxidant from Zingiber officinale for human skin cell growth and a migration enhancer. [10]-Shogaol inhibits COX-2 with an IC50 of 7.5 μM and has antiproliferation activity.
|
-
- HY-N0448
-
|
10-Gingerol
|
Others
|
Cancer
Inflammation/Immunology
|
|
10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM.
|
-
- HY-103258
-
|
TC ASK 10
|
MAP3K
Apoptosis
|
Cancer
|
|
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM).
|
-
- HY-P1116
-
|
PBP10
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
PBP10 is a cell permeable and selective gelsolin-derived peptide inhibitor of formyl peptide receptor 2 (FPR2) over FPR1. PBP10 is a 10-AA peptide with rhodamine conjugated at its N terminus, exerts bactericidal activity against gram-positive and gram-negative bacteria and limits microbial-induced inflammatory effects.
|
-
- HY-130850
-
-
- HY-135841
-
|
CM10
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
Metabolic Disease
|
|
CM10 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC50s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity.
|
-
- HY-N0446
-
|
10-Methoxycamptothecin
|
Others
|
Cancer
|
|
10-Methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata, and has been confirmed to possess high anti-cancer properties. 10-Methoxycamptothecin has higher cytotoxicity than 10-hydroxycamptothecin by testing antitumor activity against 2774 cell lines.
|
-
- HY-128553A
-
|
(Rac)-Antineoplaston A10
|
Ras
Apoptosis
|
Cancer
|
|
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.
|
-
- HY-N6679A
-
|
10,11-Dehydrocurvularin
|
HSP
TGF-beta/Smad
|
Cancer
Infection
|
|
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
|
-
- HY-19956
-
|
GI254023X
GI4023; SRI028594
|
MMP
|
Cancer
|
|
GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
|
-
- HY-107024
-
|
Osteogenic Growth Peptide (10-14)
OGP(10-14); Historphin
|
Src
|
Others
|
|
Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.
|
-
- HY-P1116A
-
|
PBP10 TFA
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
PBP10 is a cell permeable and selective gelsolin-derived peptide inhibitor of formyl peptide receptor 2 (FPR2) over FPR1. PBP10 is a 10-AA peptide with rhodamine conjugated at its N terminus, exerts bactericidal activity against gram-positive and gram-negative bacteria and limits microbial-induced inflammatory effects.
|
-
- HY-121744
-
|
PS10
|
PDHK
|
Inflammation/Immunology
|
|
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
|
-
- HY-U00050
-
-
- HY-P2247
-
|
JTP10-△-R9 TFA
|
JNK
|
Cancer
|
|
JTP10-△-R9 TFA is a selective JNK2 peptide inhibitor, with an IC50 of 89 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3.
|
-
- HY-13564A
-
|
Batimastat sodium salt
BB-94 sodium salt
|
MMP
|
Cancer
|
|
Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.
|
-
- HY-13564
-
|
Batimastat
BB94
|
MMP
|
Cancer
|
|
Batimastat is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.
|
-
- HY-126492
-
-
- HY-125835
-
|
CP-10
|
PROTAC
CDK
|
Cancer
|
|
CP-10 is a PROTAC with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.
|
-
- HY-B1720
-
|
Ubiquinol
Ubiquinol-10; CoQH2-10
|
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Ubiquinol (Ubiquinol-10) is a reduced form of coenzyme Q10 (CoQ10). Ubiquinol is a potent antioxidant that has the capacity to protect Vitamin E, and also helps to regenerate depleted vitamin E and Vitamin C. Ubiquinol is both lipophilic and hydrophilic and acts as transmembrane factor preventing lipid peroxidation and propagation by transferring electrons to ROS.
|
-
- HY-77572
-
|
7-Epi 10-desacetyl paclitaxel
7-epi-10-deacetyltaxol; 10-Deacetyl-7-epipaclitaxel
|
Others
|
Cancer
|
|
7-Epi 10-desacetyl paclitaxel (7-epi-10-deacetyltaxol), a taxol derivative, exhibits cytotoxicity against HeLa cells with an IC50 of 85 μM.
|
-
- HY-15768
-
|
Ilomastat
GM6001; Galardin
|
MMP
|
Cancer
|
|
Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).
|
-
- HY-13102
-
|
UK-383367
|
Procollagen C Proteinase
|
Others
|
|
UK-383367 (UK 383367) is a potent and selective inhibitor of BMP-1 (procollagen C-proteinase) with IC50 of 44 nM; Selective for BMP-1 over MMPs 1, 2, 3, 9 and 14 (IC50 values are >10,000 nM for listed MMPs).
|
-
- HY-16565
-
-
- HY-106992
-
|
S 3304
|
MMP
|
Cancer
|
|
S 3304 is a novel matrix metalloproteinases (MMP) inhibitor specific for MMP-2 and MMP-9.
|
-
- HY-N0111
-
-
- HY-107394
-
|
UK 356618
|
MMP
|
Cancer
Inflammation/Immunology
|
|
UK 356618 (Compound 4j) is a potent and selective inhibitor of matrix metalloprotease-3 (MMP-3) with an IC50 of 5.9 nM. UK 356618 is less potent against MMP-1, MMP-2, MMP-9, MMP-13 and MMP-14 compared with MMP-3.
|
-
- HY-107639
-
|
UK-370106
|
MMP
|
Inflammation/Immunology
|
|
UK-370106 is a potent and highly selective MMP-3 (IC50 of 23 nM) and MMP-12 (IC50 of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [ 3H]-fibronectin by MMP-3 (IC50 of 320 nM) and has little effect on keratinocyte migration in vitro.
|
-
- HY-19408
-
|
Pyr10
|
TRP Channel
|
Others
|
|
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.
|
-
- HY-117889
-
|
PARP14 inhibitor H10
|
PARP
Apoptosis
|
Cancer
|
|
PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.
|
-
- HY-U00427
-
-
- HY-113450
-
-
- HY-W011085
-
|
CP-471474
|
MMP
|
Inflammation/Immunology
|
|
CP-471474 is an orally active and pan MMP inhibitor, with IC50 values of 1170 nM (MMP-1), 0.7 nM (MMP-2), 16 nM (MMP-3), 13 nM (MMP-9) and 0.9 nM (MMP-13), respectively.
|
-
- HY-U00050S
-
|
(E)-10-Hydroxynortriptyline D3
E-10-OH-NT D3
|
Others
|
Neurological Disease
|
|
(E)-10-Hydroxynortriptyline D3 (E-10-OH-NT D3) is a deuterium labeled (E)-10-Hydroxy Nortriptyline. (E)-10-Hydroxy Nortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression.
|
-
- HY-B0914
-
-
- HY-N7602
-
-
- HY-P1789
-
-
- HY-129554
-
|
cis-9,10-Epoxystearic acid
cis-9,10-Epoxyoctadecanoic acid
|
Endogenous Metabolite
|
Others
|
|
cis-9,10-Epoxystearic acid (cis-9,10-Epoxyoctadecanoic acid) is an endogenous constituent in human blood and urine. cis-9,10-Epoxystearic acid (cis-9,10-Epoxyoctadecanoic acid) can be produced from oleic acid by enzymic and non-enzymic epoxidation.
|
-
- HY-N1463
-
|
Luteolin 7-O-glucuronide
Luteolin 7-glucuronide
|
MMP
|
Others
|
|
Luteolin 7-O-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 17.63, 7.99, 11.42, 12.85, 0.03 μM for MMP-1, MMP-3, MMP-8, MMP-9, MMP-13, respectively.
|
-
- HY-12170
-
|
Prinomastat
AG3340; KB-R9896
|
MMP
|
Cancer
|
|
Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
|
-
- HY-12170A
-
|
Prinomastat hydrochloride
AG3340 hydrochloride; KB-R9896 hydrochloride
|
MMP
|
Cancer
|
|
Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
|
-
- HY-15827
-
|
NSC 405020
|
MMP
|
Cancer
|
|
NSC 405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or MMP-2.
|
-
- HY-15801
-
-
- HY-P1789A
-
-
- HY-140333
-
-
- HY-140330
-
-
- HY-133295
-
-
- HY-130889
-
-
- HY-N1454
-
|
Apigenin-7-glucuronide
Apigenin 7-O-glucuronide
|
MMP
|
Cancer
|
|
Apigenin-7-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 12.87, 22.39, 17.52, 0.27 μM for MMP-3, MMP-8, MMP-9, MMP-13, respectively.
|
-
- HY-20584
-
-
- HY-19740
-
-
- HY-140226
-
|
m-PEG10-amine
|
ADC Linker
PROTAC Linker
|
Cancer
|
|
m-PEG10-amine is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG10-amine is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-W019939
-
|
Hydroxy-PEG10-Boc
|
ADC Linker
|
Cancer
|
|
Hydroxy-PEG10-Boc is extacted from patent CN108707228 (example 0024). Hydroxy-PEG10-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG10-Boc can be conjugated to Paclitaxel (HY-B0015) or docetaxel (HY-B0011).
|
-
- HY-N4303
-
-
- HY-100198
-
-
- HY-N7608
-
-
- HY-135425
-
|
10,12-Tricosadiynoic acid
|
Acyltransferase
|
Metabolic Disease
|
|
10,12-Tricosadiynoic acid is a highly specific, selective, high affinity and orally active acyl-CoA oxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoic acid can treat high fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism.
|
-
- HY-120761
-
-
- HY-128553
-
-
- HY-P1279
-
-
- HY-100646A
-
-
- HY-100646
-
-
- HY-109502S
-
|
10-OH-NBP D4
|
Others
|
Neurological Disease
|
|
10-OH-NBP D4 is deuterium labeled 10-OH-NBP. 10-OH-NBP is a Butylphthalide (3-n-Butylphthalide; NBP; HY-B0647) hydroxylated metabolite and can penetrates the blood-brain barrier (BBB). Butylphthalide exerts neuroprotective effects and has potential for cerebral ischemia research.
|
-
- HY-133230
-
-
- HY-130424
-
-
- HY-114091
-
|
PF-00356231 hydrochloride
|
MMP
|
Inflammation/Immunology
|
|
PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively.
|
-
- HY-15615A
-
|
TIC10
ONC-201
|
TNF Receptor
Apoptosis
|
Cancer
|
|
TIC10 is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
|
-
- HY-12168
-
|
Tanomastat
BAY 12-9566
|
MMP
|
Cancer
|
|
Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The Ki values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models.
|
-
- HY-130641
-
|
Br-C10-methyl ester
|
PROTAC Linker
|
Cancer
|
|
Br-C10-methyl ester is a PROTAC linker, which refers to the alkyl/ether composition. Br-C10-methyl ester is used in the synthesis of a series of PROTACs (MS432). PROTACs contain two different ligands connected by a linker; one is the VHL ligand portion and the other is for the target protein.
|
-
- HY-P1279A
-
-
- HY-141399
-
-
- HY-140029
-
-
- HY-133278
-
-
- HY-140861
-
-
- HY-140360
-
-
- HY-140217
-
-
- HY-140196
-
-
- HY-133270
-
-
- HY-140304
-
-
- HY-140781
-
-
- HY-140801
-
-
- HY-141104
-
-
- HY-140759
-
-
- HY-12169
-
|
Marimastat
BB2516; TA2516
|
MMP
|
Cancer
|
|
Marimastat (BB2516) is a broad spectrum and orally bioavailable inhibitor of MMPs, with potent activity against MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM) and MMP-7 (IC50=13 nM), used in the treatment of cancer. Marimastat (BB2516) is an angiogenesis and metastasis inhibitor, which limits the growth and production of blood vessels. As an antimetatstatic agent it prevents malignant cells from breaching the basement membranes.
|
-
- HY-113794
-
-
- HY-103444
-
|
ARP-100
|
MMP
|
Cancer
|
|
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM).
|
-
- HY-P0273
-
-
- HY-135920
-
-
- HY-W009037
-
-
- HY-130824
-
-
- HY-100359
-
|
CL-82198
|
MMP
|
Cancer
Inflammation/Immunology
|
|
CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.
|
-
- HY-16786
-
|
AI-10-49
|
Others
|
Cancer
|
|
AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.
|
-
- HY-Y0148
-
-
- HY-P0273A
-
-
- HY-113952
-
|
Actinonin
(-)-Actinonin
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
|
-
- HY-133621
-
|
9,10-Dichlorostearic acid
|
Others
|
Cancer
|
|
9,10-Dichlorostearic acid is a chlorinated stearic acid with antimutagenic properties. 9,10-Dichlorostearic acid can cause membrane damage by inducing leakage of adenosine triphosphate (ATP) from mammalian tumour cells in vitro.
|
-
- HY-W004298
-
|
10-Undecen-1-ol
|
Others
|
Others
|
|
10-Undecen-1-ol, converted from ricinoleic acid, can be used as a comonomer for the introduction of functional groups.
|
-
- HY-B0018
-
|
Docetaxal
10-Acetyl docetaxel; PNU-101383
|
Microtubule/Tubulin
|
Cancer
|
|
Docetaxal (10-Acetyl docetaxel; PNU-101383), an analog of Docetaxel (HY-B0011), is a microtubule disassembly inhibitor, with antimitotic activity. Docetaxal has cytotoxicity for murine leukemic cells.
|
-
- HY-15615
-
|
TIC10 isomer
ONC201 isomer
|
Others
|
Others
|
|
TIC10 isomer is the isomer of TIC10. TIC10 isomer does not possess the reported biological activity of inducing TRIAL expression.
|
-
- HY-104047
-
-
- HY-N2117
-
|
Isoginkgetin
|
MMP
|
Cancer
|
|
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
|
-
- HY-107643
-
|
Reversan
CBLC4H10
|
P-glycoprotein
|
Cancer
|
|
Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
|
-
- HY-103482
-
|
JNJ0966
|
MMP
|
Cancer
|
|
JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM.
|
-
- HY-130642
-
-
- HY-N0181A
-
|
Lumisterol
9β,10α-Ergosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
|
-
- HY-140386
-
-
- HY-141120
-
-
- HY-140327
-
-
- HY-101384A
-
-
- HY-10398
-
|
CTS-1027
Ro 1130830; RS 130830
|
MMP
|
Cancer
|
|
CTS-1027 is a potent small molecule inhibitor of MMPs, with IC50s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1.
|
-
- HY-112718
-
-
- HY-P1594
-
-
- HY-N0532
-
-
- HY-B0914A
-
-
- HY-P0236
-
-
- HY-133312
-
-
- HY-13488
-
|
HG-10-102-01
|
LRRK2
|
Neurological Disease
|
|
HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM)
IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1]
Target: LRRK2
HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2.
|
-
- HY-N6834
-
|
Fructo-oligosaccharide DP10/GF9
|
Others
|
Others
|
|
Fructo-oligosaccharide DP10/GF9 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=10). Fructo-oligosaccharides (FOS) are composed of 9 fructose units linked by (2→1)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end.
|
-
- HY-129941
-
-
- HY-130876
-
-
- HY-P1375
-
|
[D-Trp7,9,10]-Substance P
|
mAChR
|
|
|
[D-Trp7,9,10]-Substance P is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-W040270
-
|
Amino-PEG10-amine
|
PROTAC Linker
|
Cancer
|
|
Amino-PEG10-amine, a PEG-based PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer.
|
-
- HY-N1940
-
|
β-Anhydroicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
|
|
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties[1]inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
|
-
- HY-130137
-
-
- HY-141130
-
-
- HY-N6679
-
|
(R)-10,11-Dehydrocurvularin
|
Others
|
Cancer
|
|
(R)-10,11-Dehydrocurvularin is a secondary metabolite isolated from Curvularia sp.. (R)-10,11-Dehydrocurvularin displays concentration-dependent cytotoxicity towards human tumor cell lines with a mean IC50 value of 1.25 µM.
|
-
- HY-B0797
-
|
Etretinate
Ro 10-9359
|
Apoptosis
|
Others
|
|
Etretinate(Ro 10-9359) is a second-generation retinoid that has the potential for severe psoriasis treatment.
|
-
- HY-141218
-
|
m-PEG10-alcohol
Decaethylene glycol monomethyl ether
|
ADC Linker
PROTAC Linker
|
Cancer
|
|
m-PEG10-alcohol (Decaethylene glycol monomethyl ether) is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG10-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-133304
-
-
- HY-133335
-
-
- HY-133285
-
-
- HY-140631
-
-
- HY-B0107
-
-
- HY-P1594A
-
-
- HY-P1567
-
-
- HY-N6846
-
|
10-Isobutyryloxy-8,9-epoxythymol isobutyrate
|
Bacterial
|
Infection
|
|
10-Isobutyryloxy-8,9-epoxythymol isobutyrate is a major constituent of Inula helenium and Inula royleana root cultures. 10-Isobutyryloxy-8,9-epoxythymol isobutyrate shows moderate antimicrobial activity against Staphylococcus aureus FDA 209 P, Staphylococcus aureus, Enterococcus faecalis, Candida albicans and Pseudomonas aeruginosa with MICs of 50, 250, 250, 250, and 1000 μg/mL, respectively.
|
-
- HY-B0107A
-
-
- HY-W017772
-
|
Boc-NH-PEG3
PROTAC Linker 10
|
PROTAC Linker
|
Cancer
|
|
Boc-NH-PEG3 (PROTAC Linker 10) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
|
-
- HY-N7008
-
|
Fructo-oligosaccharide DP11/GF10
|
Others
|
Metabolic Disease
|
|
Fructo-oligosaccharide DP11/GF10 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=11). Fructo-oligosaccharides (FOS) are composed of 10 fructose units linked by (2→1)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end.
|
-
- HY-130716
-
-
- HY-P1375A
-
|
[D-Trp7,9,10]-Substance P TFA
|
mAChR
|
|
|
[D-Trp7,9,10]-Substance P TFA is the substance P analog that inhibits activation of Gq/11 by M1 muscarinic ACh receptors. [D-Trp7,9,10]-Substance P TFA does not inhibit Gi/o activation by M2 ACh receptors.
|
-
- HY-P0236A
-
-
- HY-131005
-
-
- HY-P2213
-
|
GPLGIAGQ
|
MMP
Apoptosis
|
Cancer
|
|
GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT).
|
-
- HY-19711
-
|
STING agonist-1
G10
|
STING
Virus Protease
|
Infection
|
|
STING agonist-1 (G10) is human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. G10 potently blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM.
|
-
- HY-16674
-
-
- HY-133357
-
-
- HY-B0099
-
-
- 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-P2213A
-
|
GPLGIAGQ TFA
|
MMP
Apoptosis
|
Cancer
|
|
GPLGIAGQ TFA, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting. GPLGIAGQ TFA can be used to synthesis unique MMP2-targeted photosensitizer in photodynamic therapy (PDT).
|
-
- HY-126355
-
-
- HY-N0262
-
|
Cordycepin
3'-Deoxyadenosine
|
MMP
Bacterial
Autophagy
Antibiotic
|
Cancer
Infection
Inflammation/Immunology
|
|
Cordycepin (3'-Deoxyadenosine) is a nucleoside derivative isolated from Cordyceps and inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner. Cordycepin kills Mycobacterium tuberculosis through hijacking the bacterial adenosine kinase.
|
-
- 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.
|
-
- HY-133307
-
-
- 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-101703
-
-
- HY-140320
-
-
- HY-100211
-
|
TAPI-2
TNF Protease Inhibitor 2
|
MMP
SARS-CoV
|
Cancer
|
|
TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.
|
-
- HY-130847
-
-
- 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-12354
-
|
SB-3CT
|
MMP
|
Cancer
|
|
SB-3CT is a potent and competitive matrix metalloproteinase MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively. SB-3CT has high selectivity for gelatinases. SB-3CT shows blood-brain barrier permeability and has neuroprotective effects and anticancer activity.
|
-
- HY-N0431
-
|
Astragaloside IV
|
MMP
ERK
JNK
|
Cancer
|
|
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
|
-
- 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-P1053
-
-
- HY-N0565
-
-
- HY-N0565A
-
-
- HY-16675
-
-
- HY-101671
-
-
- HY-130865
-
-
- HY-140471
-
-
- HY-126509
-
|
Mal-amido-PEG10-C2-NHS ester
|
ADC Linker
|
Cancer
|
|
Mal-amido-PEG10-C2-NHS ester is a nonclaevable ADC linker containing a maleimide group and an NHS ester. The NHS ester can be used to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.
|
-
- HY-W008923
-
-
- HY-140325
-
-
- HY-17468
-
|
Bumetanide
Ro 10-6338; PF 1593
|
NKCC
|
Cardiovascular Disease
|
|
Bumetanide (Ro 10-6338;PF 1593) is a selective Na +-K +-Cl - cotransporter 1 (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.
|
-
- HY-P1787
-
-
- HY-12290
-
|
Arg-Gly-Asp-Ser
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
|
-
- HY-N1981
-
-
- HY-N0318
-
-
- HY-N0565B
-
|
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
MMP
Bacterial
Antibiotic
|
Infection
|
|
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
|
-
- HY-135930
-
-
- HY-125166
-
|
DB04760
|
MMP
|
Cancer
Neurological Disease
|
|
DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity.
|
-
- HY-121879
-
-
- HY-16978
-
-
- HY-133587
-
|
1,1,1,3,10,11-Hexachloroundecane
|
Others
|
Others
|
|
1,1,1,3,10,11-Hexachloroundecane is a kind of polychlorinated alkane (PCA) that has a long carbon chain length.
|
-
- HY-77813
-
-
- 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-15581
-
-
- HY-P1031
-
-
- HY-N6844
-
-
- HY-111456
-
-
- HY-128976
-
-
- HY-19373
-
-
- 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-N6013
-
|
Aloin(mixture of A&B)
|
MMP
Bacterial
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
|
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs).
|
-
- 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-130234
-
|
SP-8356
|
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
SP-8356, an anti-inflammatory synthetic Verbenone derivative, is a potent, orally active cluster of differentiation 147 (CD147) inhibitor. SP-8356 inhibits CD147-cyclophilin A (CypA) interaction and reduces MMP-9 activity. SP-8356 exerts anti-breast cancer effects by inhibiting NF-κB signaling. Anti-atherosclerotic effects.
|
-
- HY-13648
-
|
Incyclinide
CMT-3; COL-3
|
MMP
|
Cancer
|
|
Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor, thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.
|
-
- HY-16657
-
-
- HY-W011120
-
|
Ethyl docosa-4,7,10,13,16,19-hexaenoate
|
Others
|
Metabolic Disease
|
|
Ethyl cis-4,7,10,13,16,19-Docosahexaenoate, the ethyl ester of Docosahexaenoate (DHA), is enriched in the ethyl ester fraction by the selective alcoholysis of fatty acid ethyl esters originating from tuna oil with lauryl alcohol.
|
-
- 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-N3063
-
|
Pimaric acid
|
Others
|
|
|
Pimaric acid is a resin acid that has been found in A. cordata and various pines. Pimaric acid reduces mRNA expression, protein levels, and promoter activity of matrix metalloproteinase-9 (MMP-9) in TNF-α-stimulated human aortic smooth muscle cells (HASMCs).
|
-
- 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-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-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-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-12913
-
-
- HY-112023
-
|
Lumisterol 3 (>90%)
9β,10α-Cholesta-5,7-dien-3β-ol; Cholecalciferol EP Impurity A
|
Endogenous Metabolite
|
Others
|
|
Lumisterol 3 (>90%) (9β,10α-Cholesta-5,7-dien-3β-ol) is a normal human secosterooid metabolite from the class of vitamin D3 photoisomer derivatives. Lumisterol 3 (>90%) is used in the preparation of vitamin D.
|
-
- HY-15586
-
|
L67
DNA Ligase Inhibitor
|
DNA/RNA Synthesis
|
Cancer
|
|
L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.
|
-
- HY-18728
-
-
- 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-N2388
-
|
Auraptene
|
MMP
|
Inflammation/Immunology
Cancer
|
|
Auraptene is the most abundant naturally occurring geranyloxycoumarin. Auraptene is primarily isolated from plants in the Rutaceae family, such as citrus fruits. Auraptene decreases the secretion of matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8, and chemokine (C-C motif) ligand-5(CCL5).
|
-
- HY-135848
-
-
- HY-15583
-
-
- HY-12970A
-
-
- HY-N2350
-
|
Cynaropicrin
|
MMP
NF-κB
TNF Receptor
|
Cancer
|
|
Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
|
-
- 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-130976
-
-
- HY-N0088
-
-
- HY-117604
-
|
THPP-1
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
|
-
- HY-N2205
-
|
Esculentoside H
|
NF-κB
JNK
|
Cancer
|
|
Esculentoside H (EsH) is a water-soluble saponin isolated and purified from the root extract of perennial plant Phytolacca esculenta.
Esculentoside H (EH) has anti-tumor activity, the mechanism is related to the capacity for TNFrelease.
Esculentoside H (EsH) suppresses colon cancer cell migration through blockage of the JNK1/2 and NF-κB signaling-mediated matrix metalloproteinases-9 (MMP-9) expression.
|
-
- HY-N2194
-
-
- HY-101799
-
-
- HY-16461
-
-
- HY-B0170
-
-
- HY-10836
-
-
- 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-119307
-
|
Apratastat
|
MMP
TNF Receptor
|
Cancer
|
|
Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively.
|
-
- HY-13074
-
-
- HY-14981
-
|
GSK2334470
|
PDK-1
|
Cancer
|
|
GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
|
-
- HY-B0170A
-
-
- HY-101214
-
-
- HY-13959
-
|
MS436
|
Epigenetic Reader Domain
|
Cancer
|
|
MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
|
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-14672
-
|
Soblidotin
Auristatin PE; TZT-1027
|
Microtubule/Tubulin
|
Cancer
|
|
Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.
|
-
- HY-16706A
-
-
- HY-12471
-
|
VLX1570
|
Deubiquitinase
|
Cancer
|
|
VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
|
-
- 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-140500
-
|
m-PEG10-acid
|
ADC Linker
PROTAC Linker
|
Cancer
|
|
m-PEG10-acid is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG10-acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-15842
-
-
- HY-15878
-
-
- HY-B2162
-
|
Chondroitin sulfate
Chondroitin polysulfate
|
NO Synthase
MMP
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Chondroitin sulfate, one of five classes of glycosaminoglycans, has been widely used in the treatment of osteoarthritis. Chondroitin sulfate reduces inflammation mediators and the apoptotic process and is able to reduce protein production of inflammatory cytokines, iNOS and MMPs.
|
-
- HY-B1287
-
-
- HY-19741
-
-
- HY-101054
-
-
- HY-10303
-
|
PIK-294
|
PI3K
|
Cancer
|
|
PIK-294 is a potent p110δ-selective inhibitor with an IC50 of 10 nM.
|
-
- HY-130296
-
-
- HY-10962
-
|
Momelotinib sulfate
CYT387 sulfate salt
|
JAK
Autophagy
Apoptosis
|
Cancer
|
|
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
|
-
- HY-N3387
-
|
Licoricidin
|
Apoptosis
NF-κB
Akt
MMP
|
Cancer
Inflammation/Immunology
|
|
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer. Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect. Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo. Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations.
|
-
- HY-15581S
-
-
- HY-B0494
-
-
- HY-100790
-
|
Ciliobrevin A
HPI-4
|
Hedgehog
|
Cancer
|
|
Ciliobrevin A is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
|
-
- HY-100509
-
-
- HY-112789
-
-
- HY-12014
-
-
- HY-13532
-
|
AS-252424
|
PI3K
|
Cancer
|
|
AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.
|
-
- HY-50710
-
|
KU-0063794
|
mTOR
|
Cancer
|
|
KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC50s of 10 nM.
|
-
- HY-15996
-
|
Seviteronel
VT-464
|
Cytochrome P450
|
Cancer
|
|
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
|
-
- HY-B0590B
-
|
(+)-Tetrabenazine
(+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine
|
Monoamine Transporter
|
Cancer
|
|
(+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
|
-
- HY-N0801
-
|
Polygalacic acid
|
MMP
AChE
|
Inflammation/Immunology
Neurological Disease
|
|
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment .
Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex.
|
-
- HY-15459
-
-
- HY-105185
-
|
Fidarestat
SNK 860
|
Aldose Reductase
|
Metabolic Disease
|
|
Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease.
|
-
- HY-13577A
-
|
Oclacitinib maleate
PF-03394197 maleate
|
JAK
|
Inflammation/Immunology
|
|
Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM).
|
-
- HY-12589
-
-
- HY-12589A
-
-
- HY-P1580
-
-
- HY-12808
-
-
- HY-12859
-
|
BAY1217389
|
Mps1
|
Cancer
|
|
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.
|
-
- HY-111482
-
-
- HY-140455
-
-
- HY-140020
-
-
- HY-140176
-
-
- HY-133231
-
-
- HY-15951
-
|
ML167
CID44968231; NCGC00188654
|
CDK
|
Cancer
|
|
ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B.
|
-
- HY-12050
-
|
CP-673451
|
PDGFR
|
Cancer
|
|
CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-15646
-
-
- HY-100685
-
|
MS-444
BE-34776
|
Myosin
|
Cancer
|
|
MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM.
|
-
- HY-13248
-
-
- HY-12746
-
-
- HY-15991
-
-
- HY-16676
-
-
- HY-140973
-
-
- HY-140461
-
-
- HY-140490
-
-
- HY-B0192A
-
-
- HY-100116A
-
-
- HY-B1069
-
|
Molsidomine
SIN-10; Morsydomine
|
Others
|
Cardiovascular Disease
|
|
Molsidomine is an orally active, long acting vasodilating drug, metabolized in the liver to the active metabolite linsidomine, which is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound.
|
-
- HY-112831
-
|
BI-409306
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); BI-409306 can be used in the research of memory enhancement in CNS disorders.
|
-
- HY-15245
-
|
GSK2636771
|
PI3K
|
Cancer
|
|
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
|
-
- HY-18673
-
|
PROTO-1
|
Others
|
Inflammation/Immunology
|
|
PROTO-1 shows significant protection of hair cells, with HC50(concentration that would produce 50% hair cell survival) of 1 μM-10 μM (1 μM≤HC50≤10 μM).
|
-
- HY-101757
-
-
- HY-N0303
-
-
- HY-16297A
-
|
Abemaciclib
LY2835219
|
CDK
|
Cancer
|
|
Abemaciclib (LY2835219) is a selective CDK4/6 inhibitor with IC50 values of 2 nM and 10 nM for CDK4 and CDK6, respectively.
|
-
- HY-13461A
-
-
- HY-15224
-
|
PCI-34051
|
HDAC
Apoptosis
|
Cancer
|
|
PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.
|
-
- HY-N2497
-
|
Isoliquiritin apioside
|
NF-κB
MMP
p38 MAPK
|
Cancer
|
|
Isoliquiritin apioside, a component isolated from Glycyrrhizae radix rhizome, significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells.
|
-
- HY-101840
-
-
- HY-101840A
-
-
- HY-10228
-
|
Motesanib
AMG 706
|
c-Kit
VEGFR
|
Cancer
|
|
Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
- HY-10229
-
|
Motesanib Diphosphate
AMG 706 Diphosphate
|
c-Kit
VEGFR
|
Cancer
|
|
Motesanib Diphosphate (AMG 706 Diphosphate) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
|
-
- HY-N2300
-
-
- HY-19189
-
-
- HY-18306
-
-
- HY-12990
-
|
Spautin-1
|
Autophagy
Apoptosis
|
Cancer
|
|
Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.
|
-
- 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-A0023
-
-
- HY-10406
-
|
Talmapimod
SCIO-469
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
|
-
- HY-19205A
-
-
- HY-112113
-
|
SLV-2436
SEL201-88; SEL-201
|
MNK
|
Cancer
|
|
SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.
|
-
- HY-100611
-
-
- HY-13785
-
|
ZM 306416
CB 676475
|
VEGFR
|
Cancer
|
|
ZM-306416 (CB 676475) is a potent inhibitor of VEGFR with IC50s of 0.1 and 2 μM for KDR and Flt, respectively. ZM-306416 is also a EGFR inhibitor with an IC50 of <10 nM.
|
-
- HY-13275
-
-
- HY-13003
-
|
Torin 1
|
mTOR
Autophagy
|
Cancer
|
|
Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy.
|
-
- HY-136466
-
|
A2ti-2
|
Virus Protease
|
Infection
|
|
A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 230 μM. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-136465
-
|
A2ti-1
|
Virus Protease
|
Infection
|
|
A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM. A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-13455
-
|
LDN-192960
|
Haspin Kinase
DYRK
|
Cancer
|
|
LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
|
-
- HY-18300
-
|
Filgotinib
GLPG0634
|
JAK
|
Cancer
|
|
Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
|
-
- HY-13296
-
|
PYR-41
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
|
-
- HY-13455A
-
-
- HY-101075
-
|
L-690330
|
Phosphatase
|
Others
|
|
L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 exhibits 10-fold more sensitive than mouse and rat IMPase.
|
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-100595
-
|
Sodium stibogluconate
Stibogluconate trisodium nonahydrate
|
Phosphatase
|
Cancer
|
|
Sodium stibogluconate (Stibogluconate trisodium nonahydrate) is a potent inhibitor of protein tyrosine phosphatase. Sodium stibogluconate inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.
|
-
- HY-100018
-
|
BAY1125976
|
Akt
|
Cancer
|
|
BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
|
-
- HY-129571
-
-
- HY-12659
-
|
LX7101
|
ROCK
|
Others
|
|
LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.
|
-
- HY-101284
-
|
DMU2105
|
Cytochrome P450
|
Cancer
|
|
DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
|
-
- HY-10372
-
-
- HY-U00308
-
-
- HY-N2337
-
-
- HY-16355
-
|
NVP-QAV-572
|
PI3K
|
Cancer
|
|
NVP-QAV-572 is a PI3K inhibitor extracted from patent US7998990B2, Compound Example 8, has an IC50 of 10 nM.
|
-
- HY-12472
-
-
- HY-103667
-
|
2-HBA
|
Caspase
|
Cancer
|
|
2-HBA is a potent inducer of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1) which can also activate caspase-3 and caspase-10.
|
-
- 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-N6957
-
|
8-Keto-berberine
|
Others
|
Metabolic Disease
|
|
8-Keto-berberine (compound 29) is a non-naturally occurring 11, 12-oxygenated protoberberine derived from naturally occurring 9, 10-oxygenated protoberberine.
|
-
- HY-12648A
-
-
- HY-15600
-
|
UPF-648
|
Others
|
Neurological Disease
|
|
UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.
|
-
- HY-12425
-
-
- HY-13689
-
|
Go 6983
Gö 6983; Goe 6983
|
PKC
|
Cancer
|
|
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
|
-
- HY-12648
-
-
- HY-12437
-
|
BDP5290
|
ROCK
|
Cancer
|
|
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
|
-
- HY-10257
-
-
- HY-15613
-
|
Maritoclax
Marinopyrrole A
|
Bcl-2 Family
|
Cancer
|
|
Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
|
-
- HY-18650
-
|
KU 59403
|
ATM/ATR
|
Cancer
|
|
KU 59403 is a potent ATM inhibitor, with IC50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively.
|
-
- HY-10009
-
-
- HY-N1401
-
|
20(R)-Ginsenoside Rh2
|
MMP
Apoptosis
HSV
|
Cancer
Infection
Inflammation/Immunology
|
|
20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity. 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68.
|
-
- HY-42034
-
|
Hydroquinine
|
Others
|
Inflammation/Immunology
|
|
Hydroquinine is a cinchona alkaloid, can be used in the preparation of its derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine and 10,11-dihydroquinine monohydrochloride.
|
-
- HY-23119
-
-
- HY-13560
-
|
AVN-944
VX-944
|
Others
|
Cancer
|
|
AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.
|
-
- HY-12960
-
|
SKLB4771
FLT3-IN-1
|
FLT3
|
Cancer
|
|
SKLB4771 is a novel potent and selective Flt3 inhibitor with IC50 of 10 nM; against FLT3-ITD-expressing MV4-11 cells with IC50 of 6 nM.
|
-
- HY-15594
-
|
Phen-DC3
|
DNA/RNA Synthesis
|
Cancer
|
|
Phen-DC3 is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
|
-
- HY-128583
-
|
G150
|
Others
|
Inflammation/Immunology
|
|
G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor for repression of dsDNA-triggered interferon expression, with an IC50 of 10.2 nM.
|
-
- HY-136350
-
|
BRD9500
|
Phosphodiesterase (PDE)
|
Cancer
|
|
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
|
-
- HY-15513
-
|
TC-DAPK 6
|
DAPK
|
Cancer
|
|
TC-DAPK 6 is a potent, ATP-competitive, and highly selective DAPK inhibitor (IC50=69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP).
|
-
- HY-15100
-
|
Balicatib
AAE581
|
Cathepsin
|
Inflammation/Immunology
|
|
Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.
|
-
- HY-N6607
-
|
Tryptanthrin
|
Others
|
Inflammation/Immunology
|
|
Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin inhibits LT formation in human whole blood (IC50 = 10 µM) and reduces LTB4 levels in the rat pleurisy model.
|
-
- HY-112724
-
|
SHR0302
|
JAK
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.
|
-
- HY-10472
-
|
LY2811376
|
Beta-secretase
|
Neurological Disease
|
|
LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
|
-
- HY-51424
-
|
PLX-4720
|
Raf
|
Cancer
|
|
PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
|
-
- HY-50943
-
|
AT7519 Hydrochloride
|
CDK
Apoptosis
|
Cancer
|
|
AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
|
-
- HY-107145A
-
-
- HY-50940
-
|
AT7519
|
CDK
Apoptosis
|
Cancer
|
|
AT7519 as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
|
-
- HY-50940A
-
|
AT7519 trifluoroacetate
|
CDK
|
Cancer
|
|
AT7519 trifluoroacetate as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
|
-
- HY-107999
-
|
CADD522
|
Others
|
Cancer
|
|
CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 exhibits antitumor activity.
|
-
- HY-13592
-
|
HDAC-IN-7
Chidamide impurity
|
HDAC
|
Cancer
|
|
HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
|
-
- HY-13237
-
-
- HY-15594A
-
-
- HY-107145
-
-
- HY-16297
-
|
Abemaciclib methanesulfonate
LY2835219 methanesulfonate
|
CDK
|
Cancer
|
|
Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively.
|
-
- HY-N1490
-
-
- HY-125843
-
|
Pomalidomide-PEG1-C2-N3
Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Pomalidomide-PEG1-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology. Pomalidomide-PEG1-C2-N3 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC50 of 2.1 nM.
|
-
- HY-103194
-
|
KH7
|
Others
|
Others
|
|
KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.
|
-
- HY-15320
-
-
- HY-15507
-
-
- HY-15162
-
|
Monomethyl auristatin E
MMAE; SGD-1010
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
|
-
- HY-10163
-
|
Dabigatran
BIBR 953; BIBR 953ZW
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM).
|
-
- HY-13487
-
-
- HY-108333
-
|
SB-633825
|
Others
|
Cancer
Cardiovascular Disease
|
|
SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis.
|
-
- HY-13493
-
|
AC710
|
PDGFR
c-Kit
FLT3
|
Cancer
|
|
AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
|
-
- HY-141232
-
-
- HY-10328
-
|
Neflamapimod
VX-745
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
|
-
- HY-10528
-
|
Tasquinimod
ABR-215050
|
HDAC
|
Cancer
|
|
Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor.
|
-
- HY-15391
-
|
Lucitanib
E-3810
|
VEGFR
FGFR
|
Cancer
|
|
Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
|
-
- HY-12334
-
|
HTH-01-015
|
AMPK
|
Cancer
|
|
HTH-01-015 is a selective NUAK1/ARK5 inhibitor (IC50 is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).
|
-
- HY-107589A
-
|
BIO5192 hydrate
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
|
-
- HY-16749A
-
|
Pexidartinib hydrochloride
PLX-3397 hydrochloride
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity.
|
-
- HY-N4070
-
|
6"-O-Acetylgenistin
|
Others
|
Others
|
|
6"-O-Acetylgenistin is an isoflavone glycoside isolated from soybeans. 6"-O-Acetylgenistin significantly inhibits lipid peroxidation in rat liver microsome with an IC50 of 10.6 μM.
|
-
- HY-10991
-
|
MGCD-265 analog
|
c-Met/HGFR
VEGFR
Apoptosis
|
Cancer
|
|
MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.
|
-
- HY-15356
-
-
- HY-120142
-
|
EC359
|
Apoptosis
|
Cancer
|
|
EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions.
|
-
- HY-12954
-
|
PTACH
NCH-51
|
HDAC
|
Cancer
|
|
PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDAC. PTACH exerts potent growth inhibition against various human cancer cells, with EC50 values ranging from 1 to 10 μM.
|
-
- 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-102026
-
-
- HY-50898
-
|
Lapatinib
GW572016; GW2016
|
EGFR
Autophagy
Ferroptosis
|
Cancer
|
|
Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
|
-
- HY-18770
-
-
- HY-10192
-
|
NVP-TAE 684
TAE 684
|
ALK
Apoptosis
|
Cancer
|
|
NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.
|
-
- HY-16652
-
|
Apabetalone
RVX-208; RVX000222
|
Epigenetic Reader Domain
HIV
|
Cancer
|
|
Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87±10 μM and 0.51±0.041 μM for BD1 and BD2, respectively.
|
-
- HY-N3511
-
|
Triptonine B
|
HIV
|
Infection
|
|
Triptonine B, a sesquiterpene pyridine alkaloid that isolated from Tripterygium hypoglaucum and Tripterygium wilfordii, inhibits HIV replication in H9 lymphocytes with an EC50 value of <0.10 μg/mL.
|
-
- HY-10579
-
|
Pluripotin
SC1
|
Ribosomal S6 Kinase (RSK)
ERK
|
Cancer
|
|
Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 µM, respectively.
|
-
- HY-W016867
-
|
4-Chlorosalicylic acid
|
Fungal
Bacterial
|
Infection
|
|
4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC50s of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/mL.
|
-
- HY-N3797A
-
|
Echitamine chloride
|
Apoptosis
|
Cancer
|
|
Echitamine chloride is the major monoterpene indole alkaloid present in Alstonia with potent anti-tumour activity. Echitamine chloride induces DNA fragmentation and cells apoptosis. Echitamine chloride inhibits pancreatic lipase with an IC50 of 10.92 µM.
|
-
- HY-108697A
-
-
- HY-124108
-
|
Eicosatetraynoic acid
ETYA
|
COX
PPAR
|
Others
|
|
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM.
|
-
- HY-N1910
-
|
4'-O-Methylbavachalcone
|
SARS-CoV
|
Infection
|
|
4'-O-Methylbavachalcone is a chalcone isolated from Psoralea corylifolia, inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) activity, with an IC50 of 10.1 μM.
|
-
- HY-113252
-
-
- HY-W062835
-
|
CGP77675
|
Src
|
Cancer
|
|
CGP77675 is a potent inhibitor of Src family kinases. CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity.
|
-
- HY-N2503
-
|
Ginsenoside F4
|
Apoptosis
MMP
|
Inflammation/Immunology
|
|
Ginsenoside F4 (GF4), ginseng saponinis, isolated from notoginseng or red ginseng. Ginsenoside F4 (GF4) has inhibitory effect on human lymphocytoma JK cell by inducing its apoptosis.
Ginsenoside F4 (GF4) inhibits matrix metalloproteinase 13 (MMP 13) expression in IL-1β-treated chondrocytes and blocks cartilage breakdown in rabbit cartilage tissue culture, shows therapeutic potential for preventing cartilage collagen matrix breakdown in diseased tissues.
|
-
- HY-13696
-
-
- HY-14276A
-
|
Gallopamil hydrochloride
Methoxyverapamil hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil hydrochloride (Methoxyverapamil hydrochloride), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil hydrochloride inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil hydrochloride is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-13250
-
|
Silvestrol aglycone
|
Others
|
Cancer
|
|
Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity.
|
-
- HY-15777A
-
|
Ribociclib hydrochloride
LEE011 hydrochloride
|
CDK
|
Cancer
|
|
Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-14276
-
|
Gallopamil
Methoxyverapamil
|
Calcium Channel
|
Cardiovascular Disease
|
|
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM. Gallopamil is a potent antiarrhythmic and vasodilator agent.
|
-
- HY-P1247
-
-
- HY-129150
-
|
Ganoderic acid TR
|
Influenza Virus
|
Infection
|
|
Ganoderic acid TR is a broad-spectrum inhibitor against influenza neuraminidases (NAs), particularly H5N1 and H1N1 neuraminidases. The IC50 values of 10.9 and 4.6 μM, respectively.
|
-
- HY-102031
-
-
- HY-50898A
-
|
Lapatinib ditosylate
GW572016 ditosylate; GW2016 ditosylate
|
EGFR
Autophagy
Ferroptosis
|
Cancer
|
|
Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
|
-
- 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-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-14435
-
|
Pyridone 6
|
JAK
|
Cancer
|
|
Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
|
-
- HY-127105
-
-
- HY-13101
-
-
- HY-12009
-
|
Pazopanib Hydrochloride
GW786034 (Hydrochloride)
|
PDGFR
VEGFR
FGFR
c-Kit
c-Fms
Autophagy
|
Cancer
|
|
Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
|
-
- HY-50098
-
-
- HY-50098A
-
|
Mardepodect hydrochloride
PF-2545920 hydrochloride
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier.
|
-
- HY-13998
-
|
Dasabuvir
ABT-333
|
HCV
|
Infection
|
|
Dasabuvir (ABT-333) is a nonnucleoside inhibitor of the RNA-dependent RNA polymerase encoded by the HCV NS5B gene, inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates, with IC50 between 2.2 and 10.7 nM.
|
-
- HY-16749
-
|
Pexidartinib
PLX-3397
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity.
|
-
- HY-12305
-
|
Q-VD-OPh
QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone
|
Caspase
HIV
|
Cancer
Infection
|
|
Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.
|
-
- HY-126508
-
|
Mal-amido-PEG5-C2-NHS ester
|
ADC Linker
|
Cancer
|
|
Mal-amido-PEG10-C2-NHS ester is a nonclaevable ADC linker containing a maleimide group and an NHS ester. The NHS ester can be used to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules
|
-
- HY-12418
-
|
E7449
|
PARP
|
Cancer
|
|
E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD + as substrate.
|
-
- HY-123892
-
|
RK-287107
|
PARP
|
Cancer
|
|
RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth.
|
-
- HY-P1247A
-
-
- HY-15319
-
-
- HY-15777
-
|
Ribociclib
LEE011
|
CDK
|
Cancer
|
|
Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-111818
-
|
TH34
|
HDAC
|
Cancer
|
|
TH34, an HDAC6/8/10 inhibitor with IC50s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3.
|
-
- HY-119039
-
|
RU-301
|
TAM Receptor
|
Cancer
|
|
RU-301 is a pan-TAM receptor inhibitor, exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively.
|
-
- HY-15777C
-
|
Ribociclib succinate hydrate
LEE011 succinate hydrate
|
CDK
|
Cancer
|
|
Ribociclib succinate hydrate (LEE011 succinate hydrate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-15777B
-
|
Ribociclib succinate
LEE011 succinate
|
CDK
|
Cancer
|
|
Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-W013215
-
-
- HY-12519
-
|
Oltipraz
RP 35972; NSC 347901
|
HIF/HIF Prolyl-Hydroxylase
HIV
Keap1-Nrf2
|
Cancer
|
|
Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
|
-
- HY-112597
-
-
- HY-W018061
-
-
- HY-10208
-
|
Pazopanib
GW786034
|
VEGFR
c-Kit
PDGFR
Autophagy
FGFR
|
Cancer
|
|
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
|
-
- HY-N0505
-
|
Rosiridin
|
Monoamine Oxidase
|
Neurological Disease
|
|
Rosiridin, which is isolated from Rhodiola rosea L., inhibits MAO A and MAO B with potential beneficial effect in depression and senile dementia. Rosiridin shows an inhibition of 83.8% against MAO B at 10 μM (pIC50=5.38).
|
-
- HY-110079
-
|
TNP
|
Others
|
Cancer
|
|
TNP is a cell-permeable inhibitor of IP6K1 and IP3K, with IC50 values of 0.55 µM and 10.2 µM for IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes.
|
-
- HY-112373
-
|
Aurora Kinase Inhibitor 3
|
Aurora Kinase
|
Others
|
|
Aurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50>10 μM. Aurora Kinase Inhibitor 3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket, and several induced structural changes in the active-site compared with other published AIK structures.
|
-
- HY-P2080
-
|
GIP (1-30) amide,Human
|
Glucagon Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,Human is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide (Human) dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M.
|
-
- HY-P2080B
-
|
GIP (1-30) amide,Human acetate
|
Glucagon Receptor
|
Metabolic Disease
|
|
GIP (1-30) amide,Human acetate is a glucose-dependent insulinotropic polypeptide (GIP) fragment. GIP is an incretin hormone that stimulates insulin secretion and reduces postprandial glycaemic excursions. GIP (1-30) amide (Human) dose-dependently promotes insulin secretion over the range 10 -9-10 -6 M.
|
-
- HY-15196
-
|
TAK-285
|
EGFR
|
Cancer
|
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
|
-
- HY-13522
-
|
Fimepinostat
CUDC-907
|
PI3K
HDAC
Apoptosis
|
Cancer
|
|
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
|
-
- HY-18613
-
|
CAY10603
BML-281
|
HDAC
|
Cancer
|
|
CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor, with an IC50 of 2 pM; CAY10603 (BML-281) also inhibits HDAC1, HDAC2, HDAC3, HDAC8, HDAC10, with IC50s of 271, 252, 0.42, 6851, 90.7 nM.
|
-
- HY-N2450
-
|
Sulforaphene
|
Apoptosis
EGFR
ERK
NF-κB
|
Cancer
|
|
Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.
|
-
- HY-133084
-
|
ERK-IN-2
|
ERK
|
Cancer
|
|
ERK-IN-2 is a potent, highly seletive and orally active ERK2 inhibitor probe with an IC50 value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM.
|
-
- HY-136256
-
|
DCC-3014
|
c-Fms
c-Kit
|
Cancer
|
|
DCC-3014 is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively.
|
-
- HY-123242
-
|
FTI-2153
|
Farnesyl Transferase
|
Cancer
|
|
FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity.
|
-
- HY-111388B
-
|
SEL120-34A HCl
|
CDK
|
Cancer
|
|
SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-18009
-
|
LFM-A13
|
Btk
Polo-like Kinase (PLK)
JAK
|
Cancer
|
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
|
-
- HY-N4110
-
|
Friedelin
|
Cytochrome P450
|
Metabolic Disease
|
|
Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively.
|
-
- HY-N6816
-
|
Ludaconitine
|
Parasite
|
Infection
|
|
Ludaconitine, isolated from Aconitum spicatum (Bruhl) Stapf, exhibits antileishmanial activity with an IC50 of 36.10 μg/mL.
|
-
- 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-15433
-
|
Quisinostat
JNJ-26481585
|
HDAC
|
Cancer
|
|
Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively.
|
-
- HY-116761
-
|
GSK467
|
Histone Demethylase
|
Cancer
|
|
GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.
|
-
- HY-103254
-
|
ML221
|
Others
|
Neurological Disease
|
|
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
|
-
- HY-P1194A
-
|
Spantide I TFA
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
|
-
- HY-117639
-
|
AUT1
|
Potassium Channel
|
Cancer
|
|
AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
|
-
- HY-P1194
-
|
Spantide I
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
|
-
- HY-16916
-
-
- 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-B1424
-
|
Benzthiazide
|
Carbonic Anhydrase
|
Cardiovascular Disease
Cancer
|
|
Benzthiazide is a long-acting diuretic and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells.
|
-
- HY-125286
-
|
AB-680
|
CD73
|
Cancer
|
|
AB-680 is highly potent, reversible and selective small molecule inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity.
|
-
- 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-12522
-
|
PF-06380101
Aur0101; Auristatin-0101
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. PF-06380101 (Aur0101) shows excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.
|
-
- HY-15724A
-
|
Vercirnon sodium
GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
|
-
- HY-15724
-
|
Vercirnon
GSK-1605786; CCX282-B; Traficet-EN
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
|
-
- HY-20878
-
|
Tyrphostin AG 879
AG 879
|
Trk Receptor
EGFR
Apoptosis
|
Cancer
|
|
Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity.
|
-
- HY-13267
-
|
Droxinostat
NS 41080
|
HDAC
Apoptosis
|
Cancer
|
|
Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.
|
-
- HY-17547
-
|
NMS-E973
|
HSP
|
Cancer
|
|
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
|
-
- HY-109015S
-
|
Tucidinostat D4
Chidamide D4; HBI-8000 D4; CS 055 D4
|
HDAC
|
Cancer
|
|
Tucidinostat D4 (Chidamide D4) is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively.
|
-
- HY-B1101
-
|
Pimethixene
Pimetixene
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
|
-
- HY-B1101A
-
|
Pimethixene maleate
Pimetixene maleate
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
|
-
- HY-19339
-
|
Tenovin-3
|
MDM-2/p53
|
Cancer
|
|
Tenovin-3 is able to increase p53 levels, determined in MCF-7 cells treated for 6 hr at 10 μM.
|
-
- HY-13941B
-
|
1-Naphthyl PP1 hydrochloride
1-NA-PP 1 hydrochloride
|
Src
|
Cancer
|
|
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 hydrochloride inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.
|
-
- HY-13941
-
|
1-Naphthyl PP1
1-NA-PP 1
|
Src
|
Cancer
|
|
1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.
|
-
- HY-100131
-
|
GSK481
|
RIP kinase
|
Inflammation/Immunology
|
|
GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM.
|
-
- HY-N7450
-
-
- HY-15799
-
-
- HY-P1206
-
|
CH 275
|
Somatostatin Receptor
|
Neurological Disease
|
|
CH 275 is a potent and selective somatostatin receptor 1 (sst1) agonist and display IC50 values of 30.9 nM, 345 nM, >1 μM, >10 μM for human human sst1, sst3, sst4, sst2 and sst5 respectively. CH 275 can be used for the research of Alzheimer’s disease.
|
-
- 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-10046
-
-
- HY-N6775
-
|
Sonolisib
PX-866
|
PI3K
|
Cancer
|
|
Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
|
-
- HY-100530B
-
|
Sp-cAMPS
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.
|
-
- HY-15777S
-
|
Ribociclib D6
LEE011 D6
|
CDK
|
Cancer
|
|
Ribociclib D6 (LEE011 D6) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-100530C
-
|
Sp-cAMPS sodium salt
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
|
-
- HY-18901
-
|
RIPK1-IN-4
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase.
|
-
- HY-136175
-
|
SNDX-5613
|
Epigenetic Reader Domain
|
Cancer
|
|
SNDX-5613 is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).
|
-
- HY-109785A
-
|
(R)-Gyramide A hydrochloride
|
|
|
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-135797A
-
|
DB1976 dihydrochloride
|
Apoptosis
|
Cancer
|
|
DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 dihydrochloride has apoptosis-inducing effect.
|
-
- HY-10535
-
|
Evofosfamide
TH-302
|
Apoptosis
|
Cancer
|
|
Evofosfamide (TH-302) is a hypoxia-activated prodrug with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
|
-
- HY-17402
-
-
- HY-P1203
-
-
- HY-101281B
-
-
- HY-15145
-
-
- HY-50905
-
|
Dovitinib
CHIR-258; TKI258
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
|
-
- 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-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-129522
-
|
Sulfo-ara-F-NMN
CZ-48
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.
|
-
- HY-P1206A
-
|
CH 275 TFA
|
Somatostatin Receptor
|
Neurological Disease
|
|
CH 275 TFA is a potent and selective somatostatin receptor 1 (sst1) agonist and display IC50 values of 30.9 nM, 345 nM, >1 μM, >10 μM for human human sst1, sst3, sst4, sst2 and sst5 respectively. CH 275 can be used for the research of Alzheimer’s disease.
|
-
- HY-N5132
-
|
(-)-Fenchone
|
Others
|
Others
|
|
(-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Thuja occidentalis. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6.
|
-
- HY-B0278
-
|
Bacitracin Zinc
Zinc bacitracin
|
Bacterial
Antibiotic
|
Infection
|
|
Bacitracin Zinc (Zinc bacitracin) is a dephosphorylation of the C55-isoprenyl pyrophosphate interference for inhibition of cleavage of Tyr from Met-enkephalin with IC50 of 10 μM.
|
-
- HY-P1203A
-
-
- 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-12142
-
-
- HY-B1136
-
|
Menbutone
Genabilic acid
|
Others
|
Inflammation/Immunology
|
|
Menbutone is an oxobutyric acid derivative, and is a choleretic.Menbutone has a rapid onset of action, reaching its maximum plasma level within 1 hour and lasting for roughly 10 hours.
|
-
- HY-126140
-
|
MDRTB-IN-1
|
Bacterial
|
Infection
|
|
MDRTB-IN-1 (5aα) is an antibiotic which is against Mycobacterium tuberculosis H37Rv with a MIC90 value of 10.5 μM.
|
-
- HY-15510B
-
|
Tenovin-6 Hydrochloride
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
|
Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH).
|
-
- HY-107419
-
|
NU6140
|
CDK
Aurora Kinase
|
Cancer
|
|
NU6140 is a selective CDK2-cyclin A inhibitor (IC50, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs. NU6140 also potently inhibits Aurora A and Aurora B, with IC50s of 67 and 35 nM, respectively. Enhances the apoptotic effect, with anti-cancer activity.
|
-
- HY-15510
-
|
Tenovin-6
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
|
Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
|
-
- HY-N1363
-
-
- 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-14722A
-
|
NVP-BSK805 dihydrochloride
|
JAK
|
Cancer
|
|
NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
|
-
- HY-19962
-
|
Paxalisib
GDC-0084
|
PI3K
mTOR
|
Cancer
|
|
Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
|
-
- HY-12143
-
-
- HY-10207
-
|
Dovitinib lactate
CHIR-258 lactate; TKI-258 lactate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
|
-
- HY-16578
-
|
GW9662
|
PPAR
|
Cancer
|
|
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
|
-
- HY-10871
-
-
- HY-15971A
-
|
AMD 3465
GENZ-644494
|
CXCR
HIV
|
Infection
Endocrinology
|
|
AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
|
-
- HY-10221
-
|
Vorinostat
SAHA; Suberoylanilide hydroxamic acid
|
HDAC
Autophagy
Mitophagy
Filovirus
|
Cancer
Infection
|
|
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
|
-
- HY-106369
-
-
- HY-N2484
-
|
Methylnissolin
Astrapterocarpan
|
PDGFR
ERK
|
Cardiovascular Disease
|
|
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade.
|
-
- HY-113038
-
-
- HY-125108
-
-
- HY-N6785
-
|
Okadaic acid
|
Phosphatase
Parasite
Apoptosis
|
Infection
|
|
Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively. Okadaic acid eliminate metazoan symbionts/parasites by apoptosis.
|
-
- HY-101147
-
-
- HY-17377
-
|
Vicriviroc maleate
SCH-417690 maleate; SCH-D maleate
|
CCR
HIV
|
Infection
Endocrinology
|
|
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
|
-
- 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-107422
-
|
PAT-1251
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PAT-1251 is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 is used in the research of fibrotic diseases.
|
-
- HY-15971
-
|
AMD 3465 hexahydrobromide
GENZ-644494 hexahydrobromide
|
CXCR
HIV
|
Infection
Endocrinology
|
|
AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
|
-
- HY-19807
-
|
Indirubin-3'-monoxime
Indirubin-3'-oxime
|
GSK-3
Lipoxygenase
|
Cancer
|
|
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
|
-
- HY-16680
-
|
Helioxanthin 8-1
Helioxanthin analogue 8-1
|
HBV
|
Infection
|
|
Helioxanthin 8-1 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV/HCV/HSV-1/HIV activity with EC50 of >5/10/1.4/15 uM.
|
-
- HY-B1486
-
-
- HY-N6774
-
|
Cytochalasin C
|
Others
|
Infection
|
|
Cytochalasin C is a cell-permeable fungal toxin and induces the formation of nuclear rodlets. Cytochalasin C is 10 times less toxic in mice than is cytochalasin D.
|
-
- HY-N1272
-
|
Secaubryenol
|
Endogenous Metabolite
|
Others
|
|
Secaubryenol is a class of 3,4-secocycloartane triterpenes isolated from Coussarea macrophylla. Secaubryenol does not display any cytotoxic effect at a dose of 10 µg/mL.
|
-
- HY-P1682A
-
|
Balixafortide TFA
POL6326 TFA
|
CXCR
|
Cancer
|
|
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
|
-
- HY-113402A
-
|
Gamma-glutamylcysteine TFA
γ-glutamylcysteine TFA
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Gamma-glutamylcysteine (TFA) ((γ-glutamylcysteine (TFA)), an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine (TFA) also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β) and attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes.
|
-
- HY-103387
-
|
DuP-697
|
COX
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects.
|
-
- HY-123611
-
|
Supinoxin
RX-5902
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM.
|
-
- HY-90009C
-
|
ent-Tadalafil
ent-IC-351
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS). compound (6R,12aS) is a potent PDE5 inhibitor with an IC50 of 0.090 μM, while ent-Tadalafil is inactive at concentrations up to 10 µM.
|
-
- HY-A0077
-
|
Perphenazine
|
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
|
-
- HY-10678
-
|
BMS-687453
|
PPAR
|
Cardiovascular Disease
|
|
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
|
-
- HY-N0163
-
-
- HY-12149
-
|
A-867744
|
nAChR
Autophagy
|
Neurological Disease
|
|
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
|
-
- HY-100421
-
|
CPI-455
|
Histone Demethylase
|
Cancer
|
|
CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
|
-
- HY-109015
-
|
Tucidinostat
Chidamide; HBI-8000; CS 055
|
HDAC
|
Cancer
|
|
Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.
|
-
- HY-N2284
-
|
Sophoflavescenol
|
AChE
Beta-secretase
Phosphodiesterase (PDE)
|
Cancer
|
|
Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
|
-
- HY-18299
-
|
Purvalanol B
NG 95
|
CDK
|
Cancer
|
|
Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.
|
-
- HY-10322
-
|
Falnidamol
BIBX 1382
|
EGFR
|
Cancer
|
|
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
|
-
- 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-P1495
-
-
- HY-115658
-
|
VU0420373
|
Bacterial
|
Infection
Metabolic Disease
|
|
VU0420373 is a potent heme sensor system (HssRS) activator with an EC50 of 10.7 μM and a pEC50 of 4.97. VU0420373 induces heme biosynthesis, and is toxic to fermenting S. aureus.
|
-
- HY-121385
-
-
- HY-10032
-
|
PF 477736
PF 00477736
|
Checkpoint Kinase (Chk)
VEGFR
Src
c-Fms
Aurora Kinase
FGFR
FLT3
RET
CDK
|
Cancer
|
|
PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
|
-
- HY-100349
-
|
SU4312
|
PDGFR
VEGFR
|
Cancer
|
|
SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively.
|
-
- HY-N6791
-
|
KT5823
|
PKA
PKC
Bacterial
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
|
KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
|
-
- HY-100542
-
-
- HY-100113
-
-
- HY-16903
-
|
PKC-IN-1
|
PKC
|
Inflammation/Immunology
|
|
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
|
-
- HY-14892A
-
|
Gemigliptin tartrate
LC15-0444 tartrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
|
-
- HY-108044
-
|
ONO-5334
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.
|
-
- HY-80002
-
|
BMX-IN-1
BMX kinase inhibitor
|
Btk
BMX Kinase
|
Cancer
|
|
BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
|
-
- 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-136084
-
-
- 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-100781A
-
|
L-APB
L-AP 4
|
mGluR
|
Neurological Disease
|
|
L-APB is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively.
|
-
- HY-108539
-
|
CE3F4
|
Others
|
Cardiovascular Disease
|
|
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
|
-
- HY-W011955
-
-
- 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-108628
-
|
SU16f
|
PDGFR
|
Cancer
|
|
SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration.
|
-
- HY-124151
-
|
Adenosine-2'-monophosphate
2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate
|
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
|
-
- HY-112803
-
|
GNE-371
|
DNA/RNA Synthesis
|
Cancer
|
|
GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).
|
-
- HY-100483
-
|
A-804598
|
P2X Receptor
|
Cancer
|
|
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
|
-
- HY-10264B
-
|
Edoxaban tosylate monohydrate
DU-176b monohydrate
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Edoxaban tosylate monohydrate (DU-176b monohydrate) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate monohydrate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate monohydrate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate monohydrate has antithrombotic properties and has potential for thromboembolic diseases treatment.
|
-
- HY-10264
-
|
Edoxaban
DU-176
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment.
|
-
- 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-12597
-
|
Quisqualic acid
L-Quisqualic acid
|
iGluR
mGluR
|
Neurological Disease
|
|
Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis chinensis.
|
-
- HY-N2959
-
|
Brevilin A
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
|
Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
|
-
- HY-107417
-
|
Hypothemycin
|
VEGFR
MEK
FLT3
PDGFR
ERK
|
Cancer
|
|
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
|
-
- HY-13240
-
|
LY2886721
|
Beta-secretase
|
Neurological Disease
|
|
LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment.
|
-
- HY-114191A
-
-
- HY-N2016
-
|
Arteannuin B
|
SARS-CoV
Ferroptosis
|
Infection
|
|
Arteannuin B co-occurs with artemisinin, which is the potent antimalarial principle of the Chinese medicinal herb Artemisia annua (Asteraceae). Arteannuin B shows anti-SARS-CoV-2 potential with an EC50 of 10.28 μM.
|
-
- HY-15464
-
|
(R)-(-)-Gossypol
AT-101; R-(-)-gossypol acetic acid
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
|
-
- HY-B1213
-
-
- HY-14280A
-
|
Entacapone sodium salt
|
COMT
|
Neurological Disease
|
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as a inhibits FTO demethylation activity with an IC50 of 3.5 μM and can be used for the research of metabolic disorders.
|
-
- HY-14280
-
|
Entacapone
|
COMT
|
Neurological Disease
|
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibits FTO demethylation activity with an IC50 of 3.5 μM and can be used for the research of metabolic disorders.
|
-
- HY-108568
-
-
- 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-120323
-
|
DRI-C21045
|
TNF Receptor
|
Inflammation/Immunology
|
|
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively.
|
-
- HY-112429
-
|
HJB97
|
Epigenetic Reader Domain
|
Cancer
|
|
HJB97 is a high-affinity BET inhibitor with Kis of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity.
|
-
- HY-125269
-
|
TED-347
|
YAP
|
Cancer
|
|
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
|
-
- HY-114358
-
|
ONO-7475
|
TAM Receptor
Trk Receptor
|
Cancer
|
|
ONO-7475 is a potent, selective, and orally active novel Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. ONO-7475 sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. ONO-7475 combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
|
-
- HY-135582
-
|
Raloxifene 4'-glucuronide
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression.
|
-
- HY-111388A
-
|
SEL120-34A monohydrochloride
|
CDK
|
Cancer
|
|
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
|
-
- HY-101355B
-
-
- HY-12753S1
-
|
Debutyldronedarone D6 hydrochloride
SR35021 D6 hydrochloride
|
Others
|
Cardiovascular Disease
|
|
Debutyldronedarone D6 hydrochloride (SR35021 D6 hydrochloride) is deuterium labeled Debutyldronedarone. Debutyldronedarone is a major circulating active metabolite of dronedarone (HY-A0016) in humans. Debutyldronedarone exhibits a potency that is 1/10 to 1/3 of that of the parent agent.
|
-
- HY-19843
-
|
MK-0941
|
Glucokinase
|
Metabolic Disease
|
|
MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes.
|
-
- HY-100290
-
-
- HY-112762
-
|
LHF-535
|
Arenavirus
|
Infection
|
|
LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC50s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively.
|
-
- HY-15464A
-
|
(R)-(-)-Gossypol acetic acid
AT-101 (acetic acid); (-)-Gossypol acetic acid; (R)-Gossypol acetic acid
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
(R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
|
-
- HY-107018
-
|
AR-A 2
AR-A 000002
|
5-HT Receptor
|
Neurological Disease
|
|
AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
|
-
- HY-N0600
-
-
- HY-112617A
-
-
- HY-W014421
-
|
AP-18
|
TRP Channel
|
Neurological Disease
|
|
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM.
|
-
- HY-107691
-
|
GR 159897
|
Neurokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
|
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
|
-
- HY-N7176
-
|
Kaempferol 3-O-β-D-glucuronide
Kaempferol-3-glucuronide; Kaempferol-3-O-glucuronide
|
Interleukin Related
|
Inflammation/Immunology
|
|
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10.
|
-
- 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-136379
-
|
CID44216842
Cdc42-IN-1
|
Ras
|
Cancer
|
|
CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe.
|
-
- HY-B0324A
-
|
Crystal Violet
Basic Violet 3; Gentian Violet; Methyl Violet 10B
|
Influenza Virus
Bacterial
|
Infection
|
|
Crystal violet (Basic Violet 3) is a triarylmethane dye. Crystal Violet (Gentian Violet) has antiviral effects against H1N1 and also has prominent bactericidal activities.
|
-
- HY-13213
-
-
- HY-109035
-
|
Inarigivir soproxil
SB9200
|
HCV
|
Infection
|
|
Inarigivir soproxil is an agonist of innate immunity and shows potent antiviral activity against resistant hepatitis C virus (HCV) variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.
|
-
- HY-N1775
-
|
3',4'-Dihydroxyacetophenone
3,4-DHAP
|
Tyrosinase
|
Cancer
|
|
3',4'-Dihydroxyacetophenone (3,4-DHAP), isolated from Picea Schrenkiana Needles exhibits a strong suppressive action against tyrosinase activity, with an IC50 of 10 μM. 3',4'-Dihydroxyacetophenone (3,4-DHAP) is a vasoactive agent and antioxidant.
|
-
- HY-10238
-
|
Danoprevir
ITMN-191; R7227; RO5190591; RG7227
|
HCV Protease
HCV
|
Infection
|
|
Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM).
|
-
- HY-P2454
-
|
CSP1
|
Bacterial
|
Infection
|
|
CSP1 is a potent and selective ComD1 receptor agonist, with an IC50 of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent.
|
-
- 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-N4285
-
-
- HY-114739
-
|
MA-0204
|
PPAR
|
Metabolic Disease
|
|
MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).
|
-
- HY-N5020
-
|
Carabrone
|
Bacterial
|
Infection
|
|
Carabrone is isolated from the fruits of Carpesium abrotanoides , is a well-known sesquiterpene and exhibits significant anti-bacterial and anti-tumor activities.
Carabrone exhibits antifungal activities in vitro and in vivo against Botrytis cinerea, Colletotrichum lagenarium(EC50=7.10 μg/mL) and Erysiphe graminis.
|
-
- HY-19336
-
|
BAZ2-ICR
|
Epigenetic Reader Domain
|
Cancer
|
|
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
|
-
- HY-101513
-
|
eIF4A3-IN-1
|
Eukaryotic Initiation Factor (eIF)
Autophagy
|
Cancer
|
|
eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD.
|
-
- HY-13637
-
|
Ganciclovir
BW 759; 2'-Nor-2'-deoxyguanosine
|
CMV
HSV
Antibiotic
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1).
|
-
- HY-13637A
-
|
Ganciclovir sodium
BW 759 sodium; 2'-Nor-2'-deoxyguanosine sodium
|
CMV
HSV
Antibiotic
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Ganciclovir (BW 759) sodium, a nucleoside analogue and an orally active antiviral agent, shows activity against CMV. Ganciclovir sodium also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir sodium inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir sodium has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1).
|
-
- HY-B0822
-
|
Fipronil
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
|
|
Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC500s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
- HY-130504
-
|
Propargyl-PEG1-acid
|
PROTAC Linker
|
Cancer
|
|
Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM.
|
-
- HY-P1422
-
|
Spadin
|
Potassium Channel
|
Neurological Disease
|
|
Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice.
|
-
- HY-12456
-
|
Duocarmycin SA
|
ADC Cytotoxin
DNA Alkylator/Crosslinker
|
Cancer
|
|
Duocarmycin SA is a potent antitumor antibiotic with an IC50 of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.
|
-
- HY-B0708
-
-
- HY-103076
-
|
EZ-482
|
Others
|
Neurological Disease
|
|
EZ-482, a novel ligand of apolipoprotein (apoE), binds to sites on apoE in the C-terminal domain with Kds of 5-10 μM for apoE3 and apoE4. EZ-482 binds to apoE4 by a unique N-terminal allosteric effect. EZ482 has the potential for Alzheimer’s diseas.
|
-
- 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-108669
-
|
AZ10606120 dihydrochloride
|
P2X Receptor
|
Cancer
Neurological Disease
|
|
AZ10606120 dihydrochloride is a selective, high affinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of ~10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth.
|
-
- HY-129240S
-
|
13-cis Acitretin D3
Isoacitretin D3; Ro 13-7652 D3
|
Drug Metabolite
|
Inflammation/Immunology
|
|
13-cis Acitretin D3 （Isoacitretin D3） is a deuterium labeled 13-cis Acitretin. 13-cis Acitretin is the metabolite of Acitretin after chronic administration. Acitretin(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis.
|
-
- HY-14520
-
|
Tetrahydrofolic acid
L-5,6,7,8-Tetrahydrofolic acid; L-Tetrahydrofolic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid.
|
-
- HY-10182B
-
|
CHIR-99021 trihydrochloride
CT99021 trihydrochloride
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 trihydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 trihydrochloride induces autophagy.
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-
- HY-10182
-
|
CHIR-99021
CT99021
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
CHIR-99021 (CT99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 induces autophagy.
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- HY-P1422A
-
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Spadin TFA
|
Potassium Channel
|
Neurological Disease
|
|
Spadin TFA, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin TFA binds specifically to TREK-1 with an affinity of 10 nM. Spadin TFA is an efficient antidepressant in mice.
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-
- HY-14328
-
|
Sonepiprazole
PNU-101387G; U-101387G
|
Dopamine Receptor
|
Neurological Disease
|
|
Sonepiprazole (PNU-101387G) is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively.
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-
- HY-112762A
-
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(E)-LHF-535
|
Arenavirus
|
Infection
|
|
(E)-LHF-535 is the E-isomer of LHF-535. LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC50s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively.
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-
- HY-B1658A
-
|
Frovatriptan succinate hydrate
(R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research.
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-
- HY-B1658B
-
|
Frovatriptan succinate
(R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate
|
5-HT Receptor
|
Neurological Disease
|
|
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.
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-
- HY-103606
-
|
(S,R,S)-AHPC-PEG6-C4-Cl
VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9
|
PROTAC
|
Cancer
|
|
(S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
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-
- HY-103607
-
|
(S,R,S)-AHPC-PEG2-C4-Cl
VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10
|
PROTAC
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
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-
- HY-130992
-
-
- HY-100369A
-
|
DMCM hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.
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-
- HY-101254
-
|
Luzindole
N-0774
|
Melatonin Receptor
|
Neurological Disease
|
|
Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.
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-
- HY-103665
-
|
STING agonist-3
|
STING
|
Cancer
|
|
STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
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-
- HY-15514A
-
|
Merestinib dihydrochloride
LY2801653 dihydrochloride
|
c-Met/HGFR
FLT3
ROS
Discoidin Domain Receptor
|
Cancer
|
|
Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
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-
- HY-15514
-
|
Merestinib
LY2801653
|
c-Met/HGFR
FLT3
ROS
Discoidin Domain Receptor
|
Cancer
|
|
Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).
|
-
- HY-101299A
-
|
Dihydrexidine
DAR-0100
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity. Dihydrexidine can stimulate YAP phosphorylation.
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-
- HY-101299B
-
|
Dihydrexidine hydrochloride
DAR-0100 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity. Dihydrexidine hydrochloride can stimulate YAP phosphorylation.
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-
- HY-12152
-
|
PNU-120596
NSC 216666
|
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research.
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-
- HY-10182A
-
|
CHIR-99021 monohydrochloride
CT99021 monohydrochloride
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 monohydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 monohydrochloride induces autophagy.
|
-
- HY-129602
-
|
SD-36
|
PROTAC
STAT
Apoptosis
|
Cancer
|
|
SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of CRBN ligand Lenalidomide for E3 ubiquitin ligase.
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-
- HY-P2231A
-
|
Cotadutide acetate
MEDI0382 acetate
|
Glucagon Receptor
|
Metabolic Disease
|
|
Cotadutide acetate (MEDI0382 acetate) is a potent peptide dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor with EC50 values of 6.9 pM and 10.2 pM, respectively. Cotadutide acetate (MEDI0382 acetate) exhibits ability to facilitate both weight loss and glycaemic control, has the potential for obesity and type 2 diabetes (T2D) treatment.
|
-
- HY-W000434
-
|
Fmoc-NH-PEG4-CH2CH2COOH
Fmoc-15-amino-4,7,10,13-tetraoxapentadecanoic acid
|
ADC Linker
|
Cancer
|
|
Fmoc-NH-PEG4-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-112898
-
|
DC1SMe
|
ADC Cytotoxin
|
Cancer
|
|
DC1Sme, a DC1 derivative, exhibits IC50 values of 22 pM, 10 pM, 32 pM and 250 pM for Ramos, Namalwa, HL60/s and COLO 205 cancer cells, respectively. DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is a ADC Cytotoxin. DC1 can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.
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-
- HY-14300A
-
-
- HY-117621
-
|
PF-04634817
|
CCR
|
Metabolic Disease
|
|
PF-0463481 is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy.
|
-
- HY-14300
-
-
- HY-P1300
-
-
- HY-136250
-
|
BSJ-03-204
|
PROTAC
CDK
|
Cancer
|
|
BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity.
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-
- HY-P1300A
-
-
- HY-115613
-
|
ML-180
SR1848
|
Others
|
Cancer
|
|
ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers.
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-
- HY-12355
-
|
Siponimod
BAF-312
|
LPL Receptor
|
Others
|
|
Siponimod (BAF-312) is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. It is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively). Used to treat adult multiple sclerosis.
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-
- HY-P1274
-
|
ShK-Dap22
|
Potassium Channel
|
Inflammation/Immunology
|
|
ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.
|
-
- HY-W013712
-
|
GI-530159
|
Potassium Channel
|
Neurological Disease
|
|
GI-530159 is a selective, mechanosensitive opener of TREK1 (K2P2.1) and TREK2 (K2P10.1) channels, with an EC50 of 0.76 μM for TREK1. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels. GI-530159 reduces rat dorsal root ganglion neuron excitability.
|
-
- HY-P1321
-
|
GR231118
1229U91; GW1229
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8).
|
-
- HY-P1274A
-
|
ShK-Dap22 TFA
|
Potassium Channel
|
Inflammation/Immunology
|
|
ShK-Dap22 TFA is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 TFA is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.
|
-
- HY-P1321A
-
|
GR231118 TFA
1229U91 TFA; GW1229 TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8).
|
-
- HY-D1111
-
|
TFAX 568, SE
|
Others
|
|
|
TFAX 568, SE, an amine reactive orange fluorescent dye, is insensitive to pH in the range 4-10. TFAX 568, SE forms bright and photostable conjugates with proteins and antibodies. TFAX 568, SE is suitable for use in flow cytometry, 2-photon excitation microscopy, and super resolution mircoscopy techniques, such as dSTORM. Excitation maximum=578 nm; emission maximum=602 nm; quantum yield=0.69; extinction coefficient=60720 M-1cm-1.
|
-
- HY-136258
-
|
nAChR agonist CMPI hydrochloride
|
nAChR
|
Neurological Disease
|
|
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.
|
-
- HY-136207
-
|
TC-2559 difumarate
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
|
-
- HY-D1110
-
|
TFAX 594,SE
|
Others
|
|
|
TFAX 594,SE, an amine reactive red fluorescent dye, is insensitive to pH in the range 4-10. TFAX 594,SE forms bright and photostable conjugates with proteins and antibodies. TFAX 594,SE is suitable for use in flow cytometry, 2-photon excitation microscopy, and super resolution mircoscopy techniques, such as dSTORM. Excitation/emission maxima ~ 590 / 660 nm; extinction coefficient=92,000 M-1cm-1; quantum yield=0.66.
|
-
- HY-P1345
-
|
TLQP-21
|
Complement System
|
Endocrinology
Neurological Disease
|
|
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-D1114
-
|
TFAX 488,SE dilithium
|
Others
|
|
|
TFAX 488,SE dilithium, an amine reactive green fluorescent dye, is insensitive to pH in the range 4-10. TFAX 488,SE dilithium forms bright and photostable conjugates with proteins and antibodies. TFAX 488,SE dilithium is suitable for use in flow cytometry, two-photon excitation microscopy (TPE), and super resolution microscopy techniques, such as dSTORM, SIM and STED. Excitation maximum=495 nm; emission maximum=515 nm; extinction coefficient=73,000 M-1cm-1; quantum yield=0.92.
|
-
- HY-P1345A
-
|
TLQP-21 TFA
|
Complement System
|
Endocrinology
Neurological Disease
|
|
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-136254
-
|
BzATP triethylammonium salt
|
P2X Receptor
|
Cancer
Inflammation/Immunology
|
|
BzATP triethylammonium salt acts as a P2X receptor agonist with pEC50s of 8.74, 5.26, 7.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3, P2X2/3, P2X4 and P2X7, respectively. BzATP triethylammonium salt is potent at P2X7 receptors with EC50s of 3.6 μM and 285 μM for rat P2X7 and mouse P2X7, respectively.
|
-
- HY-107836
-
|
Methiothepin mesylate
Metitepine mesylate; Ro 8-6837 mesylate
|
5-HT Receptor
|
Neurological Disease
|
|
Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
|
-
- HY-108596
-
|
BL-1249
|
Potassium Channel
|
Inflammation/Immunology
|
|
BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
|
-
- HY-10121
-
|
Asenapine
Org 5222
|
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Asenapine is an antagonist of serotonin receptors (5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7), adrenoceptors (α1, α2A, α2B, α2C), dopamine receptors (D2, D3, D4) and histamine receptors (H 1, H2), with pKis of 8.4-10.5, 8.9-9.5, 8.9-9.4 and 8.2-9.0, respectively. Asenapine has antipsychotic activity, can be used in the research of schizophrenia and bipolar disorder.
|
-
- HY-10847B
-
|
SB-277011 hydrochloride
SB-277011A hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-D1113
-
|
TFAX 488,TFP
|
Others
|
|
|
TFAX 488,TFP, an amine reactive green fluorescent dye, is insensitive to pH in the range 4-10. TFAX 488,TFP forms bright and photostable conjugates with proteins and antibodies. TFAX 488,TFP is less susceptible to spontaneous hydrolysis during conjugation reactions compared to SE or NHS dyes. TFAX 488,TFP also displays greater stability compared to NHS and SE versions, typically lasting several hours. TFAX 488,TFP is suitable for use in flow cytometry, two-photon excitation microscopy (TPE), and super resolution microscopy techniques, such as dSTORM, SIM and STED. Excitation maximum=495 nm; emission maximum=515 nm; extinction coefficient=73,000 M-1cm-1; quantum yield=0.92.
|
-
- 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-32015
-
-
- 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-112812
-
-
- HY-B0552A
-
-
- HY-112911
-
-
- HY-B0552
-
-
- HY-18353
-
|
mTOR inhibitor-3
|
mTOR
|
Cancer
|
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
- HY-112722
-
-
- HY-D0843
-
|
N-Ethylmaleimide
NEM
|
Cathepsin
Deubiquitinase
|
Others
|
|
N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
|
-
- HY-101275
-
-
- HY-13278A
-
-
- HY-111412
-
-
- 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-70005
-
-
- HY-17541A
-
-
- HY-17541
-
-
- HY-112914
-
-
- HY-128703
-
-
- HY-136660
-
|
mTOR inhibitor-7
|
mTOR
|
Neurological Disease
|
|
mTOR inhibitor-7 is an orally available, and brain-penetrant mTOR inhibitor extracted from patent WO2017198346A1, compound example 44, has an IC50 of 5 nM for mTOR. mTOR inhibitor-7 can be used for the research of neurological disorder.
|
-
- HY-128722
-
-
- HY-110101
-
-
- HY-12202
-
-
- HY-B0543
-
-
- HY-10421
-
-
- HY-B0385
-
-
- HY-P0017
-
-
- HY-112843
-
|
CNT2 inhibitor-1
|
Others
|
Others
|
|
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
|
-
- HY-136279
-
|
TrxR inhibitor D9
|
Apoptosis
|
Cancer
|
|
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
|
-
- HY-101297
-
|
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-100732
-
|
Cambinol
|
Sirtuin
Apoptosis
Phospholipase
|
Cancer
|
|
Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-15182
-
-
- HY-112474
-
-
- HY-15358
-
-
- HY-B0732
-
-
- HY-15357
-
-
- HY-136920
-
-
- HY-13662
-
-
- HY-13662A
-
-
- HY-119937
-
-
- HY-15253
-
-
- HY-13973A
-
-
- HY-104051
-
-
- HY-111347A
-
-
- HY-131100
-
-
- HY-135890
-
-
- HY-15444
-
-
- HY-112390A
-
|
Syk Inhibitor II
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-114317
-
|
MARK4 inhibitor 1
|
Apoptosis
|
Cancer
|
|
MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
|
-
- HY-15002
-
|
AST 487
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-135826
-
|
Necroptosis-IN-1
|
RIP kinase
|
Cancer
|
|
Necroptosis-IN-1, an analog of Necrostatin-1 (HY-15760), is a potent necroptosi inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.
|
-
- HY-111408
-
-
- HY-N2033
-
-
- HY-100463
-
-
- HY-112607
-
|
Tubulin inhibitor 1
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
|
-
- HY-B0884
-
-
- HY-112569
-
-
- HY-B0884A
-
-
- HY-15167
-
-
- HY-50856A
-
-
- HY-117262
-
-
- HY-U00410
-
-
- HY-13276
-
-
- HY-B0218
-
-
- HY-106067A
-
-
- HY-124798
-
-
- HY-32018
-
|
Cot inhibitor-2
|
MAP3K
|
Cancer
|
|
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
|
-
- HY-N6717
-
|
Tentoxin
|
Others
|
Infection
|
|
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
|
-
- HY-17542
-
|
PLpro inhibitor
|
SARS-CoV
|
Infection
|
|
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
|
-
- HY-15760
-
-
- HY-13662B
-
|
(R)-Lansoprazole
Dexlansoprazole
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-10217
-
-
- HY-P1029
-
-
- HY-15604
-
-
- HY-15183
-
-
- HY-U00387
-
-
- HY-107986
-
-
- HY-10249A
-
-
- HY-100962
-
|
(E)-AG 99
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
|
EGFR
|
Cancer
|
|
(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
|
-
- HY-108322
-
-
- HY-13985
-
-
- HY-50880
-
-
- HY-N2221
-
-
- HY-14657
-
-
- HY-101932
-
-
- HY-N6902
-
-
- HY-U00319
-
-
- HY-15825
-
|
IWP L6
Porcn Inhibitor III
|
Porcupine
|
Cancer
|
|
IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
|
-
- HY-12072
-
-
- HY-13718
-
-
- HY-112269
-
-
- HY-128723
-
-
- HY-50879
-
-
- HY-104032
-
-
- HY-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-136270
-
|
ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-103310
-
-
- HY-122856
-
|
AZ12601011
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-B0083
-
|
Leflunomide
HWA486; RS-34821; SU101
|
Others
|
Cancer
|
|
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
|
-
- HY-101474A
-
|
Zanubrutinib
BGB-3111
|
Btk
|
Cancer
|
|
Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
|
-
- HY-16569
-
-
- HY-N7592
-
|
Arjunetin
|
Others
|
Others
|
|
Arjunetin, isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.
|
-
- HY-12186
-
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-100110
-
|
KNK437
Heat Shock Protein Inhibitor I
|
HSP
|
Cancer
|
|
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
|
-
- HY-135384
-
-
- HY-106638
-
-
- HY-100933
-
-
- HY-A0276
-
|
Gentamicin sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-119808
-
-
- HY-128729
-
|
DNA2 inhibitor C5
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
|
-
- HY-P2478
-
-
- HY-P2477
-
-
- HY-10917
-
|
GW2580
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
|
-
- HY-13417A
-
|
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-113951
-
-
- HY-124718
-
|
p32 Inhibitor M36
M36
|
PKC
|
Cancer
|
|
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
|
-
- HY-13417
-
|
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-P1260
-
-
- HY-19797A
-
-
- HY-14274
-
|
Anastrozole
ZD1033
|
Aromatase
|
Cancer
|
|
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
|
-
- HY-131101
-
|
Nor-Acetildenafil
|
Others
|
Others
|
|
Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
|
-
- HY-10846
-
-
- HY-18930
-
|
NU6300
|
CDK
|
Cancer
|
|
NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
|
-
- HY-W013478
-
-
- HY-15700
-
-
- HY-101429
-
|
RG13022
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-N2219
-
-
- HY-19795
-
|
ML240
|
p97
|
Cancer
|
|
ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.
|
-
- HY-112639
-
-
- HY-100600
-
|
BGG463
K03859
|
CDK
|
Others
|
|
BGG463 (K03859) is an orally active type II CDK2 inhibitor.
|
-
- HY-136461
-
-
- HY-P2564
-
-
- HY-15222
-
-
- HY-14196
-
-
- HY-17396
-
-
- HY-14440
-
|
MP7
PDK1 inhibitor
|
PDK-1
|
Cancer
|
|
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
|
-
- HY-50670
-
-
- HY-U00145
-
-
- HY-116770
-
|
PFM01
|
Others
|
Cancer
|
|
PFM01, N-alkylated Mirin derivative, is a MRE11 endonuclease inhibitor.
|
-
- HY-B0113A
-
|
Omeprazole sodium
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-111429
-
|
YAP/TAZ inhibitor-1
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μΜ in firefly luciferase assay.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- 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-15699A
-
-
- HY-B2063
-
|
Chlorobenzuron
|
Others
|
Others
|
|
Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate.
|
-
- HY-N1447
-
-
- HY-15167A
-
-
- HY-112634
-
-
- HY-133248
-
-
- HY-13972
-
-
- HY-15699
-
-
- HY-118165
-
-
- HY-B1596
-
-
- HY-P1260A
-
-
- HY-103593A
-
-
- HY-103593
-
|
LCL521
|
Phospholipase
|
Cancer
|
|
LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
|
-
- HY-I0637
-
-
- HY-16187
-
-
- HY-133247
-
-
- HY-D0886
-
-
- HY-18965
-
-
- HY-12277
-
|
AZ191
|
DYRK
|
Cancer
|
|
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
|
-
- HY-107451
-
-
- HY-107485
-
-
- HY-14174
-
-
- HY-N7511
-
-
- HY-N4294
-
-
- HY-B2007
-
-
- HY-13818
-
-
- HY-100498
-
|
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-14445
-
-
- HY-11009
-
|
CGP60474
|
VEGFR
PKC
|
Cancer
|
|
CGP60474 is a potent VEGFR-2 inhibitor, with an IC50 of 84 nM, and also an ATP-competitive PKC inhibitor.
|
-
- HY-19707
-
-
- HY-112822
-
|
ON-013100
|
CDK
|
Cancer
|
|
ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
|
-
- HY-100456
-
-
- HY-111493
-
-
- HY-100932
-
|
ML-9
|
Myosin
|
Cancer
|
|
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-B0113
-
|
Omeprazole
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-50706A
-
|
Selumetinib sulfate
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-105917
-
|
Endovion
NS3728
|
Chloride Channel
|
Others
|
|
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-13228
-
-
- HY-10227
-
|
Bortezomib
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-17367
-
|
Atazanavir
BMS-232632
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Infection
Cancer
|
|
Atazanavir (BMS-232632) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-12031A
-
-
- HY-U00453
-
-
- HY-112910
-
|
Grp94 Inhibitor-1
|
HSP
|
Cancer
Infection
|
|
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
|
-
- HY-15339
-
|
CVT-313
Cdk2 Inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
|
-
- 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-22166
-
-
- HY-W047428
-
-
- HY-112451
-
-
- HY-15217
-
-
- HY-13902
-
|
Berzosertib
VE-822; VX-970
|
ATM/ATR
|
Cancer
|
|
Berzosertib (VE-822) is an ATR inhibitor with a Ki value of less than 0.2 nM. It also inhibits ATM with a Ki of 34 nM.
|
-
- HY-15859
-
|
Atglistatin
|
ATGL
|
Metabolic Disease
|
|
Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC50 of 0.7 μM in vitro.
|
-
- HY-77521
-
-
- HY-13502
-
-
- HY-107994
-
-
- HY-N2567
-
|
(±)-Decursinol
|
Bacterial
|
Cancer
|
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-13278
-
-
- HY-112860
-
-
- HY-12000
-
-
- HY-A0116S
-
-
- HY-13060
-
-
- HY-101474
-
|
(±)-Zanubrutinib
(±)-BGB-3111
|
Btk
|
Cancer
|
|
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
|
-
- HY-19731
-
-
- HY-B0392
-
-
- HY-101462
-
-
- 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-101963
-
-
- HY-70073
-
-
- HY-15775
-
-
- HY-13502A
-
-
- HY-70003
-
-
- HY-112720
-
-
- HY-111784
-
-
- HY-10439
-
|
HPGDS inhibitor 1
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
|
-
- HY-100816
-
|
Rbin-1
Ribozinoindole-1
|
Phosphatase
|
Metabolic Disease
|
|
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
|
-
- HY-120675
-
|
SSTC3
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
|
-
- HY-100556
-
|
Tie2 kinase inhibitor 1
|
Others
|
Cancer
|
|
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
|
-
- HY-112715
-
-
- HY-14165
-
-
- HY-128918
-
|
SIS17
|
HDAC
|
Others
|
|
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
|
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-100932A
-
|
ML-9 Free Base
|
Myosin
|
Cancer
|
|
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-135318
-
|
NBDHEX
|
Glutathione Peroxidase
Apoptosis
Autophagy
|
Cancer
|
|
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
-
- HY-121172
-
|
1,4-DPCA
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
|
-
- HY-12364
-
-
- HY-P0081
-
-
- HY-133110
-
|
Afatinib N-Oxide
|
Others
|
Others
|
|
Afatinib N-Oxide is a impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor.
|
-
- HY-15798
-
-
- HY-N5038
-
|
Mauritianin
|
Topoisomerase
|
Cancer
|
|
Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor.
|
-
- HY-13606
-
|
Dacinostat
NVP-LAQ824; LAQ824
|
HDAC
Autophagy
|
Cancer
|
|
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
|
-
- HY-13256
-
-
- HY-P1452A
-
-
- HY-Y0882
-
-
- HY-16420
-
|
R112
|
Syk
|
Inflammation/Immunology
|
|
R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
|
-
- HY-111919
-
-
- HY-15588
-
-
- HY-B0830
-
|
Isoprocarb
|
AChE
|
Neurological Disease
|
|
Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.
|
-
- HY-N1502
-
|
Carboxyatractyloside
Gummiferin
|
Others
|
Cancer
|
|
Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.
|
-
- HY-12054A
-
-
- HY-114423
-
-
- HY-10809
-
|
Bitopertin
RG1678; RO4917838
|
GlyT
|
Neurological Disease
|
|
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
|
-
- HY-19609
-
-
- HY-131268
-
-
- HY-N6619A
-
|
Lycoramine
|
AChE
|
Neurological Disease
|
|
Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor.
|
-
- HY-104028
-
-
- HY-12814
-
|
TH588
|
DNA/RNA Synthesis
|
Cancer
|
|
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
|
-
- HY-12054
-
-
- 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-16982
-
|
Cercosporamide
(-)-Cercosporamide
|
Fungal
MNK
|
Cancer
Infection
|
|
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
|
-
- HY-136347
-
-
- HY-13280
-
-
- HY-N4186
-
-
- 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-B0497B
-
-
- HY-131446
-
|
Chk1-IN-5
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
|
-
- HY-50202
-
|
Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-19727A
-
-
- HY-50202A
-
|
Etomoxir sodium salt
(R)-(+)-Etomoxir sodium salt
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- 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-103490
-
|
Takinib
|
MAP3K
Apoptosis
|
Cancer
|
|
Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
|
-
- HY-17367A
-
|
Atazanavir sulfate
BMS-232632 sulfate
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Cancer
Infection
|
|
Atazanavir sulfate (BMS-232632 sulfate) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate (BMS-232632 sulfate) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-122866
-
|
ZT-12-037-01
|
Ras
|
Cancer
|
|
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.
|
-
- HY-100227
-
|
E 64c
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-66004
-
|
4-Acetamidophenyl acetate
|
Others
|
Inflammation/Immunology
|
|
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
|
-
- HY-115502
-
|
BCI
(E)-BCI
|
Phosphatase
|
Cancer
Inflammation/Immunology
|
|
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
|
-
- HY-15766A
-
|
GNE-617 hydrochloride
|
Nampt
|
Cancer
|
|
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-15233
-
|
Letermovir
AIC246
|
CMV
|
Infection
|
|
Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
|
-
- HY-12399
-
|
MKC9989
|
IRE1
|
Cancer
|
|
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
|
-
- HY-101053
-
|
Src Inhibitor 1
Src Kinase Inhibitor 1; Src-l1
|
Src
|
Cancer
|
|
Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
|
-
- HY-10247
-
|
BRAF inhibitor
|
Raf
|
Cancer
|
|
BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
|
-
- HY-N2522
-
-
- HY-109565
-
|
ASTX660
|
IAP
|
Cancer
|
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-108820
-
-
- HY-108817
-
-
- HY-10978
-
-
- HY-13452
-
-
- HY-119459
-
|
Fluopyram
|
Fungal
|
Infection
|
|
Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL.
|
-
- HY-135383A
-
-
- HY-17469
-
|
Gimeracil
Gimestat
|
Others
|
Cancer
|
|
Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.
|
-
- HY-A0122
-
-
- HY-17381
-
-
- HY-N6031
-
|
Dendrophenol
|
NF-κB
|
Cancer
|
|
Dendrophenol, isolated from the stem of Dendrobium loddigesii Rolfe, act as a NF-κB inhibitor. Antineoplastic activity.
|
-
- HY-Y0172
-
-
- HY-108941
-
|
Salicyl-AMS
|
Bacterial
|
Infection
|
|
Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.
|
-
- HY-15282
-
-
- HY-B0806
-
|
Proguanil
|
Parasite
Antifolate
|
Infection
|
|
Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
|
-
- HY-N2597
-
-
- HY-B0806A
-
-
- HY-13420
-
-
- HY-100736
-
|
ML348
GNF-Pf-1127
|
Phospholipase
|
Cancer
|
|
ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2.
|
-
- HY-15202
-
|
Binimetinib
MEK162; ARRY-162; ARRY-438162
|
MEK
Autophagy
|
Cancer
|
|
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
|
-
- HY-18988
-
|
ETC-159
ETC-1922159
|
Wnt
|
Cancer
|
|
ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
|
-
- HY-12726
-
-
- HY-N1724
-
-
- HY-15766
-
|
GNE-617
|
Nampt
|
Metabolic Disease
Cancer
|
|
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-111489B
-
-
- HY-126253
-
|
BI-4916
|
Others
|
Cancer
|
|
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD +-competitive PHGDH inhibitor.
|
-
- HY-136485
-
-
- HY-B1863
-
|
Iprobenfos
|
Fungal
|
Infection
|
|
Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor.
|
-
- HY-B0882
-
|
Edrophonium chloride
|
AChE
|
Neurological Disease
|
|
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-100899
-
-
- HY-101705
-
-
- HY-14807
-
-
- HY-P1045
-
|
187-1, N-WASP inhibitor
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-124653
-
|
HSP27 inhibitor J2
J2
|
HSP
|
Cancer
|
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
|
-
- HY-P1045A
-
|
187-1, N-WASP inhibitor TFA
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-P1111A
-
|
Lyn peptide inhibitor TFA
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-135899
-
|
SIRT7 inhibitor 97491
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
|
-
- 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-107412
-
|
Proteasome inhibitor IX
PS-IX; AM114
|
Proteasome
|
Cancer
|
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
|
-
- HY-130795
-
|
GSK-3β inhibitor 2
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-N7674A
-
|
Angoline hydrochloride
|
STAT
|
Cancer
|
|
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-13624A
-
|
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P1290
-
|
PKA Inhibitor Fragment (6-22) amide
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-N7674
-
|
Angoline
|
STAT
|
Cancer
|
|
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-109019
-
|
Vorolanib
CM082; X-82
|
VEGFR
PDGFR
|
Cancer
Cardiovascular Disease
|
|
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
|
-
- HY-100734
-
-
- HY-123772
-
|
CDK5 inhibitor 20-223
|
CDK
|
Cancer
|
|
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
|
-
- HY-13624
-
|
Epirubicin
4'-Epidoxorubicin
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
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- HY-N6619
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-
- HY-109877
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-
- HY-100299
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-
- HY-P2470
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-
- HY-B0106
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-
- HY-137239
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-
- HY-100303A
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FR194738
|
Others
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Metabolic Disease
|
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FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
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- HY-50946
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- HY-15886
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-
- HY-112131
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-
- HY-19326
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-
- HY-12971
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Nampt-IN-1
LSN3154567
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Nampt
|
Cancer
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Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
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- HY-101479
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Iclaprim
AR-100
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Bacterial
|
Infection
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Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
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- HY-108900A
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-
- HY-N5118
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Chimonanthine
(-)-Chimonanthine
|
Tyrosinase
|
Cancer
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Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.
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-
- HY-U00049
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-
- HY-16904
-
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RI-2
|
RAD51
|
Cancer
|
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RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
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- HY-130760
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-
- HY-103036
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-
- HY-111410
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-
- HY-13229
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BOC-D-FMK
|
Caspase
|
Cancer
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Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
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-
- HY-10862
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FAAH inhibitor 1
Benzothiazole analog 3
|
FAAH
Autophagy
|
Cancer
|
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FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM.
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- HY-13256A
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