Search Result
Results for "Amine containing corrosion Inhibitors" in MCE Product Catalog:
7839
Inhibitors & Agonists
15
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-U00439
-
-
- HY-140649
-
-
- HY-140648
-
-
- HY-140646
-
-
- HY-140650
-
-
- HY-140647
-
-
- HY-B1092A
-
|
Gluconate sodium
D-Gluconic acid sodium salt; Sodium D-gluconate; D-Gluconate sodium salt
|
Endogenous Metabolite
|
Others
|
|
Gluconate sodium (D-Gluconic acid sodium salt) is a corrosion and scale inhibitor of ordinary steel in simulated cooling water.
|
-
- HY-B1798A
-
|
Tocainide hydrochloride
|
Sodium Channel
|
Inflammation/Immunology
|
|
Tocainide hydrochloride is a sodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus.
|
-
- HY-126976
-
|
Propargyl-PEG5-amine
|
ADC Linker
PROTAC Linker
|
Cancer
|
|
Propargyl-PEG5-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
|
-
- HY-W051634
-
|
Propargyl-PEG2-amine
|
ADC Linker
PROTAC Linker
|
Cancer
|
|
Propargyl-PEG2-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
|
-
- HY-130435
-
|
DBCO-PEG4-amine
|
ADC Linker
|
Cancer
|
|
DBCO-PEG4-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-amine can be used in the synthesis of FPM-PEG4-DBCO (a homobifunctional azide-to-azide cross-linker).
|
-
- HY-W040289
-
|
Mal-amido-PEG2-NHS ester
|
ADC Linker
|
Cancer
|
|
Mal-amido-PEG2-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-140215
-
|
Azido-PEG6-amine
|
PROTAC Linker
ADC Linker
|
Cancer
|
|
Azido-PEG6-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-amine is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- 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-140227
-
|
m-PEG12-amine
|
PROTAC Linker
ADC Linker
|
Cancer
|
|
m-PEG12-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. m-PEG12-amine is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-133230
-
-
- HY-114670
-
-
- HY-130373
-
-
- HY-141178
-
-
- HY-141181
-
-
- HY-133495
-
-
- HY-140742
-
-
- HY-140283
-
-
- HY-140285
-
-
- HY-23105
-
-
- HY-140282
-
-
- HY-140008
-
-
- HY-140284
-
-
- HY-130659
-
-
- HY-140210
-
-
- HY-130447
-
-
- HY-140219
-
-
- HY-141262
-
-
- HY-140743
-
-
- HY-140034
-
-
- HY-140217
-
-
- HY-140229
-
-
- HY-140209
-
-
- HY-140220
-
-
- HY-141261
-
-
- HY-140216
-
-
- HY-140901
-
-
- HY-140214
-
-
- HY-140218
-
-
- HY-141180
-
-
- HY-140230
-
-
- HY-141179
-
-
- HY-140033
-
-
- HY-135822
-
-
- HY-141177
-
-
- HY-141080
-
-
- HY-140035
-
-
- HY-140212
-
-
- HY-140897
-
-
- HY-133505
-
-
- HY-140211
-
-
- HY-W040236
-
-
- HY-130408
-
-
- HY-W018174
-
-
- HY-120237
-
-
- HY-W040214
-
-
- HY-W008429
-
-
- HY-130571
-
-
- HY-140895
-
-
- HY-140896
-
-
- HY-140900
-
-
- HY-140899
-
-
- 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-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-126507
-
|
Mal-amido-PEG1-C2-NHS ester
|
ADC Linker
|
Cancer
|
|
Mal-amido-PEG1-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-135140
-
|
Methyltetrazine-Amine
|
Others
|
Others
|
|
Methyltetrazine-Amine is a tetrazine compound, is used for the site-specific dual functionalization of the resulting bioconjugates.
|
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- HY-114750
-
-
- HY-141176
-
-
- HY-W000423
-
-
- HY-135961
-
-
- HY-136086
-
-
- HY-140244
-
-
- HY-125924
-
|
DSPE-PEG(2000)-Amine
|
Others
|
Others
|
|
DSPE-PEG(2000)-Amine is used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents.
|
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- HY-136047
-
-
- HY-130939
-
-
- HY-130977
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-
- HY-136186
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-
- HY-130324
-
-
- HY-130169
-
-
- HY-W053709
-
|
Tetrazine-Amine
|
Others
|
Cancer
|
|
Tetrazine-Amine is a tetrazine linker that can be used to covalently label live cells through a cycloaddition.
|
-
- HY-133366
-
-
- HY-140976
-
-
- HY-140428
-
-
- HY-140238
-
-
- HY-135083
-
-
- HY-140286
-
-
- HY-141178A
-
-
- HY-141010
-
-
- HY-133368
-
-
- HY-140233
-
-
- HY-133367
-
-
- HY-140231
-
-
- HY-W018291
-
-
- HY-43721
-
|
N-Boc-4-pentyne-1-amine
|
PROTAC Linker
|
Cancer
|
|
N-Boc-4-pentyne-1-amine is a PROTAC linker, which refers to the alkyl chain composition. N-Boc-4-pentyne-1-amine can be used in the synthesis of the PROTAC MG-277 (HY-130122).
|
-
- HY-141055
-
-
- HY-136269
-
-
- HY-136274
-
-
- HY-128064
-
-
- HY-133695
-
|
Florfenicol amine
|
Others
|
Infection
|
|
Florfenicol amine is a metabolite of Florfenicol (HY-B1374). Florfenicol, a veterinary antibiotic, is used in aquaculture to control susceptible bacterial diseases.
|
-
- HY-140429
-
-
- HY-127056
-
-
- HY-135978
-
-
- HY-135972
-
-
- HY-136039
-
-
- HY-110303
-
-
- HY-W015088
-
-
- HY-140287
-
-
- HY-140288
-
-
- HY-22335
-
-
- 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-130411
-
|
Amino-PEG11-amine
|
PROTAC Linker
|
Cancer
|
|
Amino-PEG11-amine, a PEG-based (12 units) 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-140243
-
-
- HY-W012896
-
|
2-Thiohydantoin
|
Others
|
Others
|
|
2-Thiohydantoin acts as an inhibitor for the corrosion of mild steel in 0.1 M HCl and its inhibition efficiency is both concentration and immersion time dependent.
|
-
- HY-140570
-
-
- HY-140573
-
-
- HY-116677
-
-
- HY-128925
-
|
AMAS
|
ADC Linker
|
Cancer
|
|
AMAS is a nonclaevable heterobifunctional crosslinker with NHS ester and maleimide groups that allows covalent conjugation of amine- and sulfhydryl-containing molecules.
|
-
- HY-129655
-
|
Sulfo-SMPB sodium
|
ADC Linker
|
Cancer
|
|
Sulfo-SMPB sodium is a non-cleavable, heterobifunctional chemical cross-linking reagent which contains N-hydroxysuccinimide (NHS) ester and maleimide groups, allowing covalent conjugation of amine- and sulfhydryl-containing molecules.
|
-
- HY-141004
-
-
- HY-140426
-
-
- HY-133504
-
-
- HY-124386
-
|
DBCO-NHCO-PEG4-amine
|
ADC Linker
|
Cancer
|
|
DBCO-NHCO-PEG4-amine is a cleavable ADC linker used to conjugate MMAE (HY-15162) and antibody (e.g., DBCO-VCpAB−MMAE and DBCO-TRX−MMAE with EC50s of 280 nM and 22 nM in SKBR3 cells, respectively).
|
-
- HY-136272
-
-
- HY-136273
-
-
- HY-140632
-
-
- HY-140246
-
-
- HY-W002820
-
|
2-Amino-5-phenylpyridine
|
Endogenous Metabolite
|
Cancer
|
|
2-Amino-5-phenylpyridine is a mutagenic heterocyclic aromatic amine that is formed by pyrolysis of phenylalanine in proteins. 2-Amino-5-phenylpyridine is in broiled sardines and is considered as potentially carcinogenic.
|
-
- HY-140651
-
-
- HY-140652
-
-
- HY-140655
-
-
- HY-140661
-
-
- HY-140716
-
-
- HY-140641
-
-
- HY-140654
-
-
- HY-140653
-
-
- HY-140713
-
-
- HY-140735
-
-
- HY-140734
-
-
- HY-140662
-
-
- HY-140663
-
-
- HY-140715
-
-
- HY-140714
-
-
- HY-141182
-
-
- HY-135410
-
|
ABZ-amine
Amino albendazole
|
Others
|
Infection
|
|
ABZ-amine (Amino albendazole) is an impurity of Albendazole. Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
|
-
- HY-140248
-
-
- HY-140237
-
-
- HY-133403A
-
-
- HY-140726
-
-
- HY-140727
-
-
- HY-140725
-
-
- HY-130945
-
-
- HY-141008
-
-
- HY-140251
-
-
- HY-140249
-
-
- HY-140250
-
-
- HY-Y0015
-
|
p-Dimethylaminobenzaldehyde
4-Dimethylaminobenzaldehyde
|
Others
|
Others
|
|
p-Dimethylaminobenzaldehyde (4-Dimethylaminobenzaldehyde) is an organic compound containing amine and aldehyde moieties which is used in Ehrlich's reagent and Kovac's reagent to test for indoles.
|
-
- HY-133327
-
-
- HY-133329
-
-
- HY-133330
-
-
- HY-133328
-
-
- HY-140645
-
-
- HY-140644
-
-
- HY-140643
-
-
- HY-141252
-
-
- HY-131005
-
-
- HY-141057
-
-
- HY-130871A
-
-
- HY-140213
-
|
Azido-PEG2-C2-amine
N3-PEG2-CH2CH2NH2
|
PROTAC Linker
ADC Linker
|
Cancer
|
|
Azido-PEG2-C2-amine (N3-PEG2-CH2CH2NH2) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG2-C2-amine is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-121879
-
-
- 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-141065
-
-
- 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-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-B0135A
-
|
Furosemide sodium
|
NKCC
|
Cancer
Metabolic Disease
|
|
Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-B0135
-
|
Furosemide
|
NKCC
|
Metabolic Disease
Cancer
|
|
Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-22044
-
|
ICA
N-[4-(2-Pyridinyl)-2-thiazolyl]-2-pyridinAmine
|
Parasite
|
Infection
Cardiovascular Disease
|
|
ICA (N-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine) is a SK channel inhibitor that has antileishmanial activity with an IC50 of 2.1 µM.
|
-
- 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-18685
-
-
- HY-19985
-
-
- 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-W000438
-
-
- HY-13777
-
|
Zoledronic Acid
Zoledronate; CGP 42446; CGP42446A; ZOL 446
|
Autophagy
|
Cancer
|
|
Zoledronic Acid is a third-generation, nitrogen-containing bisphosphonate, inhibits osteoclast-mediated bone resorption, and also has antitumor activity.
|
-
- HY-13777A
-
|
Zoledronic acid monohydrate
Zoledronate monohydrate; CGP 42446 monohydrate; CGP42446A monohydrate; ZOL 446 monohydrate
|
Autophagy
|
Cancer
|
|
Zoledronic acid monohydrate is a third-generation, nitrogen-containing bisphosphonate, inhibits osteoclast-mediated bone resorption, and also has antitumor activity.
|
-
- HY-114157
-
|
DO-264
|
MAGL
|
Neurological Disease
|
|
DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM.
|
-
- 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-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-50769
-
-
- HY-12642
-
|
Diethylcarbamazine citrate
|
Parasite
|
Infection
|
|
Diethylcarbamazine citrate is an inhibitor of arachidonic acid metabolism in filarial microfilaria; is highly specific for several parasites and does not contain any toxic metallic elements.
|
-
- HY-16586
-
-
- HY-119254
-
|
BAY-850
|
Others
|
Metabolic Disease
|
|
BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC50 of 166 nM.
|
-
- HY-W016785
-
-
- HY-101748
-
-
- HY-B0446
-
-
- HY-15583
-
-
- HY-117286
-
|
(S)-JQ-35
TEN-010
|
Epigenetic Reader Domain
|
Cancer
|
|
(S)-JQ-35 (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity.
|
-
- HY-133644
-
-
- HY-133643
-
-
- 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-13343
-
|
ZM 336372
|
Raf
Apoptosis
|
Cancer
|
|
ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC50 value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.
|
-
- HY-113523
-
-
- HY-130521
-
|
Pomalidomide-amido-PEG3-C2-NH2
Cereblon Ligand-Linker Conjugates 22; E3 ligase Ligand-Linker Conjugates 55
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Pomalidomide-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-P2292
-
|
Omiganan-FITC
|
Bacterial
Fungal
|
Infection
|
|
Omiganan-FITC is a peptide-FITC complex composed of Omiganan and a FITC. Omiganan is a bactericidal and fungicidal cationic peptide being developed as a topical gel for prevention of catheter-associated infections. FITC is a derivative of fluorescein for the labeling of amines.
|
-
- HY-13803C
-
|
Tazemetostat hydrobromide
EPZ-6438 hydrobromide; E-7438 hydrobromide
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC50 of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-B0515B
-
-
- HY-B0515A
-
|
Ibandronic acid
|
Others
|
Cancer
|
|
Ibandronic acid is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.
|
-
- HY-B0515
-
-
- HY-B1426
-
-
- HY-B0730
-
-
- 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-120215
-
|
KT203
|
MAGL
|
Metabolic Disease
|
|
KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
|
-
- HY-19776
-
-
- HY-120177
-
|
KT182
|
MAGL
|
Others
|
|
KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
|
-
- HY-B0949
-
-
- HY-U00316
-
-
- HY-16141
-
|
Cilengitide
EMD 121974
|
Integrin
Autophagy
|
Cancer
|
|
Cilengitide, a cyclic RGD-containing peptide, is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50s of 4 and 79 nM, respectively.
|
-
- HY-13803
-
|
Tazemetostat
EPZ-6438; E-7438
|
Histone Methyltransferase
|
Cancer
|
|
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
|
-
- HY-N0170
-
-
- HY-B1000
-
-
- HY-B2118
-
-
- HY-15383
-
|
Glyparamide
|
Others
|
Others
|
|
Glyparamide is a chlorophenyl-containing sulfonylurea with hypoglycemic activity; Glyparamide rarely causes hepatic injury.
|
-
- HY-19424
-
-
- HY-U00393
-
-
- HY-B2132
-
-
- HY-B0991
-
|
Amoxapine
CL-67772
|
Others
|
Neurological Disease
|
|
Amoxapine is a tetracyclic antidepressant of the dibenzoxazepine family, though it is often classified as a secondary amine tricyclic antidepressant.
|
-
- HY-130684
-
|
MDM2-IN-1
|
MDM-2/p53
|
Cancer
|
|
MDM2-IN-1 (Compound 30) is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration.
|
-
- HY-112149
-
-
- HY-B1260
-
|
Cetrimonium bromide
CTAB; Cetyltrimethylammonium bromide; Hexadecyltrimethylammonium bromide
|
Others
|
Others
|
|
Cetrimonium bromide (CTAB) is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
|
-
- HY-131097
-
-
- HY-101540
-
-
- HY-100374
-
|
Val-Cit-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.
|
-
- HY-50846
-
|
SCH772984
|
ERK
|
Cancer
|
|
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
|
-
- HY-B1526
-
|
Thiacetazone
Thioacetazone; Amithiozone
|
Bacterial
|
Infection
|
|
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL.
|
-
- HY-111879
-
|
Biotin-BS
|
SNIPER
|
Cancer
|
|
Biotin-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and biotin, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.
|
-
- HY-19537
-
-
- HY-101415
-
-
- HY-131091
-
-
- HY-12424
-
|
Zotarolimus
ABT-578; A 179578
|
Others
|
Cancer
|
|
Zotarolimus is a tetrazole-containing Rapamycin analog which is used as animmunomodulator, and is useful in the treatment of restenosis, immune, and autoimmune diseases.
|
-
- HY-18699
-
-
- HY-B0528A
-
-
- HY-W040222
-
-
- HY-19347
-
-
- HY-13993A
-
-
- HY-N7436
-
-
- HY-D0799
-
-
- HY-103638
-
-
- HY-113356
-
-
- HY-N6772
-
|
Cytochalasin E
|
Autophagy
|
Cancer
|
|
Cytochalasin E, an epoxide containing Aspergillus-derived fungal metabolite, inhibits angiogenesis and tumor growth. Cytochalasin E is a potent actin depolymerization agent, and it binds and caps the barbed end of actin filaments to prevent actin elongation.
|
-
- HY-W009301
-
-
- HY-108315
-
-
- HY-19757
-
|
Lp-PLA2 -IN-1
|
Phospholipase
|
Cancer
|
|
Lp-PLA2 -IN-1 inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.
|
-
- HY-12523
-
|
Peptide M
|
Others
|
Others
|
|
Peptide M is a 50 aa synthetic peptide derived from a streptococcal M protein containing an additional C-terminal cysteine residue.
|
-
- HY-126505
-
-
- HY-130085
-
-
- HY-126506
-
-
- HY-126504
-
-
- HY-108285
-
|
(Rac)-Telmesteine
|
Others
|
Inflammation/Immunology
|
|
(Rac)-Telmesteine is a protease inhibitor and is thus a suitable enzyme stabilizer extracted from patent WO 2017220302 A1, compound II-1. (Rac)-Telmesteine can be used as an enzyme stabilizer in protease-containing detergents and cleaning agents.
|
-
- HY-128975
-
-
- HY-11048
-
|
NS11394
|
GABA Receptor
|
Neurological Disease
|
|
NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
|
-
- HY-N2156
-
-
- HY-10996A
-
-
- HY-122898
-
|
Ru360
|
Calcium Channel
Mitochondrial Metabolism
|
Cardiovascular Disease
|
|
Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca 2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects.
|
-
- HY-23642
-
-
- HY-130084
-
-
- HY-Y1416
-
-
- HY-133137
-
|
SJF620
|
PROTAC
Btk
|
Cancer
|
|
SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
|
-
- HY-D0975
-
|
Sulfo-SMCC sodium
|
ADC Linker
|
Cancer
|
|
Sulfo-SMCC sodium is a commonly used hetero-bifunctional, noncleavable ADC crosslinker bearing N-hydroxysuccinimide (NHS) ester and maleimide groups to react with primary amines and sulfhydryl groups, respectively.
|
-
- HY-112705
-
|
VU0529331
|
Potassium Channel
|
Neurological Disease
|
|
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
|
-
- HY-117275
-
|
Meclofenamic acid
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Meclofenamic Acid, a non-steroidal, anti-inflammatory agent, is a highly selective fat mass and obesity-associated (FTO) enzyme inhibitor. Meclofenamic Acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker.
|
-
- HY-114334
-
|
Glutaminase-IN-1
CB839 derivative
|
Glutaminase
|
Cancer
|
|
Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
|
-
- HY-130994
-
|
Aeruginosin 865
|
NF-κB
ADC Cytotoxin
|
Cancer
Inflammation/Immunology
|
|
Aeruginosin 865, isolated from terrestrial cyanobacterium Nostoc sp. Lukešová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety. Aeruginosin 865 inhibits translocation of NF-kB to the nucleus. Aeruginosin 865 has anti-inflammatory effect
|
-
- HY-18686
-
|
AS1949490
|
Phosphatase
|
Metabolic Disease
|
|
AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes.
|
-
- HY-18979
-
|
Lactimidomycin
|
Influenza Virus
|
Cancer
Infection
|
|
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities.
|
-
- HY-100503
-
|
Maytansinoid DM4
|
ADC Cytotoxin
|
Cancer
|
|
Maytansinoid DM4 is a thiol-containing maytansine derivative with highly potent cytotoxicity. Maytansinoid DM4 can be used as a cytotoxic moiety of ADC.
|
-
- HY-124669
-
|
RTC-30
|
Others
|
Cancer
|
|
RTC-30 is an optimized phenothiazine with anti-cancer potency. RTC-30 contains a hydroxylated linker (N) that confers increased oral bioavailability.
|
-
- HY-104031
-
|
tCFA15
|
Notch
|
Neurological Disease
|
|
tCFA15 is a trimethyl cyclohexenonic long chain fatty alcohol containing 15 carbon atoms on the side chain, promotes the differentiation of neurons, and may regulates Notch signaling.
|
-
- HY-130999
-
|
Microcolin B
|
Others
|
Inflammation/Immunology
|
|
Microcolin B is an extremely potent unusual acylpeptide, proline-containing potent immunosuppressant. Microcolin B is isolated from blue-green alga Lyngbya majuscule.
|
-
- HY-113949
-
-
- HY-B0853
-
|
Paclobutrazol
|
Fungal
|
|
|
Paclobutrazol is a triazole-containing plant growth retardant that is known to inhibit the biosynthesis of gibberellins. Paclobutrazol also has antifungal activities. Paclobutrazol, transported acropetally in plants, can also suppress the synthesis of abscisic acid and induce chilling tolerance in plants.Paclobutrazol is typically used to support research on the role of gibberellins in plant biology.
|
-
- HY-B1132
-
|
Clidinium bromide
Ro 2-3773
|
mAChR
|
Neurological Disease
|
|
Clidinium bromide is a quaternary amine antimuscarinic agent. Clidinium bromide may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines in vivo.
|
-
- HY-P1365
-
|
α-Conotoxin MII
α-CTxMII
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-130768
-
-
- HY-P1043A
-
|
NGR peptide Trifluoroacetate
|
Aminopeptidase
|
Cancer
|
|
NGR peptide Trifluoroacetate containing the asparagine-glycine-arginine (NGR) motif is recognized by CD13/aminopeptidase N (APN) receptor isoforms that are selectively overexpressed in tumor neovasculature.
|
-
- HY-B0800
-
|
Guanethidine sulfate
Guanethidine monosulfate
|
Others
|
Neurological Disease
|
|
Guanethidine sulfate (Guanethidine monosulfate) ia an antihypertensive agents. Guanethidine is also an adrenergic neurone blocking drug, enters noradrenergic nerve terminals by the neuronal amine carrier.
|
-
- HY-P1365A
-
|
α-Conotoxin MII TFA
α-CTxMII TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-129767
-
|
CMLD012612
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity.
|
-
- HY-100468
-
|
REV7/REV3L-IN-1
|
Others
|
Cancer
|
|
REV7/REV3L-IN-1 is a REV7/REV3L interaction inhibitor with an IC50 of 78 μM, which directly binds to REV7 in nuclear magnetic resonance analyses, and inhibits the reactivation of a reporter plasmid containing an interstrand crosslink (ICL) in between the promoter and reporter regions.
|
-
- HY-N2558
-
|
Murrayone
|
Others
|
Cancer
|
|
Murrayone, a coumarin-containing compound extracted from M. paniculata, is the most bioactive substance in this species and is a cancer metastasis chemopreventive agent based on its unique pharmacological properties.
|
-
- HY-133646
-
|
Bromochloroacetonitrile
|
DNA/RNA Synthesis
|
Others
|
|
Bromochloroacetonitrile is a by-product of the chlorine disinfection of water containing natural organic material. Bromochloroacetonitrile possesses direct acting mutagenic activity and is capable of inducing DNA strand breakage.
|
-
- HY-126457
-
|
Thalidomide-propargyl
|
Ligand for E3 Ligase
|
Cancer
|
|
Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs.
|
-
- HY-16579A
-
|
Etifoxine
HOE 36-801
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors.
|
-
- HY-126669
-
|
Mal-PEG4-VA
|
ADC Linker
|
Cancer
|
|
Mal-PEG4-VA is a noncleavable ADC linker containing a Maleimide group. Mal-PEG4-VA is used for making antibody-drug conjugate.
|
-
- HY-D0227
-
|
Trometamol
TromethAmine
|
Others
|
Metabolic Disease
|
|
Trometamol is a biologically inert amino alcohol of low toxicity, which buffers carbon dioxide and acids in vitro and in vivo. Trometamol is an effective amine compound for pH control in the physiological range.
|
-
- HY-B1132S
-
-
- HY-13491
-
|
GNF-5837
|
Trk Receptor
|
Cancer
|
|
GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
|
-
- HY-W009749B
-
|
D,L-Cystathionine dihydrochloride
|
Others
|
Others
|
|
D,L-Cystathionine dihydrochloride is an intermediate in the synthesis of cysteine that is produced from homocysteine and serine by the action of cystathionine-β-synthase (CBS). DL-Cystathionine contains a carbon-sulfide bond of cystathionine (βC-S) linkage.
|
-
- HY-B1449
-
|
Uridine
β-Uridine
|
Endogenous Metabolite
|
Others
|
|
Uridine (β-Uridine) is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond.
|
-
- HY-B0816
-
|
Etofenprox
|
Others
|
Others
|
|
Etofenprox is a non-ester pyrethroid insecticide. Etofenprox induces toxicity in the housefly M. domestica (LD50 = 23 ng/fly). Formulations containing Etofenprox have been used in the control of agricultural pests.
|
-
- HY-P1082
-
-
- HY-D0227A
-
|
Trometamol hydrochloride
TromethAmine hydrochloride
|
Others
|
Metabolic Disease
|
|
Trometamol hydrochloride (Tromethamine hydrochloride) is a biologically inert amino alcohol of low toxicity, which buffers carbon dioxide and acids in vitro and in vivo. Trometamol hydrochloride is an effective amine compound for pH control in the physiological range.
|
-
- HY-129938
-
-
- HY-P2031
-
|
Phallacidin
|
Others
|
|
|
Phallacidin is a natural mycotoxin first isolated from the death cap mushroom, A. phalloides. Phallacidin binds filamentous actin (F-actin) like phalloidin (Item No. 18039), but contains a carboxyl group for coupling reactions.
|
-
- HY-135306
-
-
- HY-105272A
-
-
- HY-130708
-
|
UNC6852
|
Histone Methyltransferase
PROTAC
|
Cancer
|
|
UNC6852 is a selective rolycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a VHL ligand, with an IC50 of 247 nM for EED.
|
-
- HY-N6705
-
|
Tropodithietic acid
|
Bacterial
|
Infection
|
|
Tropodithietic acid is a sulfur-containing antibiotic produced by the marine bacterium Phaeobacter inhibens. Tropodithietic acid exhibits a strong antibiotic activity against a broad spectrum of bacteria including alpha- and gammaproteobacteria, flavobacteria and actinobacteria.
|
-
- HY-129526
-
|
Mal-PEG3-NHS ester
|
ADC Linker
|
Cancer
|
|
Mal-PEG3-NHS ester is a noncleavable ADC linker containing a Maleimide group. Mal-PEG3-NHS ester is used for making antibody-drug conjugate.
|
-
- HY-105272
-
|
Loreclezole
R 72063
|
GABA Receptor
|
Neurological Disease
|
|
Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
|
-
- HY-19773
-
|
beta-lactamase-IN-1
|
Bacterial
|
Cancer
|
|
beta-lactamase-IN-1 targets Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.
|
-
- HY-140247
-
-
- HY-B1599
-
|
Chloramphenicol palmitate
|
Bacterial
|
Infection
|
|
Chloramphenicol palmitate is an orally active broad spectrum antibiotic and has a broad spectrum of activity against gram positive and gram negative bacteria. Chloramphenicol palmitate inhibits bacterial protein synthesis by blocking the peptidyl transferase step. Chloramphenicol palmitate can be used as bacterial selection agent in transformed cells containing chloramphenicol resistance genes.
|
-
- HY-107846
-
|
Xylan
|
Others
|
Others
|
|
Xylan represents the main hemicellulose component in the secondary plant cell walls of flowering plants. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose.
|
-
- HY-130993
-
|
Isatropolone A
|
Parasite
|
Infection
|
|
Isatropolone A, a natural product containing a 1,5-diketone moiety, is reisolated from Streptomyces Gö66. Isatropolone A shows potent activity against Leishmania donovani with an IC50 of 0.5 μM.
|
-
- HY-124418
-
|
SBI-477
|
Others
|
Metabolic Disease
|
|
SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
|
-
- HY-111753A
-
|
WDR5-IN-4 TFA
|
Histone Methyltransferase
|
Cancer
|
|
WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
|
-
- HY-N6712
-
|
Thiolutin
Acetopyrrothin
|
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
|
Thiolutin (Acetopyrrothin) is a disulfide-containing antibiotic and anti-angiogenic compound produced by Streptomyces. Thiolutin inhibits the JAMM metalloproteases Csn5, Associated-molecule-with-the-SH3-Domain-of-STAM (AMSH) and Brcc36. Thiolutin is a potent and selective inhibitor of endothelial cell adhesion accompanied by rapid induction of Heat-shock protein beta-1 (Hsp27) phosphorylation.
|
-
- HY-13821
-
|
Epoxomicin
BU-4061T
|
Proteasome
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
|
-
- HY-D1070
-
|
DBCO-PEG4-TAMRA
|
Others
|
Others
|
|
DBCO-PEG4-TAMRA is a PEG-based TARMA dye and contains a DBCO group, which enables Click Chemistry. The TAMRA dye is a dye widely used in oligonucleotide labeling and automated DNA sequencing applications.
|
-
- HY-103463
-
|
SA57
|
FAAH
MAGL
|
Neurological Disease
|
|
SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases.
|
-
- HY-14648
-
-
- HY-109124A
-
|
Taniborbactam hydrochloride
VNRX-5133 hydrochloride
|
Bacterial
|
Infection
|
|
Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam hydrochloride has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria.
|
-
- HY-I0501
-
|
2'-Aminoacetophenone
|
Others
|
Inflammation/Immunology
|
|
2'-Aminoacetophenone is an aromatic compound containing a ketone substituted by one alkyl group, and a phenyl group. 2'-Aminoacetophenone can be used as a breath biomarker for the detection of Ps. Aeruginosa infections in the cystic fibrosis lung.
|
-
- HY-126671
-
-
- HY-N0325
-
|
DL-Methionine
|
Parasite
|
Infection
Inflammation/Immunology
|
|
DL-Methionine is an essential amino acid containing sulfur with oxidative stress defense effects. DL-Methionine can be used for animal natural feed. DL-Methionine also kills H. rostochiensis on potato plants.
|
-
- HY-118716
-
|
PhIP
|
Others
|
Cancer
|
|
PhIP is the most abundant of generation of heterocyclic amines (HCA), resulted in the cooking of meat. DNA damaging and mutagenic activities. PhIP also has oestrogenic activity that could contribute to its tissue specific carcinogenicity.
|
-
- HY-79369
-
|
Succinic anhydride
|
ADC Linker
|
Cancer
|
|
Succinic anhydride is a cyclic anhydride and a nonclaevable ADC linker extracted from patent WO2009064913A1. Succinic anhydride can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide.
|
-
- HY-15989A
-
|
SM-164 Hydrochloride
|
IAP
|
Cancer
|
|
SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
|
-
- HY-126668
-
|
Mal-PEG4-VC-PAB-DMEA
|
ADC Linker
|
Cancer
|
|
Mal-PEG4-VC-PAB-DMEA is a cleavable ADC linker containing a Maleimide group. Mal-PEG4-VC-PAB-DMEA is used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-126672
-
|
Mal-PEG4-Val-Cit-PAB
|
ADC Linker
|
Cancer
|
|
Mal-PEG4-Val-Cit-PAB is a cleavable ADC linker containing a Maleimide group. Mal-PEG4-Val-Cit-PAB is used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-15989
-
|
SM-164
|
IAP
|
Cancer
|
|
SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
|
-
- HY-117570
-
|
KSC-34
|
Others
|
Neurological Disease
|
|
KSC-34 is a potent and site-selective inhibitor of PDIA1 (containing two active-site domains a and a′). KSC-34 displays a 30-fold selectivity for a domain over a′ domain and time-dependent inhibition of PDIA1 reductase activity. KSC-34 displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family.
|
-
- HY-122198
-
|
ML367
|
Others
|
Cancer
|
|
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
|
-
- HY-126674
-
-
- HY-112496
-
|
Cl-C6-PEG4-O-CH2COOH
PROTAC Linker 4
|
PROTAC Linker
|
Cancer
|
|
Cl-C6-PEG4-O-CH2COOH (PROTAC Linker 4) is a PEG-based PROTAC linker can be used in the synthesis of chloroalkane-containing PROTACs (HaloPROTACs).
|
-
- HY-126673
-
|
Mal-C2-Gly3-EDA
|
ADC Linker
|
Cancer
|
|
Mal-C2-Gly3-EDA is a cleavable ADC linker containing a Maleimide group. Mal-C2-Gly3-EDA is used for making antibody-drug conjugate.
|
-
- HY-125837A
-
|
MS31 trihydrochloride
|
Epigenetic Reader Domain
|
Cancer
|
|
MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells.
|
-
- HY-P0178A
-
|
LXW7 TFA
|
Integrin
|
Inflammation/Immunology
|
|
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
|
-
- HY-100216
-
|
SPDP
SPDP Crosslinker
|
ADC Linker
|
Cancer
|
|
SPDP (SPDP Crosslinker) is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls. It is a glutathione cleavable ADC linker used for the antibody-drug conjugates (ADCs).
|
-
- HY-N6840
-
|
Xylotetraose
|
Others
|
Others
|
|
Xylotetraose is a hydrolysis product of Xylan. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose. Xylotetraose can be used for enzyme biochemical analysis.
|
-
- HY-12881
-
|
Eliprodil
SL-820715
|
iGluR
|
Neurological Disease
|
|
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
|
-
- HY-107604
-
|
UBP 302
|
iGluR
|
Neurological Disease
|
|
UBP 302 is a potent and selective GLUK5-subunit containing kainate receptor antagonist (apparent Kd=402 nM), and displays very little affinity on GluK2 (GluR6) kainate receptors. Anxiolytic effects.
|
-
- HY-120435
-
|
Tyrothricin
|
Bacterial
Fungal
Influenza Virus
|
Infection
|
|
Tyrothricin is a polypeptide antibiotic mixture isolated from Bacillus brevis and consists of tyrocidines and gramicidins. Tyrothricin shows activity against bacteria, fungi and some viruses. Tyrothricin containing formulations are used in sore throat agents and in agents for the healing of infected superficial and small-area wounds.
|
-
- HY-B0840
-
|
Chlorfenapyr
|
Others
|
Others
|
|
Chlorfenapyr is a pyrrole pro-insecticide that is metabolized in vivo into CL 303268 by mixed function oxidases. Chlorfenapyr is active against a variety of insects including those susceptible and resistant to pyrethroid and organophosphate insecticides. Formulations containing Chlorfenapyr have been used to control termites and in agriculture to control various insects.
|
-
- HY-130835
-
|
FKBP12 PROTAC RC32
RC32
|
PROTAC
FKBP
|
Cancer
|
|
FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an E3 ubiquitin ligase (Pomalidomide; HY-10984).
|
-
- HY-113679
-
|
Ceramides Mixture
|
Telomerase
|
Endocrinology
Metabolic Disease
|
|
Ceramides Mixture is an endogenous ceramide and consists of hydroxy and non-hydroxy fatty acid-containing ceramides. Ceramides Mixture is a main lipid component of the permeability barrier in epidermis. Ceramides Mixture is involved in the regulation of growth inhibition, cell cycle arrest, and modulation of telomerase activity.
|
-
- HY-128945
-
|
CL2A
|
ADC Linker
|
Cancer
Inflammation/Immunology
|
|
CL2A is a claevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker.
|
-
- HY-N7032
-
-
- HY-N6742
-
|
Borrelidin
Treponemycin
|
CDK
Parasite
Apoptosis
Antibiotic
|
Infection
|
|
Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin (Treponemycin) is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM. Borrelidin (Treponemycin) is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM, and induces apoptosis of the tube-forming cells. Borrelidin (Treponemycin) has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum.
|
-
- HY-135581
-
|
Raloxifene 6-glucuronide
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal 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-112610
-
|
CF53
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
|
-
- 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-117541
-
|
Glycyl-glutamine
Glycyl-L-glutAmine
|
Others
|
Neurological Disease
|
|
Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems. Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln).
|
-
- HY-P1268
-
|
α-Conotoxin PIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-P1268A
-
|
α-Conotoxin PIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-118870
-
-
- HY-N6711
-
|
Equisetin
|
HIV Integrase
|
Infection
|
|
Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537. Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity. Equisetin inhibits the growth of Gram-positive bacteria and HIV-1 integrase activity but shows no activity against Gram-negative bacteria. Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections.
|
-
- HY-130695
-
-
- HY-B0836
-
|
λ-Cyhalothrin
|
Parasite
Sodium Channel
|
Infection
Endocrinology
Neurological Disease
|
|
λ-Cyhalothrin is a high efficiency, broad-spectrum type II synthetic pyrethroid insecticide containing α-cyano group. λ-Cyhalothrin is used to control a wide range of pests in a variety of applications. λ-Cyhalothrin is a neurotoxin that targets sodium channels in the membranes of neurons in the central nervous system.
|
-
- HY-14264
-
|
Cyamemazine
|
5-HT Receptor
|
Neurological Disease
|
|
Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.
|
-
- HY-N7384
-
-
- HY-69220
-
|
7-Octynoic acid
|
PROTAC Linker
|
Cancer
|
|
7-Octynoic acid (compound 42) is a PROTAC linker and can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-110199
-
|
TC-I 2014
|
TRP Channel
|
Neurological Disease
|
|
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.
|
-
- HY-108588
-
|
NS5806
|
Potassium Channel
|
Cardiovascular Disease
|
|
NS5806, a potent potassium current activator, increases KV4.3/KChIP2 peak current amplitudes with an EC50 of 5.3 μM. NS5806 slows KV4.3 and KV4.2 current dacay in channel complexes containing KChIP2.
|
-
- HY-101884
-
|
Biocytin
(+)-Biocytin
|
Endogenous Metabolite
|
Others
|
|
Biocytin is a conjugate of D-biotin and L-lysine, where the carboxylate of D-biotin is coupled with the ϵ-amine of L-lysine via a secondary amide bond. Biocytin is a classical neuroanatomical tracer commonly used to map brain connectivity. Biocytin is used as a versatile marker in anterograde, retrograde and intracellular neuroanatomical investigations and in biotinidase assays.
|
-
- HY-P0175
-
|
740 Y-P
740YPDGFR; PDGFR 740Y-P
|
PI3K
Autophagy
|
Cancer
|
|
740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
|
-
- HY-130809
-
|
DBCO-PEG4-Biotin
|
Others
|
Cancer
|
|
DBCO-PEG4-Biotin is an azadibenzocyclooctyne-biotin derivative containing a biotin group and 4 PEGs. DBCO-PEG4-Biotin is a versatile biotinylation reagent used for the introduction of a biotin moiety to azide-labeled biomolecules via copper-free strain-promoted alkyne-azide click chemistry (SPAAC) reaction.
|
-
- 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-126493
-
|
DM4-SPDP
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
|
DM4-SPDP is a drug-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody drug conjugate. SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls.
|
-
- HY-16023B
-
|
(Rac)-Acolbifene
EM-343; (Rac)-EM-652
|
Estrogen Receptor/ERR
|
Cancer
|
|
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380.
|
-
- HY-13993
-
|
Ro 25-6981
|
iGluR
|
Neurological Disease
|
|
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.
|
-
- HY-N0175
-
|
Cytisinicline
Cytisine; Sophorine; Baptitoxine
|
nAChR
|
Metabolic Disease
|
|
Cytisinicline (Cytisine) is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.
|
-
- HY-117147A
-
|
GSK2945 hydrochloride
|
Cytochrome P450
|
Metabolic Disease
|
|
GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
|
-
- HY-117147
-
|
GSK2945
|
Cytochrome P450
|
Metabolic Disease
|
|
GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
|
-
- HY-107676
-
|
SIB-1553A
|
nAChR
|
Neurological Disease
|
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
|
-
- HY-N6743
-
|
Cercosporin
|
PKC
|
Cancer
|
|
Cercosporin is produced by a plant pathogen, Cercosporakikuchii, and the elsinochromes, pigments of the elsinoe family of fungi. Cercosporin is a potent photosensitizer with a short activation wavelength, mostly suitable for superficial photodynamic therapy (PDT) treatments, especially when it is necessary to avoid perforations.
Cercosporin contains the perylenequinone structural features necessary to PKC activity with an IC50 of 0.6-1.3 μM.
|
-
- HY-116084
-
-
- HY-A0072S
-
|
Zilpaterol-d7
|
Adrenergic Receptor
|
|
|
Zilpaterol-d7 is a deuterium labeled Zilpaterol. Zilpaterol is a β-adrenergic receptor agonist that putatively, through activation of protein kinase A, increases protein synthesis in skeletal muscle fibers as well as reduces lipogenesis and increases lipolysis in adipose tissues. Formulations containing Zilpaterol have been used to increase lean body weight and improve feed efficiency in commercial beef cattle.
|
-
- HY-P1839
-
|
Angiotensin I/II (1-5)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-5 is a peptide that contains the amino acids 1-5, which is converted from Angiotensin I/II. Angiotensin I is formed by the action of renin on angiotensinogen. Angiotensin II is produced from angiotensin I. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-W001189
-
|
1,3-Dithiane
|
Bacterial
Endogenous Metabolite
|
Infection
|
|
1,3-Dithiane is a protected formaldehyde anion equivalent that could serve as a useful labeled synthon. 1,3-Dithiane is also a sulfur-containing Maillard reaction products (MRPs) found in boiled beef extracts. 1,3-Dithiane shows a potent direct-acting mutagenicity toward S. typhimurium TA98 and TA100.
|
-
- HY-P1829
-
|
Angiotensin I/II (1-6)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-6 contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. Angiotensin I is formed by the action of renin on angiotensinogen. Angiotensin II is produced from angiotensin I. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-B0425A
-
|
Novobiocin Sodium
Albamycin; Cathomycin
|
Bacterial
Autophagy
Antibiotic
|
Infection
Cancer
|
|
Novobiocin Sodium (Albamycin; Cathomycin) is an orally active antibiotic compound derived from Streptomyces niveus and a potent DNA gyrase inhibitor by binding the ATP-binding site in the ATPase subunit. Novobiocin Sodium manifests strong anti-bacterial activities effectively against gram-positive pathogens and shows limited activity against gram-negative organisms due to LPS-containing outer membrane.Novobiocin Sodium binds to the C-terminus of Hsp90 and slightly induces degradation of Hsp90-dependent client proteins (IC50=700 µM).
|
-
- HY-135593
-
|
LY88074 analog 1
|
Others
|
Endocrinology
|
|
LY88074 analog 1 is a benzothiophene compound with nitrogen-containing non-basic side chains, Compound 26, extracted from patent EP0747380A1. LY88074 analog 1 is an agent for alleviating the symptoms of post-menopausal symptoms, such as osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer. LY88074 analog 1 can be used alone or in combination with estrogen or progestin.
|
-
- HY-129774
-
|
Phthalimide-PEG4-MPDM-OH
|
PROTAC Linker
|
Cancer
|
|
Phthalimide-PEG4-MPDM-OH is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-MPDM-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-130715
-
|
tert-Butyl 11-aminoundecanoate
|
PROTAC Linker
|
Cancer
|
|
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-129773
-
|
Phthalimide-PEG4-PDM-OTBS
|
PROTAC Linker
|
Cancer
|
|
Phthalimide-PEG4-PDM-OTBS is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-PDM-OTBS can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-128946
-
|
CL2A-SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
Inflammation/Immunology
|
|
CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
|
-
- HY-P1854
-
|
β-Amyloid (1-9)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism .
|
-
- HY-126975
-
-
- HY-123023
-
|
12(S)-HETE D8
|
Others
|
|
|
12(S)-HETE D8 contains eight deuterium atoms at the 5, 6, 8, 9, 11, 12, 14 and 15 positions. It is intended for use as an internal standard for the quantification of 12(S)-HETE by GC- or LC-mass spectrometry (MS). 12(S)-HETE D8 is the predominant lipoxygenase product of mammalian platelets. It enhances tumor cell adhesion to endothelial cells, fibronectin, and the subendothelial matrix at 0.1 µM.
|
-
- HY-130871
-
-
- HY-130872
-
-
- HY-130873
-
-
- 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-129772
-
|
Phthalimide-PEG3-C2-OTs
|
PROTAC Linker
|
Cancer
|
|
Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-40178
-
|
NH2-C4-NH-Boc
|
PROTAC Linker
|
Cancer
|
|
NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-P1695
-
|
Cinnamycin
Ro 09-0198
|
Bacterial
Antibiotic
|
|
|
Cinnamycin is tetracyclic lantibiotic produced from S. cinnamoneus that contains four unusual amino acids: erythro-β-hydroxyaspartic acid, mesolanthionine, threo-β-methyllanthionine, and lysinoalanine.1 Cinnamycin has demonstrated antiviral activity against herpes simplex virus type 1 KOS strain infection in Vero cells via a cytopathic effect reduction assay. Cinnamycin recognizes the structure of phosphatidylethanolamine and forms an equimolar complex with the phospholipid on biological membranes. This peptide has been used as a probe for analyzing the transbilayer movement of phosphatidylethanolamine.
|
-
- 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-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-100991
-
|
FG 7142
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
|
-
- HY-122815
-
|
Fusicoccin
Fusicoccin A
|
Apoptosis
|
Cancer
|
|
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
|
-
- HY-130618
-
|
Boc-C1-PEG3-C4-OH
|
PROTAC Linker
|
Cancer
|
|
Boc-C1-PEG3-C4-OH is a PROTAC linker, which refers to the Alkyl/ether composition. Boc-C1-PEG3-C4-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- 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-130619
-
|
Boc-C1-PEG3-C4-OBn
|
PROTAC Linker
|
Cancer
|
|
Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- 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-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-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-N0565
-
-
- 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-N0565A
-
-
- 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-W008923
-
-
- 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-16657
-
-
- 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-N2117
-
|
Isoginkgetin
|
MMP
|
Cancer
|
|
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
|
-
- 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-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-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-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-114418
-
-
- 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-10009
-
-
- 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.
|
-
- HY-N6619
-
-
- HY-109877
-
-
- HY-100299
-
-
- HY-P2470
-
-
- HY-B0106
-
-
- 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-137239
-
-
- HY-100303A
-
|
FR194738
|
Others
|
Metabolic Disease
|
|
FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
|
-
- HY-50946
-
-
- HY-15886
-
-
- HY-112131
-
-
- HY-19326
-
-
- HY-12971
-
|
Nampt-IN-1
LSN3154567
|
Nampt
|
Cancer
|
|
Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
|
-
- HY-101479
-
|
Iclaprim
AR-100
|
Bacterial
|
Infection
|
|
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.
|
-
- HY-108900A
-
-
- HY-N5118
-
|
Chimonanthine
(-)-Chimonanthine
|
Tyrosinase
|
Cancer
|
|
Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.
|
-
- HY-U00049
-
-
- HY-16904
-
|
RI-2
|
RAD51
|
Cancer
|
|
RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
|
-
- HY-130760
-
-
- HY-103036
-
-
- HY-111410
-
-
- HY-13229
-
|
BOC-D-FMK
|
Caspase
|
Cancer
|
|
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.
|
-
- HY-10862
-
|
FAAH inhibitor 1
Benzothiazole analog 3
|
FAAH
Autophagy
|
Cancer
|
|
FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM.
|
-
- HY-13256A
-
|
Desmethyl Erlotinib
OSI-420 free base; CP-373420
|
Drug Metabolite
|
Cancer
|
|
Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.
|
-
- HY-15735
-
|
c-Met inhibitor 1
|
c-Met/HGFR
|
Cancer
|
|
c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.
|
-
- HY-10997S
-
|
Ibrutinib D5
PCI-32765 D5
|
Btk
|
Cancer
|
|
Ibrutinib D5 (PCI-32765 D5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
|
-
- 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-B0008
-
-
- HY-115502A
-
|
BCI hydrochloride
(E)-BCI hydrochloride
|
Phosphatase
|
Cancer
Inflammation/Immunology
|
|
BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.
|
-
- HY-12031
-
-
- HY-136538
-
|
LQZ-7I
|
Survivin
|
Cancer
|
|
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
|
-
- HY-19727
-
-
- HY-N2006
-
|
Ganoderic acid B
|
HIV Protease
|
Infection
|
|
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.
|
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-114169
-
|
WRG-28
|
Discoidin Domain Receptor
|
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
|
-
- HY-16592
-
|
Brefeldin A
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
|
Cancer
Infection
|
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-101664
-
|
Ilaprazole
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-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-135396
-
|
(1S,2S)-Bortezomib
|
Proteasome
|
Cancer
|
|
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
|
-
- HY-P1290A
-
|
PKA Inhibitor Fragment (6-22) amide TFA
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-B0166
-
-
- HY-P0222
-
|
PKI(5-24)
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-114996
-
-
- HY-103032
-
|
Multi-kinase inhibitor 1
|
PDGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
|
-
- HY-Y0445A
-
|
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-66005
-
-
- HY-13512
-
|
Camostat mesylate
Camostat mesilate; FOY305; FOY-S980
|
Ser/Thr Protease
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
|
-
- HY-122632
-
|
Ciliobrevin D
|
Hedgehog
|
Cancer
|
|
Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.
|
-
- HY-16594
-
|
Lactacystin
|
Proteasome
|
Neurological Disease
|
|
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC50 of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.
|
-
- HY-B0166A
-
|
L-Ascorbic acid sodium salt
Sodium L-ascorbate; Vitamin C sodium salt
|
Calcium Channel
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.
|
-
- HY-135391
-
-
- HY-50909
-
|
Perifosine
KRX-0401; NSC 639966; D21266
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
|
-
- HY-101766
-
-
- HY-16510A
-
-
- HY-N0143
-
|
Phlorizin
Floridzin; NSC 2833
|
SGLT
Na+/K+ ATPase
|
Metabolic Disease
|
|
Phlorizin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na +/K +-ATPase inhibitor.
|
-
- HY-U00096
-
-
- HY-B1243
-
-
- HY-32351
-
-
- HY-13012
-
|
RepSox
E-616452; SJN 2511
|
TGF-β Receptor
|
Cancer
|
|
RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
|
-
- HY-N7089
-
|
Benzoyleneurea
|
Bacterial
|
Infection
|
|
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.
|
-
- HY-18931A
-
|
NSC305787 hydrochloride
|
Others
|
Cancer
|
|
NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
|
-
- HY-15247
-
-
- HY-16510
-
-
- HY-12357
-
-
- HY-101464
-
|
ML329
|
Others
|
Others
|
|
ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC50 of 1.2 μM.
|
-
- HY-12682
-
|
Glutaminase C-IN-1
Compound 968
|
Glutaminase
|
Cancer
|
|
Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
|
-
- HY-102007A
-
|
Gamitrinib TPP hexafluorophosphate
|
HSP
|
Cancer
|
|
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-100541
-
|
INH6
|
Apoptosis
|
Cancer
|
|
INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.
|
-
- HY-32351A
-
-
- HY-100735
-
-
- HY-13067
-
-
- HY-15679
-
-
- HY-19352
-
-
- HY-107433
-
-
- HY-126134
-
-
- HY-18931
-
|
NSC305787
|
Others
|
Cancer
|
|
NSC305787 is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
|
-
- HY-15223
-
-
- HY-15457
-
-
- HY-100792
-
|
URB602
|
Others
|
Cancer
|
|
URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC50 of 28±4 μM through a noncompetitive mechanism.
|
-
- HY-112164
-
-
- HY-N7452
-
-
- HY-N0149
-
-
- HY-100263
-
-
- HY-N0342
-
-
- HY-101244
-
-
- HY-100384
-
-
- HY-112870A
-
-
- HY-P0290A
-
-
- HY-19763
-
|
BEBT-908
PI3Kα inhibitor 1
|
PI3K
|
Cancer
|
|
BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
|
-
- HY-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis.
|
-
- HY-23460A
-
|
4-Ethynyl-L-phenylalanine hydrochloride
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
4-Ethynyl-L-phenylalanine hydrochloride is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine hydrochloride is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine hydrochloride selectively and reversibly inhibits the biosynthesis of serotonin.
|
-
- 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-23460
-
|
4-Ethynyl-L-phenylalanine
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
4-Ethynyl-L-phenylalanine is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine is a competitive inhibitor with regard to the substrate tryptophan, with a Ki of 32.6 μM. 4-Ethynyl-L-phenylalanine selectively and reversibly inhibits the biosynthesis of serotonin.
|
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
|
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-133114
-
-
- HY-W006230
-
|
Anthraflavic acid
|
Others
|
Cancer
|
|
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
|
-
- HY-118532
-
|
Tyrphostin AG30
AG30
|
EGFR
|
Cancer
|
|
Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
|
-
- HY-N0112
-
|
Dihydromyricetin
Ampelopsin; Ampeloptin
|
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Cancer
Infection
|
|
Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 nM.
|
-
- HY-11001
-
|
PHA-793887
|
CDK
Apoptosis
|
Cancer
|
|
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
|
-
- HY-100222
-
|
CZ415
|
mTOR
|
Cancer
|
|
CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.
|
-
- HY-119692
-
|
Curvulin
|
Microtubule/Tubulin
|
Others
|
|
Curvulin, isolated from Curvularia lunata, is a phytotoxin. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.
|
-
- HY-12056
-
|
BIX02189
|
MEK
ERK
|
Cancer
|
|
BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
|
-
- HY-12957
-
-
- HY-10367A
-
|
Canertinib dihydrochloride
CI-1033 dihydrochloride; PD-183805 dihydrochloride
|
EGFR
|
Cancer
|
|
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
|
-
- HY-135383
-
-
- HY-12204
-
|
PFK-015
|
Autophagy
|
Cancer
|
|
PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.
|
-
- HY-100750
-
-
- 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-N3002
-
|
α-Arbutin
4-Hydroxyphenyl α-D-glucopyranoside
|
Tyrosinase
|
Metabolic Disease
|
|
α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.
|
-
- HY-111357
-
|
Antifungal agent 2
|
Fungal
|
Infection
|
|
Antifungal agent 2 is a broad-spectrum fungal inhibitor which inhibits growth of pertinent species of Candida, Cryptococcus, and Aspergillus at a concentration as low as 0.5 μg/mL.
|
-
- HY-13966
-
|
2-Deoxy-D-glucose
2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose
|
Hexokinase
HSV
Apoptosis
|
Cancer
|
|
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase.
|
-
- HY-12589
-
-
- HY-126482
-
|
Telomerase-IN-2
|
Telomerase
|
Cancer
|
|
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity.
|
-
- HY-15162A
-
-
- HY-15417
-
|
ML-7 hydrochloride
|
Myosin
YAP
|
Cancer
|
|
ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.
|
-
- HY-12622
-
|
HSP70-IN-1
|
HSP
|
Cancer
|
|
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
|
-
- HY-112861A
-
-
- HY-12444
-
|
Y15
FAK Inhibitor 14
|
FAK
|
Cancer
|
|
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
|
-
- HY-100852
-
-
- HY-12289A
-
|
Defactinib hydrochloride
VS-6063 hydrochloride; PF 04554878 hydrochloride
|
FAK
|
Cancer
|
|
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.
|
-
- HY-W018931
-
-
- HY-12589A
-
-
- HY-115666
-
|
COH34 analog 1
|
Others
|
Cancer
|
|
COH34 analog 1, a metabolite, is an oxidized analog of COH34. COH34 is a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
|
-
- HY-13806
-
|
XL388
|
mTOR
Autophagy
|
Cancer
|
|
XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.
|
-
- HY-12744
-
-
- HY-10129
-
|
Veliparib
ABT-888
|
PARP
Autophagy
|
Cancer
|
|
Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
|
-
- HY-11108
-
-
- HY-111651
-
-
- HY-N5015
-
|
Rosmanol
|
Others
|
Inflammation/Immunology
Cancer
|
|
Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.
|
-
- HY-133246
-
-
- HY-10366
-
-
- HY-112445
-
-
- HY-12479A
-
|
Epetraborole hydrochloride
GSK2251052 hydrochloride
|
Bacterial
|
Infection
|
|
Epetraborole hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding "to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase".
|
-
- HY-19832
-
|
SC66
|
Akt
Apoptosis
|
Cancer
|
|
SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
- HY-136110
-
-
- HY-115584
-
|
Lufenuron
|
Parasite
|
Infection
|
|
Lufenuron is a lipophilic benzoylurea insecticide and a chitin synthesis inhibitor that can used for flea and fish lice control. Lufenuron inhibits moulting of arthropods.
|
-
- HY-N2182
-
-
- HY-100303
-
-
- HY-135328
-
-
- HY-B1479C
-
-
- HY-112136
-
|
TAO Kinase inhibitor 1
|
Others
|
Cancer
|
|
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.
|
-
- HY-P0222A
-
|
PKI(5-24) TFA
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-B1479
-
-
- HY-15480
-
|
NSC 42834
JAK2 Inhibitor V; Z3
|
JAK
|
Cancer
|
|
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
|
-
- HY-B1479B
-
-
- HY-100126
-
|
Tubercidin
7-Deazaadenosine
|
Bacterial
DNA/RNA Synthesis
Influenza Virus
Antibiotic
|
Infection
|
|
Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC50 of 0.02 μM. Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis. Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP. Tubercidin has antiviral activity.
|
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-15463
-
|
Imatinib
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-110100
-
|
CPYPP
|
Others
|
Inflammation/Immunology
|
|
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.
|
-
- HY-112701
-
|
CCR6 inhibitor 1
|
CCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
|
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer.
|
-
- HY-B0968
-
|
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-B0879A
-
|
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-B0879
-
-
- HY-100434
-
|
PD-161570
|
FGFR
PDGFR
EGFR
Src
TGF-β Receptor
|
Cancer
Cardiovascular Disease
|
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
|
-
- HY-12041
-
|
SP600125
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates apoptosis.
|
-
- HY-N2360
-
|
Hinokiflavone
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
|
-
- HY-122727
-
|
STL127705
|
DNA-PK
|
Cancer
|
|
STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
|
-
- HY-113957
-
|
MPI_5a
|
HDAC
|
Cancer
|
|
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
|
-
- HY-N2150
-
|
Psammaplin A
|
HDAC
DNA Methyltransferase
DNA/RNA Synthesis
Bacterial
|
Cancer
Infection
|
|
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
|
-
- HY-18707
-
-
- HY-101938
-
-
- HY-15769A
-
-
- HY-19762
-
-
- HY-16511
-
|
Upamostat
WX-671
|
Ser/Thr Protease
PAI-1
|
Cancer
|
|
Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
|
-
- HY-14754
-
|
Salirasib
S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
|
Ras
Autophagy
|
Cancer
|
|
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
|
-
- HY-101873
-
-
- HY-70035
-
|
Otamixaban
FXV673
|
Factor Xa
|
Cardiovascular Disease
|
|
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
|
-
- 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-100737
-
|
ML349
|
Phospholipase
|
Cancer
|
|
ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
|
-
- HY-50714
-
|
Quiflapon sodium
MK-591 sodium
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
|
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
|
-
- HY-103334
-
-
- HY-18729A
-
|
L-NAME hydrochloride
NG-Nitroarginine methyl ester hydrochloride
|
NO Synthase
|
Cancer
|
|
L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM.
|
-
- HY-B0069
-
-
- HY-16214
-
|
FX-11
LDHA Inhibitor FX11
|
Lactate Dehydrogenase
|
Cancer
|
|
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell，a Ki value of 8 μM.
|
-
- HY-12055
-
|
BIX02188
|
MEK
ERK
|
Cancer
|
|
BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
|
-
- HY-100891
-
-
- HY-15248
-
|
GDC-0349
|
mTOR
Autophagy
|
Cancer
|
|
GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a Ki of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.
|
-
- HY-13327
-
|
Evacetrapib
LY2484595
|
CETP
|
Cardiovascular Disease
|
|
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
|
-
- HY-19331
-
|
WZB117
|
GLUT
|
Cancer
|
|
WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
|
-
- HY-N3266
-
|
Methyl rosmarinate
|
Tyrosinase
|
Cancer
|
|
Methyl rosmarinate is a noncompetitive tyrosinase inhibitor which is isolated from Rabdosia serra, with an IC50 of 0.28 mM for mushroom tyrosinase, and also inhibits a-glucosidase.
|
-
- HY-100965
-
-
- HY-33900
-
|
Dihydrofuran-3(2H)-one
3-Oxotetrahydrofuran
|
Others
|
Others
|
|
Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) is used for synthesizing cyclic ketone inhibitors that inhibits the serine protease plasmin.
|
-
- HY-15769
-
|
WHI-P180
Janex 3
|
VEGFR
EGFR
|
Cancer
|
|
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
|
-
- HY-100562
-
-
- HY-15338
-
|
TG003
|
CDK
|
Cancer
|
|
TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
|
-
- HY-111621
-
|
DC661
|
Autophagy
Apoptosis
|
Cancer
|
|
DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity.
|
-
- HY-12964
-
|
SGI-7079
|
TAM Receptor
|
Cancer
|
|
SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.
|
-
- HY-10165
-
|
PSI-6130
R 1656
|
HCV
|
Infection
|
|
PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM.
|
-
- HY-P1044
-
|
Spinorphin
LVV-hemorphin-4
|
Others
|
Neurological Disease
|
|
Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect.
|
-
- HY-135570
-
-
- HY-101587
-
-
- HY-101872
-
-
- HY-10005
-
|
Flavopiridol
HMR-1275; Alvocidib; L86-8275
|
CDK
Autophagy
HIV
|
Cancer
|
|
Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
|
-
- HY-111381
-
|
BI-3812
|
Bcl-2 Family
|
Cancer
|
|
BI-3812 is potent and efficacious BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM; BI-3812 has antitumor activity.
|
-
- HY-12062
-
-
- HY-14645
-
-
- HY-112504
-
-
- HY-B1480
-
-
- HY-17479A
-
-
- HY-19819
-
-
- HY-A0063A
-
-
- HY-U00208
-
-
- HY-19649
-
-
- HY-100143
-
-
- HY-B0715
-
-
- HY-112502B
-
-
- HY-N0274
-
-
- HY-112502
-
|
MethADP
Adenosine 5'-(α,β-methylene)diphosphate
|
CD73
|
Cancer
|
|
MethADP is a specific CD73 inhibitor.
|
-
- HY-15759A
-
-
- HY-17620
-
-
- HY-U00065
-
-
- HY-112504A
-
-
- HY-N2553
-
|
4-Deoxypyridoxine 5'-phosphate
|
LPL Receptor
|
Metabolic Disease
|
|
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase.
|
-
- HY-15509A
-
|
Semapimod tetrahydrochloride
CNI-1493; CPSI-2364 tetrahydrochloride
|
TNF Receptor
Interleukin Related
p38 MAPK
|
Inflammation/Immunology
|
|
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
|
-
- HY-124756
-
|
SBI-425
|
Phosphatase
|
Cardiovascular Disease
|
|
SBI-425 is a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor. Long-term administration of SBI-425 effectively reaches and inhibits TNAP in the vasculature, improving cardiovascular parameters and survival at a dose that does not cause a detectable change in bone.
|
-
- HY-12842
-
|
UC-112
|
IAP
|
Cancer
|
|
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
|
-
- HY-B0789
-
|
SU6656
|
Src
FAK
Akt
|
Cancer
|
|
SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.
|
-
- HY-106697
-
|
Statil
Ponalrestat
|
Aldose Reductase
|
Metabolic Disease
|
|
Statil (Ponalrestat) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Statil selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Statil inhibits the conversion of glucose to sorbitol.
|
-
- HY-108486
-
|
Herbimycin A
|
Bacterial
Antibiotic
|
|
|
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL. Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
|
-
- HY-12810
-
|
EHop-016
|
Ras
|
Cancer
|
|
EHop-016 is a novel potent and selective inhibitor of Rac GTPase; inhibits Rac1 activity in MDA-MB-435 cells with an IC50 of 1.1 uM.
|
-
- HY-100111
-
-
- HY-12871C
-
|
Atuveciclib S-Enantiomer
BAY-1143572 S-Enantiomer
|
CDK
|
Cancer
|
|
Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and selective CDK9 inhibitor, which inhibits CDK9/CycT1 with an IC50 of 16 nM.
|
-
- HY-B0856
-
|
Validamycin A
|
Fungal
Tyrosinase
|
Infection
|
|
Validamycin A is an aminoglycoside agricultural antibiotic. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM.
|
-
- HY-W011044
-
|
CID 5951923
|
KLF
|
Cancer
|
|
CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro.
|
-
- HY-19363
-
-
- HY-13991
-
|
CCG-1423
|
Ras
|
Cancer
|
|
CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.
|
-
- HY-50866
-
-
- HY-124861
-
-
- HY-16667
-
|
HLM006474
|
Others
|
Cancer
|
|
HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
|
-
- HY-19696A
-
|
Tauroursodeoxycholate Sodium
Sodium tauroursodeoxycholate; Tauroursodeoxycholic acid sodium salt
|
ERK
Caspase
|
Cancer
|
|
Tauroursodeoxycholate Sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
|
-
- HY-15881
-
|
TCS JNK 5a
JNK Inhibitor IX
|
JNK
Apoptosis
|
Cancer
|
|
TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
|
-
- HY-13227
-
|
SD-208
|
TGF-β Receptor
|
Cancer
|
|
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
|
-
- HY-15125
-
-
- HY-14682
-
|
GSK319347A
|
IKK
|
Inflammation/Immunology
|
|
GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
|
-
- 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-15192
-
|
GSK 650394
|
SGK
Influenza Virus
|
Cancer
Infection
|
|
GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.
|
-
- HY-15719
-
|
NU 7026
LY293646
|
DNA-PK
Apoptosis
|
Cancer
|
|
NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
|
-
- HY-12993
-
|
RSV604
(S)-1-(2-Fluorophenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea
|
RSV
|
Infection
|
|
RSV604 is a novel inhibitor of respiratory syncytial virus replication(EC50=0.86 uM); a putative RSV nucleoprotein(N) inhibitor in phase 2 clinical trials.
|
-
- HY-B0869A
-
|
Bispyribac sodium
|
Others
|
Others
|
|
Bispyribac sodium is a selective, systemic and post emergent herbicide used to eradicate grasses and broad leaf weeds. Bispyribac sodium is also an acetolactate synthase (ALS or known as AHAS) inhibitor.
|
-
- HY-13915
-
|
NSC348884
|
Apoptosis
|
Cancer
|
|
NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.
|
-
- HY-112522
-
|
HS79
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
HS-79 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-79 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 1.57 μM.
|
-
- HY-16663
-
|
ITX3
|
Others
|
Others
|
|
ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.
|
-
- HY-100223
-
-
- HY-W009783
-
|
1-Deoxymannojirimycin hydrochloride
|
HIV
Influenza Virus
|
Infection
|
|
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity.
|
-
- HY-101920
-
|
Autophinib
|
Autophagy
|
Cancer
Neurological Disease
|
|
Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
|
-
- HY-N1127
-
|
Tricin
|
CMV
|
Cancer
Infection
|
|
Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.
|
-
- HY-W011094
-
|
Win 18446
|
Aldehyde Dehydrogenase (ALDH)
|
Endocrinology
|
|
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.
|
-
- HY-N2532
-
|
Diphyllin
|
HIV
Proton Pump
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
|
Diphyllin is an arylnaphthalene lignan isolated from Justicia procumbens and is a potent HIV-1 inhibitor with an IC50 of 0.38 μM. Diphyllin is active against vesicular stomatitis virus (VSV) and influenza virus. Diphyllin is a vacuolar type H +-ATPase (V-ATPase) inhibitor with an IC50 value of 17 nM and inhibits lysosomal acidification in human osteoclasts. Diphyllin inhibits NO production with an IC50 of 50 μM and has anticancer and anti-inflammatory activities.
|
-
- HY-115510
-
|
SPR inhibitor 3
SPRi3
|
Others
|
Inflammation/Immunology
|
|
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
|
-
- HY-12276
-
|
MALT1 inhibitor MI-2
|
MALT1
|
Cancer
|
|
MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
|
-
- HY-14521
-
|
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-131275
-
|
Imatinib Impurity E
|
Others
|
Others
|
|
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-14521B
-
|
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-N6701
-
|
Dihydrocytochalasin B
|
Arp2/3 Complex
|
Cancer
|
|
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport. Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis. Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca 2+increase in the mucosal scrapings.
|
-
- HY-12688A
-
|
Succinyl phosphonate trisodium salt
|
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
Metabolic Disease
Neurological Disease
|
|
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-B1320
-
|
Meclofenamate sodium
Meclofenamic acid sodium
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Meclofenamic acid sodium is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.
|
-
- HY-N5011
-
|
5,7-Dimethoxyflavone
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
|
-
- HY-N7204
-
-
- HY-111549
-
|
Bragsin1
|
Others
|
Cancer
|
|
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
|
-
- HY-17401
-
|
Ranolazine dihydrochloride
CVT 303 dihydrochloride; RS 43285
|
Calcium Channel
Sodium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.
|
-
- HY-13982
-
|
JSH-23
|
NF-κB
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
|
-
- HY-W009156
-
-
- HY-13599
-
|
Cladribine
2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA
|
Adenosine Deaminase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Cladribine (2CdA), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity and can be used for the research of several hematologic malignancies and multiple sclerosis.
|
-
- HY-125586
-
|
β-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-11006
-
|
KU-57788
NU7441
|
DNA-PK
CRISPR/Cas9
|
Cancer
|
|
KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively.
|
-
- HY-14644A
-
|
Apilimod mesylate
STA 5326 mesylate
|
Interleukin Related
PIKfyve
|
Inflammation/Immunology
|
|
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.
|
-
- 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-136199
-
|
SIRT1-IN-1
|
Sirtuin
CMV
|
Infection
|
|
SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC50 of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.
|
-
- HY-108900
-
|
Leu-AMS
|
Aminoacyl-tRNA Synthetase
Bacterial
|
Cancer
Infection
|
|
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
|
-
- HY-14644
-
|
Apilimod
STA 5326
|
Interleukin Related
PIKfyve
|
Inflammation/Immunology
|
|
Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.
|
-
- HY-N2036
-
|
Mosloflavone
|
Enterovirus
Bacterial
|
Infection
|
|
Mosloflavone is a flavonoid isolated from Scutellaria baicalensis Georgi with anti-EV71 activity. Mosloflavone inhibits VP2 virus replication and protein expression during the initial stage of virus infection and inhibits viral VP2 capsid protein synthesis. Mosloflavone is a promising biocide and inhibits P. aeruginosa virulence and biofilm formation.
|
-
- HY-108341A
-
|
PF-06424439 methanesulfonate
|
Acyltransferase
|
Metabolic Disease
|
|
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
|
-
- HY-15982
-
-
- HY-W015445
-
|
SD-169
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
|
-
- HY-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-110150
-
|
UNC3230
|
Others
|
Cancer
Inflammation/Immunology
|
|
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects.
|
-
- HY-18643
-
|
TZ9
|
E1/E2/E3 Enzyme
|
Cancer
|
|
TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
|
-
- HY-18696
-
|
AMG-337
|
c-Met/HGFR
|
Cancer
|
|
AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.
|
-
- HY-B1490
-
-
- HY-P2502
-
-
- HY-10006
-
|
Flavopiridol Hydrochloride
Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride
|
CDK
Autophagy
HIV
|
Cancer
|
|
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
|
-
- HY-N0102
-
-
- HY-11102
-
-
- HY-14427
-
-
- HY-13865
-
|
P 22077
|
Deubiquitinase
|
Cancer
|
|
P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. It also inhibits USP47 with an EC50 of 8.74 μM.
|
-
- HY-16712
-
|
LDN-214117
|
TGF-β Receptor
|
Cancer
|
|
LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
|
-
- HY-15716
-
|
Kobe0065
|
Ras
Apoptosis
|
Cancer
|
|
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
|
-
- HY-U00422
-
|
K-756
|
PARP
|
Cancer
|
|
K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively.
|
-
- HY-100742
-
-
- HY-114166
-
-
- HY-109031
-
|
Dotinurad
|
URAT1
|
Metabolic Disease
|
|
Dotinurad is a potent and selective urate reabsorption inhibitor. Dotinurad inhibits urate transporter 1 (URAT1) with an IC50 value of 37.2 nM. Dotinurad acts as a uricosuric agent.
|
-
- HY-101840
-
-
- HY-15004
-
|
AUZ 454
K03861
|
CDK
|
Cancer
|
|
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
|
-
- HY-12067
-
|
R406
|
Syk
Apoptosis
|
Cancer
|
|
R406 is a competitive Syk inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value.
|
-
- HY-N6738
-
-
- HY-128726
-
-
- HY-19712
-
-
- HY-102087
-
|
JPM-OEt
|
Cathepsin
|
Cancer
|
|
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.
|
-
- HY-50908
-
|
Ridaforolimus
MK-8669; Deforolimus; AP23573
|
mTOR
Autophagy
|
Cancer
|
|
Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
|
-
- HY-101840A
-
-
- HY-15839
-
-
- HY-10074
-
-
- HY-13020
-
-
- HY-112433
-
|
NIK SMI1
|
NF-κB
|
Inflammation/Immunology
|
|
NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC50 of 0.23±0.17 nM.
|
-
- HY-129700
-
-
- HY-124944
-
|
APS6-45
|
Ras
|
Cancer
|
|
APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
|
-
- HY-18964
-
|
MG-101
Calpain inhibitor I; Ac-LLnL-CHO; ALLN
|
Proteasome
|
Cancer
|
|
MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
|
-
- HY-12961A
-
-
- HY-19236
-
-
- HY-101835
-
-
- HY-B1839
-
-
- HY-B0207A
-
-
- HY-15681
-
-
- HY-112670
-
-
- HY-19123
-
-
- HY-103710
-
-
- HY-U00222
-
-
- HY-12703
-
-
- HY-B1542A
-
-
- HY-112097
-
-
- HY-19979
-
-
- HY-U00176
-
-
- HY-N0221
-
-
- HY-U00175
-
-
- HY-10827
-
-
- HY-13061
-
-
- HY-15723A
-
-
- HY-66009
-
-
- HY-B0597
-
-
- HY-101644A
-
-
- HY-101647
-
-
- HY-50671
-
-
- HY-12804
-
-
- HY-104074
-
-
- HY-107362
-
-
- HY-101862
-
-
- HY-113057
-
-
- HY-12527
-
-
- HY-U00444
-
-
- HY-13555
-
|
β-Lapachone
ARQ-501; NSC-26326
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
|
-
- HY-17393
-
-
- HY-N4315
-
|
Pomiferin
NSC 5113
|
HDAC
mTOR
|
Cancer
|
|
Pomiferin (NSC 5113), a flavonoid from the fruits of Maclura pomifera, acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).
|
-
- HY-13728A
-
|
(R)-Plevitrexed
(R)-ZD 9331; (R)-BGC9331
|
Others
|
Cancer
|
|
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.
|
-
- HY-100578
-
|
AGK2
|
Sirtuin
Apoptosis
|
Cancer
|
|
AGK2 is a selective SIRT2 inhibitor with IC50 of 3.5 μM. AGK2 can also inhibit SIRT1 and SIRT3 with IC50 of 30 and 91 μM, respectively.
|
-
- HY-108318
-
-
- HY-16736A
-
-
- HY-112220
-
|
VIT-2763
|
Others
|
Metabolic Disease
|
|
VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia.
|
-
- HY-16134A
-
|
Celgosivir hydrochloride
MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride
|
Glucosidase
HCV
HIV
|
Infection
|
|
Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
|
-
- HY-107366
-
|
SGN-2FF
|
Others
|
Cancer
|
|
SGN-2FF is a potent and orally active inhibitor of fucosylation, directly inhibits fucosyltransferase activity. SGN-2FF possesses antitumor activity.
|
-
- HY-13605
-
-
- HY-113950
-
-
- HY-16956
-
|
CC-223
|
mTOR
Apoptosis
|
Cancer
|
|
CC-223 is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. CC-223 inhibits both mTORC1 and mTORC2.
|
-
- HY-14908
-
-
- HY-13605A
-
-
- HY-12558
-
