Search Result
Results for "
orally available
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
24
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-147041
-
GB1211
|
Galectin
|
Cancer
|
Selvigaltin (GB1211) is an orally available galectin-3 (Gal-3) inhibitor .
|
-
-
- HY-17359
-
ICL 670
|
Bacterial
Ferroptosis
|
Cancer
|
Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload .
|
-
-
- HY-145598
-
HMPL-523
|
Syk
|
Cancer
|
Sovleplenib (HMPL-523) is a highly potent, orally available and selective SYK inhibitor with an IC50 of 25 nM. Anti-tumor activity. Sovleplenib can be used for the research of immune thrombocytopenia (ITP) .
|
-
-
- HY-116524
-
|
5-HT Receptor
|
Neurological Disease
|
PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile .
|
-
-
- HY-144110
-
|
HCV
|
Infection
|
HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage .
|
-
-
- HY-107623
-
|
MCHR1 (GPR24)
|
Metabolic Disease
|
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R . TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively .
|
-
-
- HY-13540
-
GPI 21016
|
PARP
|
Cancer
|
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent .
|
-
-
- HY-12085
-
-
-
- HY-106080A
-
U-63557A
|
Others
|
Cardiovascular Disease
|
Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent .
|
-
-
- HY-14806
-
MP-513
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM .
|
-
-
- HY-106080
-
U-63557A free acid
|
Others
|
Cardiovascular Disease
|
Furegrelate (U-63557A free acid) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate is being developed as an antiplatelet agent .
|
-
-
- HY-128575
-
|
nAChR
|
Neurological Disease
|
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-agent like properties and clinical candidate potential. .
|
-
-
- HY-112823A
-
HS-10296 mesylate
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
|
-
-
- HY-142663
-
-
-
- HY-100830
-
|
Wnt
MAP4K
|
Cancer
|
NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
|
-
-
- HY-16445
-
-
-
- HY-10159
-
AMN107
|
Bcr-Abl
Autophagy
|
Cancer
|
Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
|
-
-
- HY-16774
-
-
-
- HY-12507
-
-
-
- HY-12727
-
-
-
- HY-10180
-
|
Aurora Kinase
|
Cancer
|
MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
|
-
-
- HY-11077
-
-
-
- HY-110095
-
-
-
- HY-145355
-
-
-
- HY-15828
-
-
-
- HY-100388
-
|
SHP2
Phosphatase
|
Cancer
|
SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM .
|
-
-
- HY-100388A
-
|
SHP2
Phosphatase
|
Cancer
|
SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM .
|
-
-
- HY-13796
-
-
-
- HY-114332
-
-
-
- HY-109032
-
DS-8500a
|
GPR119
|
Metabolic Disease
|
Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
|
-
-
- HY-14857
-
-
-
- HY-115777
-
|
ROR
|
Neurological Disease
|
ARN-6039 is an orally available inverse agonist of RORγ for autoimmune demyelinating disease.
|
-
-
- HY-19741
-
|
Bcl-2 Family
|
Cancer
|
A-1331852 is an orally available BCL-XL selective inhibitor with a Ki of less than 10 pM.
|
-
-
- HY-13742
-
IPdR
|
Others
|
Cancer
|
Ropidoxuridine (IPdR) is a novel orally available, halogenated thymidine analog and is a potential radiosensitizer for use in human tumors.
|
-
-
- HY-109018
-
|
SGLT
|
Metabolic Disease
|
Velagliflozin is an orally available sodium-glucose cotransporter 2 (SGLT2) inhibitor, with anti-diabetic activity.
|
-
-
- HY-15291
-
|
GPR119
|
Metabolic Disease
|
MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
|
-
-
- HY-15599
-
SSR
|
FGFR
|
Cancer
|
SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
|
-
-
- HY-14870
-
-
-
- HY-15411
-
-
-
- HY-101611
-
|
CDK
|
Cancer
|
MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC50 of 2.6 nM for CDK8.
|
-
-
- HY-14832
-
-
-
- HY-B0177
-
-
-
- HY-18954
-
|
PARP
|
Cancer
|
NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
|
-
-
- HY-12428
-
-
-
- HY-108339
-
|
Acyltransferase
|
Metabolic Disease
|
PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
|
-
-
- HY-109059
-
BAY1142524
|
Others
|
Cardiovascular Disease
|
Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
|
-
-
- HY-109096
-
LMB763
|
FXR
Autophagy
|
Inflammation/Immunology
|
Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH) .
|
-
-
- HY-15599A
-
SSR free acid
|
FGFR
|
Cancer
|
SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
|
-
-
- HY-109082A
-
SKI-O-703 dimesylate
|
Syk
|
Inflammation/Immunology
|
Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities .
|
-
-
- HY-40354
-
-
- HY-100946
-
RXDX-106
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.
|
-
- HY-103020
-
|
Others
|
Cancer
|
BAY-1816032 is a potent and oral available BUB1 (budding uninhibited by benzimidazoles 1) kinase inhibitor with an IC50 of 7 nM.
|
-
- HY-16785A
-
INXN-1001 racemate; RG-115932 racemate
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
Veledimex racemate (INXN-1001 racemate) is the racemate of veledimex. Veledimex is an orally available, small-molecule activator ligand for the RheoSwitch Therapeutic System .
|
-
- HY-101773
-
|
c-Met/HGFR
|
Cancer
|
c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
|
-
- HY-15837
-
|
PI3K
|
Cancer
|
SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC50 of 23 nM .
|
-
- HY-128604
-
|
ROR
|
Cancer
|
XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM .
|
-
- HY-101782
-
|
SGLT
|
Metabolic Disease
|
HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities .
|
-
- HY-162076
-
|
Others
|
Neurological Disease
|
AEP-IN-3 (compound 18) is an orally active, potent and brain penetrant asparagine endopeptidase (AEP) inhibitor, with an IC50 of 7.8 ± 0.9 nM. AEP-IN-3 can be used for Alzheimer’s Disease (AD) research .
|
-
- HY-14817
-
PPM 204
|
PPAR
|
Metabolic Disease
|
Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ .
|
-
- HY-A0076
-
LJC 11036
|
Bacterial
Antibiotic
|
Infection
|
Tebipenem is an orally available carbapenem antibiotic, shows broad-spectrum activity against Gram-positive and -negative bacteria, except for Pseudomonas aeruginosa.
|
-
- HY-100493
-
|
STAT
|
Cancer
|
BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
|
-
- HY-101729
-
|
Others
|
Cardiovascular Disease
|
Anti-Heart Failure Agent 1 an orally available compound suitable for the treatment of heart failure without inducing nausea, vomiting and restlessness.
|
-
- HY-117632
-
ABX-1431
|
MAGL
|
Neurological Disease
|
Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
|
-
- HY-17627
-
CCX168
|
|
|
Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor (C5aR) inhibitor with an IC50 of 0.1 nM.
|
-
- HY-12042
-
AS703026; MSC1936369B
|
MEK
|
Cancer
|
Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
|
-
- HY-10804
-
|
Aurora Kinase
Apoptosis
|
Cancer
|
CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
|
-
- HY-16265
-
-
- HY-100209
-
TAK-013
|
GnRH Receptor
|
Endocrinology
|
Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
|
-
- HY-14272
-
BMS-207147; ER-30346
|
Fungal
|
Infection
Cancer
|
Ravuconazole (BMS-207147;ER-30346) is an orally available triazole antifungle agent that potently inhibits a wide range of fungi.
|
-
- HY-108413
-
BMN 673ts
|
PARP
|
Cancer
|
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
|
-
- HY-A0176
-
|
|
|
Glisoxepide, a sulphonamide derivative, is an orally available nonselective K(ATP) channel blocker, with antihyperglycemic activity and cardiovascular regulation effect .
|
-
- HY-106392
-
NB-DGJ; N-(n-Butyl)deoxygalactonojirimycin
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
Lucerastat, the galactose form of Miglustat, is an orally-available inhibitor of glucosylceramide synthase (GCS). Lucerastat has the potential for Fabry disease study .
|
-
- HY-139847
-
|
ROR
|
Inflammation/Immunology
|
RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.
|
-
- HY-19680
-
|
|
|
Prinomide tromethamine is an orally available nonsteroidal anti-inflammatory agent. Prinomide tromethamine can be used to study inflammation, such as rheumatoid arthritis .
|
-
- HY-110043
-
|
Others
|
Cardiovascular Disease
|
(±)-Clopidogrel hydrochloride is an antithrombotic agent that is ADP-selective and orally available. (±)-Clopidogrel hydrochloride inhibits platelet aggregation by inhibiting the binding of ADP to its platelet receptors .
|
-
- HY-101570
-
Peposertib; M3814
|
DNA-PK
|
Cancer
|
Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. Anti-tumor activity .
|
-
- HY-15324
-
-
- HY-19189
-
-
- HY-13041
-
-
- HY-18072
-
GSK2606414
Maximum Cited Publications
67 Publications Verification
|
PERK
Autophagy
Apoptosis
|
Cancer
|
GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
|
-
- HY-19903
-
|
Others
|
Cancer
|
ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3.
|
-
- HY-10159S
-
AMN107-d6
|
|
|
Nilotinib-d6 is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1].
|
-
- HY-101437
-
FCE-26742A
|
|
|
Ralfinamide (FCE-26742A) is an orally available Na + blocker derived from α-aminoamide, with function of suppressing pain .
|
-
- HY-19803
-
ASP8273 mesylate
|
EGFR
|
Cancer
|
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
|
-
- HY-32721
-
HKI-272
|
EGFR
|
Cancer
|
Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively .
|
-
- HY-132549S
-
-
- HY-112912
-
|
P-glycoprotein
|
Cancer
|
P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR) .
|
-
- HY-19729
-
ASP8273
|
EGFR
|
Cancer
|
Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
|
-
- HY-101437A
-
FCE-26742A mesylate
|
Sodium Channel
|
Neurological Disease
|
Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na + channel blocker derived from α-aminoamide, with function of suppressing pain .
|
-
- HY-32721B
-
HKI-272 maleate
|
EGFR
|
Cancer
|
Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively .
|
-
- HY-14574
-
|
Aurora Kinase
VEGFR
|
Cancer
|
PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
|
-
- HY-10011
-
-
- HY-B1141
-
NC-503
|
Amyloid-β
|
Others
|
Eprodisate disodium (NC-503) is the orally available disodium salt form of Eprodisate, a negatively charged sulfonated inhibitor of fibrillogenesis, that can be used in the treatment of amyloid A (AA) amyloidosis.
|
-
- HY-100844
-
|
MAP3K
Apoptosis
|
Cancer
|
GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM .
|
-
- HY-19612B
-
|
Histone Demethylase
|
Cancer
|
DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
|
-
- HY-13233B
-
|
Dipeptidyl Peptidase
|
Others
|
Talabostat isomer mesylate is an isomer of talabostat mesylate. Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
|
-
- HY-16511
-
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-109754
-
PF-03709270
|
Bacterial
Antibiotic
|
Infection
|
Sulopenem etzadroxil (PF-03709270) is an orally available ester proagent form of sulopenem, with broad-spectrum antibacterial activity against most gram-positive and gram-negative bacteria.
|
-
- HY-10286A
-
PHX-1149
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
Dutogliptin tartrate (PHX-1149) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
|
-
- HY-108532
-
|
RAR/RXR
|
Cancer
|
AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC50 of 8.0 .
|
-
- HY-14870S3
-
-
- HY-10286
-
PHX-1149 free base
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
Dutogliptin (PHX-1149 free base) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
|
-
- HY-13328
-
INK-128; MLN0128; TAK-228
|
mTOR
Autophagy
|
Cancer
|
Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.
|
-
- HY-B0263
-
-
- HY-19612A
-
|
|
|
DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM .
|
-
- HY-111409
-
|
RIP kinase
|
Inflammation/Immunology
|
RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04) .
|
-
- HY-120872
-
|
Others
|
Metabolic Disease
|
AJS1669 free acid is a potent and orally available glycogen synthase (GS) activator. AJS1669 improves glucose metabolism and reduces body fat mass in mice[1].
|
-
- HY-16774S
-
BAY1021189-d3 hydrochloride
|
Isotope-Labeled Compounds
|
Others
|
Vericiguat-d3 (BAY1021189-d3) hydrochloride is a deuterated Vericiguat with tracer functionality. Vericiguat is an orally available stimulator of guanylate cyclase .
|
-
- HY-15889
-
AMG 925
2 Publications Verification
|
FLT3
CDK
|
Cancer
|
AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
|
-
- HY-18988
-
ETC-1922159
|
Porcupine
Wnt
|
Cancer
|
ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
|
-
- HY-17617
-
Z-360
|
Cholecystokinin Receptor
|
Endocrinology
Cancer
|
Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
|
-
- HY-15889A
-
|
FLT3
CDK
|
Cancer
|
AMG 925 HCl is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively.
|
-
- HY-107781
-
-
- HY-14272S
-
|
Isotope-Labeled Compounds
Fungal
|
Infection
|
Ravuconazole-d4 is the deuterium labeled Ravuconazole. Ravuconazole (BMS-207147) is an orally available triazoleantifungle agent that potently inhibits a wide range of fungi[1][2].
|
-
- HY-112439
-
-
- HY-17359S
-
-
- HY-B0177S
-
|
Bacterial
|
Infection
|
Tinidazole-d5 is the deuterium labeled Tinidazole. Tinidazole, an orally available antibacterial agent, is a 5-nitroimidazole with selective activity against anaerobic bacteria and protozoa[1].
|
-
- HY-14806S
-
MP-513 D8
|
|
|
Teneligliptin-d8 is a deuterium labeled Teneligliptin (MP-513). Teneligliptin is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor[1].
|
-
- HY-124281
-
|
Others
|
Others
|
9(R)-PAHSA is a R-enantiomer of 9-PAHSA. 9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation .
|
-
- HY-124281A
-
|
Others
|
Others
|
9(S)-PAHSA is a S-enantiomer of 9-PAHSA. 9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation .
|
-
- HY-40354A
-
-
- HY-15564
-
|
GPR119
|
Metabolic Disease
|
AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s .
|
-
- HY-12789
-
APD334
|
LPL Receptor
|
Inflammation/Immunology
|
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
|
-
- HY-19650
-
MKC-733; DDP-733
|
5-HT Receptor
|
Metabolic Disease
|
Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
|
-
- HY-14870S1
-
-
- HY-105634
-
|
Progesterone Receptor
|
Endocrinology
Cancer
|
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
|
-
- HY-U00002
-
|
VEGFR
EGFR
|
Cancer
|
ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
|
-
- HY-19957
-
Debio 1347; CH5183284
|
FGFR
|
Cancer
|
Zoligratinib (Debio 1347) is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
|
-
- HY-40354S
-
Tasocitinib-13C3; CP-690550-13C3
|
JAK
Apoptosis
|
Inflammation/Immunology
Cancer
|
Tofacitinib- 13C3 is the 13C-labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
|
-
- HY-101784
-
|
GPR4
|
Inflammation/Immunology
|
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity .
|
-
- HY-114330A
-
|
PAI-1
Ser/Thr Protease
|
Inflammation/Immunology
|
ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively .
|
-
- HY-128770
-
|
Dopamine Receptor
|
Neurological Disease
|
LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor
positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM) .
|
-
- HY-12744A
-
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
Genz-123346 is a potent, orally available glucosylceramide synthase inhibitor. Genz-123346 blocks the conversion of ceramide to glucosylceramide (GL1) and inhibits GM1 with an IC50 value of 14 nM .
|
-
- HY-126361
-
|
Ser/Thr Protease
PAI-1
|
Inflammation/Immunology
|
ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively .
|
-
- HY-114330
-
|
PAI-1
Ser/Thr Protease
|
Inflammation/Immunology
|
ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively .
|
-
- HY-124502
-
|
TAM Receptor
FLT3
|
Cancer
|
UNC4203 is a potent, orally available and highly selective MERTK inhibitor, with IC50s of 1.2 nM, 140 nM, 42 nM and 90 nM for MERTK, AXL, TYRO3 and FLT3, respectively .
|
-
- HY-19926
-
RG-7602
|
|
|
GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies .
|
-
- HY-138802
-
|
Others
|
Metabolic Disease
|
ML089 is a potent, selective, and orally available phosphomannose isomerase (PMI) inhibitor with an IC50 of 1.3 µM. ML089 can be used for the research of congenital disorder of glycosylation Ia .
|
-
- HY-126361A
-
|
Ser/Thr Protease
PAI-1
|
Inflammation/Immunology
|
ZK824190 hydrochloride is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively .
|
-
- HY-17359R
-
ICL 670 (Standard)
|
Bacterial
Ferroptosis
|
Cancer
|
Deferasirox (Standard) is the analytical standard of Deferasirox. This product is intended for research and analytical applications. Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload .
|
-
- HY-B0177R
-
|
Bacterial
Antibiotic
Parasite
|
Infection
Cancer
|
Tinidazole (Standard) is the analytical standard of Tinidazole. This product is intended for research and analytical applications. Tinidazole, an orally available antibacterial agent, is a 5-nitroimidazole with selective activity against anaerobic bacteria and protozoa .
|
-
- HY-101212
-
CYC065
|
CDK
|
Cancer
|
Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively .
|
-
- HY-112256
-
ACP-105
5 Publications Verification
|
Androgen Receptor
|
Inflammation/Immunology
|
ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
|
-
- HY-11021
-
PRT060128
|
P2Y Receptor
|
Cardiovascular Disease
|
Elinogrel (PRT060128) is a potent, direct acting, competitive, and reversible platelet P2Y12 antagonist (IC50=20 nM). It is orally and intravenously available and has potent antiplatelet effects .
|
-
- HY-W127442
-
Ethyl 2-Ethylbutyrate
|
Bacterial
|
Others
|
Etzadroxil (Ethyl 2-Ethylbutyrate) is a volatile ester compound. Sulopenem Etzadroxil is an orally available ester proagent form of Sulopenem, an antibiotic with broad-spectrum activities against Gram-positive and Gram-negative bacteria .
|
-
- HY-B1069R
-
SIN-10 (Standard); Morsydomine (Standard)
|
Drug Metabolite
|
Cardiovascular Disease
|
Molsidomine (Standard) is the analytical standard of Molsidomine. This product is intended for research and analytical applications. Molsidomine is an orally available, long-acting vasodilator that is metabolized in the liver to the active metabolite Linsidomine, an unstable compound that releases NO and acts as a vasodilator.
|
-
- HY-156290
-
-
- HY-14691
-
BAY 869766; RDEA119
|
MEK
|
Cancer
|
Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively.
|
-
- HY-12296
-
AMG 232; KRT-232
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM .
|
-
- HY-19822B
-
RAD1901 S enantiomer dihydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
Elacestrant S enantiomer dihydrochloride (RAD1901 S enantiomer dihydrochloride) is an low activity enantiomer of elacestrant dihydrochloride. Elacestrant (RAD1901) dihydrochloride is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.
|
-
- HY-101026
-
|
HSP
|
Cancer
|
CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
|
-
- HY-103007
-
GPR39-C3
|
GHSR
|
Metabolic Disease
Endocrinology
|
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
|
-
- HY-109024
-
RG7314
|
Vasopressin Receptor
|
Neurological Disease
Endocrinology
|
Balovaptan (RG7314) is an orally available, selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
|
-
- HY-W012550
-
|
Parasite
|
Infection
|
D-Carnitine is an orally available isomer of the essential nutrient L-carnitine that promotes long-chain fatty acid transport into the mitochondrial matrix for beta-oxidation. D-Carnitine has antiparasitic activity .
|
-
- HY-13904
-
HHGV678
|
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively .
|
-
- HY-111407
-
MK-8353
2 Publications Verification
SCH900353
|
ERK
|
Cancer
|
MK-8353 (SCH900353) is a potent, selective and orally available ERK1/2 inhibitor, with IC50s of 23.0 nM and 8.8 nM, respectively; MK-8353 has antitumor activity.
|
-
- HY-19822D
-
RAD1901 S enantiomer
|
Estrogen Receptor/ERR
|
Cancer
|
Elacestrant S enantiomer (RAD1901 S enantiomer) is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively .
|
-
- HY-102037
-
-
- HY-10716A
-
|
GlyT
|
Neurological Disease
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
|
-
- HY-123475
-
RV521
|
RSV
|
Infection
|
Sisunatovir (RV521), an orally available inhibitor of the RSV protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively .
|
-
- HY-161065
-
|
Bacterial
|
Infection
|
HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection .
|
-
- HY-13038A
-
R788
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-18708
-
JNJ-42756493
|
FGFR
Apoptosis
|
Cancer
|
Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
|
-
- HY-109061
-
YH25448; GNS-1480
|
EGFR
|
Cancer
|
Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer .
|
-
- HY-18317
-
|
VEGFR
RET
c-Kit
|
Cancer
|
JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively .
|
-
- HY-W751099
-
|
Isotope-Labeled Compounds
|
Others
|
Corticosterone- 13C3 is a 13C-labeled corticosterone (HY-B1618). Corticosterone (17-Deoxycortisol) is an orally available glucocorticoid that can regulate limbic system neurons and has good immunosuppressive activity.
|
-
- HY-13038
-
R788(Disodium)
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
Fostamatinib Disodium (R788 Disodium) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-13038B
-
R788 disodium hexahydrate
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-112134
-
|
Others
|
Cancer
|
CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM .
|
-
- HY-B1693
-
Methotrimeprazine
|
|
|
Levomepromazine (Methotrimeprazine) is an orally available neuroleptic agent, which is commonly used to relieve nausea and vomiting in palliative care settings. Levomepromazine has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors .
|
-
- HY-145653
-
-
- HY-101268
-
|
|
|
CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available BCR-ABL, SRC and p38 kinase inhibitor with IC50 values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively .
|
-
- HY-149430
-
|
Amyloid-β
|
Neurological Disease
|
YIAD-0205 is an orally available Aβ(1?42) aggregation inhibitor. YIAD-0205 demonstrated in vivo efficacy in an AD transgenic mouse model with five familial AD mutations (5XFAD) .
|
-
- HY-13049
-
AZD-2171 maleate
|
VEGFR
Autophagy
PDGFR
|
Cancer
|
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
- HY-17612
-
NW-3509
|
Sodium Channel
|
Neurological Disease
|
Evenamide (NW-3509) is an orally available voltage-gated sodium channel (VGSC) blocker (Ki=0.4 µM) for the research of schizophrenia. Evenamide shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness .
|
-
- HY-112134A
-
|
Others
|
Cancer
|
(R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5 .
|
-
- HY-12206
-
MR-12842
|
Histamine Receptor
|
Neurological Disease
|
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM .
|
-
- HY-123475A
-
RV521 hydrochloride
|
RSV
|
Infection
|
Sisunatovir (RV521) hydrochloride, an orally available inhibitor of the RSV fusion (RSV-F) protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively .
|
-
- HY-12206A
-
MR-12842 maleate
|
Histamine Receptor
|
Neurological Disease
|
Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide maleate inhibits [ 3H]histamine synthesis with a Ki of 31 nM .
|
-
- HY-400766
-
|
Others
|
Cancer
|
BWA-522 intermediate-2 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
|
-
- HY-401056
-
|
Others
|
Cancer
|
BWA-522 intermediate-3 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .
|
-
- HY-19822S1
-
RAD1901-d4-1
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
|
-
- HY-10205
-
AZD2171
|
VEGFR
Autophagy
PDGFR
|
Cancer
|
Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
- HY-132831B
-
RO-7486967 potassium
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
Selnoflast (RO-7486967) Potassium, formerly Somalix/RG6418/IZD334, Selnoflast is an orally available inhibitor of NLRP3. Selnoflast is used in the study of systemic inflammation, such as ulcerative colitis and chronic obstructive pulmonary disease .
|
-
- HY-32721S
-
|
EGFR
|
Cancer
|
Neratinib-d6 (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
|
-
- HY-132831
-
RO-7486967
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
Selnoflast (RO-7486967) Formerly known as Somalix/RG6418/IZD334, Selnoflast is an orally available inhibitor of NLRP3. Selnoflast is used in research into systemic inflammation, such as ulcerative colitis and chronic obstructive pulmonary disease .
|
-
- HY-40354AS
-
-
- HY-156111
-
|
PROTACs
Androgen Receptor
|
Cancer
|
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
|
-
- HY-17602
-
BBI503
|
Others
|
Cancer
|
Amcasertib (BBI503) is an orally active and small-molecule multi-kinase inhibitor. Amcasertib exhibits inhibitory activity against the NANOG and CD133 expression and cell viability in PC-9/GR cells. As an orally available cancer cell stemness kinase inhibitor with potential antineoplastic activity, it is currently being studied in phase I clinical trials in a number of cancers.
|
-
- HY-155111
-
|
Phospholipase
|
Neurological Disease
|
nSMase2-IN-1 is an orally active Neutral sphingomyelinase 2 (nSMase2) inhibitor with an IC50 value of 0.13 ± 0.06 μM. nSMase2-IN-1 is metabolically stable in liver microsomes and orally available with a favorable brain-to-plasma ratio. nSMase2-IN-1 can be used for nervous system disease research .
|
-
- HY-12066
-
|
GPR119
|
Metabolic Disease
Inflammation/Immunology
|
GSK-1292263 is an orally available GPR119 agonist with pEC50s of 6.9 and 6.7 for human and rat GPR119, respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM) .
|
-
- HY-15446
-
RG7090; CTEP Derivative
|
mGluR
|
Neurological Disease
|
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM . Basimglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-19822A
-
RAD1901 dihydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
- HY-111388B
-
|
CDK
|
Cancer
|
SEL120-34A hydrochloride is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-19822
-
RAD1901
|
Estrogen Receptor/ERR
|
Cancer
|
Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
- HY-111388
-
|
CDK
|
Cancer
|
SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-12085S
-
CC-10004-d5
|
|
|
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
|
-
- HY-120394
-
|
Fatty Acid Synthase (FASN)
Apoptosis
|
Cancer
|
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth .
|
-
- HY-108015
-
|
Trace Amine-associated Receptor (TAAR)
|
Neurological Disease
|
RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect .
|
-
- HY-101466A
-
|
FGFR
|
Cancer
|
E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively .
|
-
- HY-120062
-
|
Fatty Acid Synthase (FASN)
|
Cancer
|
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression .
|
-
- HY-103023
-
CLP290
1 Publications Verification
|
Potassium Channel
|
Neurological Disease
|
CLP290 is an orally available activator of the neuron-specific K +-Cl − cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats .
|
-
- HY-101447A
-
EPH 116 hydrochloride
|
Others
|
Cancer
|
SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability .
|
-
- HY-101466
-
|
FGFR
|
Cancer
|
E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively .
|
-
- HY-163003
-
|
Parasite
|
Infection
|
Antitrypanosomal agent 19 (compound 10) is an orally available antitrypanosomal agent. Antitrypanosomal agent 19 effectively inhibits the growth of trypanosomatids T. b. brucei, T. b. gambiense and T. b. rhodesiense, mitigating the Human trypanosomiasis (HAT)-induced acute infectious toxicity in mice .
|
-
- HY-155478
-
|
Androgen Receptor
|
Cancer
|
Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
|
-
- HY-100653A
-
|
Epigenetic Reader Domain
|
Cancer
|
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
|
-
- HY-112233
-
O-304
3 Publications Verification
|
AMPK
|
Cardiovascular Disease
Metabolic Disease
|
O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a agent to treat type 2 diabetes (T2D) and associated cardiovascular complications .
|
-
- HY-12296S
-
AMG 232-d7; KRT-232-d7
|
Isotope-Labeled Compounds
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
Navtemadlin-d7 is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM[1][2].
|
-
- HY-129411
-
ACT-519276; OGT2378
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
Sinbaglustat (OGT2378) is a dual inhibitor of glucosylceramide synthase (GCS) and non-lysosomal glucosyl ceramidase (GBA2). Sinbaglustat is an orally available N-alkyl iminosugar that crosses the blood-brain barrier. Sinbaglustat can be used for the research of central neurodegenerative diseases associated with lysosomal dysfunctions .
|
-
- HY-13904S
-
HHGV678-d3
|
Isotope-Labeled Compounds
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
Flumatinib-d3 is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].
|
-
- HY-147268
-
RAF/KIN_2787
|
Raf
p38 MAPK
|
Cancer
|
Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity .
|
-
- HY-114739
-
|
PPAR
|
Metabolic Disease
|
MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC50s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD) .
|
-
- HY-114452
-
BTRX-246040
|
Opioid Receptor
|
Neurological Disease
|
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models .
|
-
- HY-101246
-
|
|
|
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
|
-
- HY-132831A
-
RO-7486967 calcium
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
Selnoflast (RO-7486967) calcium Formerly known as Somalix/RG6418/IZD334, Selnoflast is an orally available inhibitor of NLRP3. Selnoflast is used in the study of systemic inflammation, such as ulcerative colitis and chronic obstructive pulmonary disease[1]/s.br/
|
-
- HY-19322B
-
LGH447 dihydrochloride
|
Pim
Apoptosis
|
Cancer
|
PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis .
|
-
- HY-19322
-
PIM447
3 Publications Verification
LGH447
|
|
|
PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis .
|
-
- HY-10942
-
NVP-BEP800
|
HSP
|
Cancer
|
VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
|
-
- HY-13314
-
XL-647; EXEL-7647; KD-019
|
EGFR
VEGFR
Ephrin Receptor
|
Cancer
|
Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
|
-
- HY-111372A
-
(Rac)-BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold) .
|
-
- HY-130149
-
MRTX849
|
Ras
|
Cancer
|
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
|
-
- HY-130992
-
|
Androgen Receptor
Ligands for Target Protein for PROTAC
|
Cancer
|
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM . Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively .
|
-
- HY-15433A
-
JNJ-26481585 dihydrochloride
|
HDAC
Apoptosis
Autophagy
|
Cancer
|
Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity .
|
-
- HY-19888
-
|
|
|
GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases .
|
-
- HY-160142
-
|
Btk
|
Cancer
|
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .
|
-
- HY-157585S
-
-
- HY-19822S2
-
RAD1901-d10
|
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Cancer
|
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
- HY-117259
-
ALZ-801
|
Amyloid-β
|
Neurological Disease
|
ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
|
-
- HY-12143
-
GR 205171A
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [ 3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent .
|
-
- HY-14806S1
-
MP-513-d4
|
Isotope-Labeled Compounds
Dipeptidyl Peptidase
|
Metabolic Disease
|
Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
|
-
- HY-156121
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
Cancer
|
NLRP3-IN-20 (compound 11) is an orally available inhibitor of the NLRP3 inflammasome with an IC50 of 25 nM for IL-1β secretion. NLRP3-IN-20 has excellent pharmacokinetic properties and demonstrated significant efficacy in models of non-alcoholic steatohepatitis, fatal septic shock, and colitis .
|
-
- HY-13011
-
CH5424802; RO5424802; RG7853
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-13007
-
PF-03758309
|
PAK
Apoptosis
|
Cancer
|
PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-50101A
-
AMD-070 trihydrochloride
|
CXCR
HIV
|
Infection
Endocrinology
Cancer
|
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
|
-
- HY-13007B
-
PF-03758309 dihydrochloride
|
PAK
Apoptosis
|
Cancer
|
PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-50101
-
AMD-070
|
CXCR
HIV
|
Infection
Endocrinology
Cancer
|
Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
|
-
- HY-13007A
-
PF-03758309 hydrochloride
|
PAK
Apoptosis
|
Cancer
|
PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-114452A
-
BTRX-246040 tartrate
|
Opioid Receptor
|
Neurological Disease
|
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models .
|
-
- HY-10885
-
ABT-472
|
PARP
|
Cancer
|
A-620223 succinate (ABT-472) is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor. A-620223 succinate (ABT-472) exhibits very good potency against the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in whole cell assay, making it useful in cancer research .
|
-
- HY-14532
-
CMX001; HDP-CDV
|
CMV
HSV
Orthopoxvirus
|
Infection
|
Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections. Brincidofovir, an oral antiviral in late stage development, has proven effective against orthopoxviruses in vitro and in vivo. .
|
-
- HY-10811
-
GNE-493
2 Publications Verification
|
PI3K
mTOR
|
Cancer
|
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
|
-
- HY-145153
-
|
Cannabinoid Receptor
|
Neurological Disease
|
S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a Ki of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism .
|
-
- HY-153802
-
|
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
Antitumor agent-100 (compound A6) is an orally available apoptosis inducer and molecular gel targeting PDE3A-SLFN12 (IC50: 0.3 μM) with antitumor activity. Antitumor agent-100 binds to the PDE3A enzyme pocket to recruit and stabilize SLFN12, thereby preventing protein translation and leading to apoptosis .
|
-
- HY-15292
-
S107
1 Publications Verification
|
Others
|
Cardiovascular Disease
|
S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca 2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold .
|
-
- HY-155463
-
|
NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM .
|
-
- HY-163110
-
|
HIV
Reverse Transcriptase
|
Infection
|
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC50 of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .
|
-
- HY-13011A
-
CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-111372
-
BAY 94-8862
|
Mineralocorticoid Receptor
|
Cardiovascular Disease
|
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
-
- HY-114491
-
|
ERK
Raf
|
Cancer
|
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-114491A
-
|
ERK
Raf
|
Cancer
|
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-12296A
-
(3S,5S,6R)-AMG 232; (3S,5S,6R)-KRT-232
|
Others
|
Cancer
|
(3S,5S,6R)-Navtemadlin is the isomer of Navtemadlin (HY-12296), and can be used as an experimental control. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM .
|
-
- HY-19822S
-
RAD1901-d4
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
Elacestrant-d4 (RAD1901-d4) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo.
|
-
- HY-19822S3
-
RAD1901-d6
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
Elacestrant-d6 (RAD1901-d6) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo.
|
-
- HY-12067
-
|
Syk
FLT3
Apoptosis
|
Inflammation/Immunology
Cancer
|
R406 is an orally available and competitive Syk/FLT3 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. R406 reduces immune complex-mediated inflammation . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-13010
-
ABR-215062
|
NF-κB
Apoptosis
|
Inflammation/Immunology
|
Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research .
|
-
- HY-10472
-
|
Beta-secretase
|
Neurological Disease
|
LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
|
-
- HY-19834
-
GDC-0853
|
Btk
|
Cancer
|
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research .
|
-
- HY-100867A
-
|
Syk
FLT3
|
Cancer
|
TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-100867
-
|
Syk
FLT3
|
Cancer
|
TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-128895
-
KL1333
1 Publications Verification
|
Mitochondrial Metabolism
|
Metabolic Disease
|
KL1333, a derivative of β-lapachone, is an orally available NAD+ modulator. KL1333 reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL1333 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. KL1333 protects against Cisplatin-induced ototoxicity in mouse cochlear cultures .
|
-
- HY-W062904
-
ABR-215062 sodium
|
NF-κB
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
Laquinimod (ABR-215062) sodium, an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod sodium reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod sodium has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research .
|
-
- HY-120657
-
|
Endogenous Metabolite
|
|
9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation. 9-PAHSA also improved carotid vascular calcification and attenuates cardiac hypertrophy and dysfunction in db/db mice. 9-PAHSA increases the viability of steatosis primary mouse hepatocytes (PMH). 9-PAHSA can be used in research on diabetes, inflammation, and cardiovascular disease .
|
-
- HY-15160
-
TAK-960
2 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-15160B
-
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-19835
-
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM) .
|
-
- HY-13440
-
AMG 511
2 Publications Verification
|
PI3K
|
Cancer
|
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
|
-
- HY-15160A
-
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-13011S
-
CH5424802-d8; RO5424802-d8; AF802-d8
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
- HY-13011S1
-
CH5424802-d6; RO5424802-d6; AF802-d6
|
Isotope-Labeled Compounds
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
|
-
- HY-104036
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)) .
|
-
- HY-111509
-
|
ROR
|
Inflammation/Immunology
|
TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC50=1.9 nM, reporter gene IC50=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ) .
|
-
- HY-12972
-
PF-06747775
|
EGFR
|
Cancer
|
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-76474
-
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-14985
-
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-11108
-
|
Syk
FLT3
Apoptosis
|
Inflammation/Immunology
Cancer
|
R406 free base is an orally available and competitive Syk/FLT3 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. R406 free base reduces immune complex-mediated inflammation . R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-B1201
-
3,3',5-Triiodothyroacetic acid
|
Flavivirus
Thyroid Hormone Receptor
TNF Receptor
|
Endocrinology
|
Tiratricol is an orally available thyroid hormone analog that inhibits pituitary thyroid-stimulating hormone secretion. Tiratricol is an intracellular toxin neutralizer that inhibits LPS and lipid A cytotoxicity with IC50s of 20 μM and 32 μM, respectively. Tiratricol reduces TNF production in lipopolysaccharide-stimulated macrophages. Tiratricol also has antiviral activity and is an inhibitor of yellow fever virus (Flavivirus). It can bind to the RdRp domain of the viral NS5 protein to hinder YFV replication. .
|
-
- HY-107390A
-
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-107390
-
AX-024
1 Publications Verification
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-136927
-
|
STING
|
Inflammation/Immunology
Cancer
|
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
|
-
- HY-15160C
-
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-139554
-
KBP-7072
|
Bacterial
|
Infection
|
Zifanocycline (KBP-7072) is a semisynthetic third-generation aminomethylcycline antibiotic that inhibits the normal function of the bacterial ribosome. Zifanocycline exhibits a broad spectrum of in vitro antibacterial activity against Gram-positive and Gram-negative bacteria, including many multidrug-resistant pathogens. Zifanocycline is available in both oral and injectable formulations. Zifanocycline can be used for the research of acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections .
|
-
- HY-111372S
-
BAY 94-8862-d3
|
Mineralocorticoid Receptor
|
Others
|
Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
|
-
- HY-101562
-
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα .
|
-
- HY-N6660
-
Tricaprin; Glyceryl tridecanoate
|
Endogenous Metabolite
Androgen Receptor
|
Metabolic Disease
|
Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
|
-
- HY-151829
-
|
ADC Linker
|
Others
|
Fmoc-L-Asn(EDA-N3)-OH is a click chemistry reagent containing an azide group. This building block is reported in literature for the modification of Amanitin via Click Chemistry. Alpha-Amanitin is the deadliest member of the amatoxin peptide family produced by the death-cap mushroom A. phalloides. It is an orally available, rigid, bicyclic octapeptide and one of the most lethal known natural products (LD50 = 50-100 μg/kg) acting as highly selective allosteric inhibitor of the RNA polymerase II .
|
-
- HY-149695
-
|
EGFR
|
Cancer
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-13010S
-
ABR-215062-d5
|
Isotope-Labeled Compounds
Apoptosis
NF-κB
|
Inflammation/Immunology
|
Laquinimod-d5 (ABR-215062-d5) is deuterium labeled Laquinimod. Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research .
|
-
- HY-108006
-
DS 5565 besylate
|
Calcium Channel
|
Neurological Disease
|
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
|
-
- HY-117287
-
BMS-986165
|
JAK
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .
|
-
- HY-107535
-
|
GPR119
TRP Channel
|
Metabolic Disease
|
AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes .
|
-
- HY-112289
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
|
-
- HY-130240
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells) . GCN2-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-149539
-
|
FLT3
RET
|
Cancer
|
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
|
-
- HY-157169
-
AMU302
|
Pim
mTOR
Akt
PI3K
|
Cancer
|
IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629) .
|
-
- HY-149770
-
|
Cytochrome P450
|
Metabolic Disease
|
CYP4A11/CYP4F2-IN-2 (compound 15) is an orally available inhibitor of CYP4A11/4F2 with IC50s of 120 nM and 220 nM, respectively. CYP4A11/CYP4F2-IN-2 inhibits 20-HETE production in rat kidney and has potential inhibitory effects on diabetic nephropathy and autosomal dominant polycystic kidney disease .
|
-
- HY-19896
-
COTI-2
2 Publications Verification
|
MDM-2/p53
Apoptosis
|
Cancer
|
COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation .
|
-
- HY-112823B
-
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
|
-
- HY-112823
-
HS-10296
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-13803
-
EPZ-6438; E-7438
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells .
|
-
- HY-N2038
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
Cancer
|
3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma .
|
-
- HY-149433
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
|
-
- HY-12678S1
-
NMS-E628-d8; RXDX-101-d8
|
Isotope-Labeled Compounds
Autophagy
Anaplastic lymphoma kinase (ALK)
Trk Receptor
ROS Kinase
|
Cancer
|
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
|
-
- HY-104042
-
AG-881
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K .
|
-
- HY-109014
-
CMX-157
|
HIV
HBV
Nucleoside Antimetabolite/Analog
|
Infection
|
Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
|
-
- HY-101514
-
-
- HY-112289B
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
(1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
|
-
- HY-109082
-
SKI-O-703
|
Syk
|
Inflammation/Immunology
|
Cevidoplenib (SKI-O-703) is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities. Cevidoplenib is also the mesylate form of SKI-O-592. Cevidoplenib and SKI-O-592 inhibits BCR-mediated survival, proliferation, and differentiation of B cells. And SKI-O-592 potently inhibits multiple kinases with IC50s of 6.2 nM (Syk), 1.859 μM (Jak2), 5.807 μM (Jak3), 0.412 μM (RET), 0.687 μM (KOR), 1.783 μM (FLT3), 16.96 μM (FGFR1), 5.662 μM (FGFR3), and 0.709 μM (Pyk2), respectively .
|
-
- HY-155238
-
|
GABA Receptor
|
Neurological Disease
|
E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
|
-
- HY-149454
-
|
P2Y Receptor
|
Cancer
|
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
|
-
-
-
HY-L061
-
|
3489 compounds
|
Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 3489 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
|
-
-
HY-L0121V
-
|
10,000 compounds
|
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 10K Natural Product-like Compound Library consists of 10,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
|
Cat. No. |
Product Name |
Type |
-
- HY-114491
-
|
Fluorescent Dyes/Probes
|
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
Cat. No. |
Product Name |
Type |
-
- HY-W012550
-
|
Biochemical Assay Reagents
|
D-Carnitine is an orally available isomer of the essential nutrient L-carnitine that promotes long-chain fatty acid transport into the mitochondrial matrix for beta-oxidation. D-Carnitine has antiparasitic activity .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-120657
-
-
-
- HY-N6660
-
Tricaprin; Glyceryl tridecanoate
|
Ketones, Aldehydes, Acids
Source classification
umbellularia californica
Metabolic Disease
Plants
Lauraceae
Disease Research Fields
|
Endogenous Metabolite
Androgen Receptor
|
Trisdecanoin (Tricaprin; Glyceryl tridecanoate) is an orally available precursor of decanoic acid (DA precursor) that can be hydrolyzed to decanoic acid. Trisdecanoin and its metabolite capric acid not only provide the body with a quick source of energy, but can also affect lipid metabolism. Trisdecanoin is a major component of medium chain triglycerides (MCT), which has preventive or inhibitory properties for abdominal aortic aneurysms (AAA), inhibition of cardiovascular disease, and anti-androgen (NSAA) and anti-hyperglycemic properties. Trisdecanoin can be used as an additive in food, medicine and cosmetics .
|
-
-
- HY-N2038
-
|
Structural Classification
Flavonols
Flavonoids
Rutaceae
Plants
Citrus reticulata Blanco
|
Phosphodiesterase (PDE)
|
3,5,6,7,8,3',4'-Heptemthoxyflavone, a flavonoid from satsuma peel, is an orally available CREB activator with anti-tumor and anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-Heptemthoxyflavone inhibits collagenase activity and increases the content of type I procollagen in human dermal fibroblast neoblast (HDFn) cells. 3,5,6,7,8,3',4'-Heptemthoxyflavone induces brain-derived neurotrophic factor (BDNF) expression through the cAMP/ERK/CREB signaling pathway and reduces phosphodiesterase activity in C6 glioma .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-132549S
-
|
Nilotinib-d3 is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1][2].
|
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- HY-14870S3
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Selexipag-d6 is deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
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- HY-16774S
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Vericiguat-d3 (BAY1021189-d3) hydrochloride is a deuterated Vericiguat with tracer functionality. Vericiguat is an orally available stimulator of guanylate cyclase .
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- HY-14272S
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Ravuconazole-d4 is the deuterium labeled Ravuconazole. Ravuconazole (BMS-207147) is an orally available triazoleantifungle agent that potently inhibits a wide range of fungi[1][2].
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- HY-17359S
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Deferasirox-d4 is the deuterium labeled Deferasirox. Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload[1][2][3].
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- HY-B0177S
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Tinidazole-d5 is the deuterium labeled Tinidazole. Tinidazole, an orally available antibacterial agent, is a 5-nitroimidazole with selective activity against anaerobic bacteria and protozoa[1].
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- HY-14870S1
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Selexipag-d7 is the deuterium labeled Selexipag. Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor)[1][2].
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- HY-40354S
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Tofacitinib- 13C3 is the 13C-labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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- HY-W751099
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Corticosterone- 13C3 is a 13C-labeled corticosterone (HY-B1618). Corticosterone (17-Deoxycortisol) is an orally available glucocorticoid that can regulate limbic system neurons and has good immunosuppressive activity.
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- HY-19822S1
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Elacestrant-d4-1 is the deuterium labeled Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively .
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- HY-32721S
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Neratinib-d6 (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
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- HY-40354AS
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Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
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- HY-12296S
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Navtemadlin-d7 is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM[1][2].
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- HY-13904S
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Flumatinib-d3 is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].
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- HY-157585S
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21-Dehydro Budesonide-d8-1 is deuterated labeled dehydrogenated Budesonide (HY-13580). Budesonide is an orally available glucocorticoid receptor agonist with anti-cancer activity. 21-Dehydro Budesonide-d8-1 acts as a probe for glucocorticoid receptors and is used in isotope tracing studies .
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- HY-19822S2
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Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
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- HY-14806S1
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Teneligliptin-d4 is deuterium labeled Teneligliptin. Teneligliptin (MP-513) is a potent, orally available, competitive, and long-lasting DPP-4 inhibitor. Teneligliptin competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
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- HY-19822S
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Elacestrant-d4 (RAD1901-d4) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo.
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- HY-19822S3
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Elacestrant-d6 (RAD1901-d6) is deuterated labeled Elacestrant (HY-19822) Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo.
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- HY-13011S
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Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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- HY-13011S1
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Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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- HY-111372S
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Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease .
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- HY-13010S
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Laquinimod-d5 (ABR-215062-d5) is deuterium labeled Laquinimod. Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research .
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- HY-12678S1
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Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
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- HY-151829
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Azide
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Fmoc-L-Asn(EDA-N3)-OH is a click chemistry reagent containing an azide group. This building block is reported in literature for the modification of Amanitin via Click Chemistry. Alpha-Amanitin is the deadliest member of the amatoxin peptide family produced by the death-cap mushroom A. phalloides. It is an orally available, rigid, bicyclic octapeptide and one of the most lethal known natural products (LD50 = 50-100 μg/kg) acting as highly selective allosteric inhibitor of the RNA polymerase II .
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