Search Result
Results for "Atr atm dna pk drug Inhibitors" in MCE Product Catalog:
1751
Inhibitors & Agonists
10
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-11006
-
|
KU-57788
NU7441
|
DNA-PK
CRISPR/Cas9
|
Cancer
|
|
KU-57788 is a potent and selective inhibitor of DNA-PK with an IC50 of 13 nM, with selectivity over a range of kinases including mTOR, PI 3-K, ATM and ATR.
|
-
- HY-12016
-
|
KU-55933
|
ATM/ATR
Autophagy
|
Cancer
|
|
KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
|
-
- HY-136270
-
|
ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-100948
-
|
ATM-3507
|
Myosin
|
Cancer
|
|
ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.
|
-
- HY-U00447
-
-
- HY-100948B
-
-
- HY-128784
-
|
PK11007
|
MDM-2/p53
Reactive Oxygen Species
|
Cancer
|
|
PK11007 is a mild thiol alkylator with anticancer activity. PK11007 stabilizes p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.
|
-
- HY-18650
-
|
KU 59403
|
ATM/ATR
|
Cancer
|
|
KU 59403 is a potent ATM inhibitor, with IC50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively.
|
-
- HY-112614
-
|
ATM Inhibitor-1
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.
|
-
- HY-111451
-
|
ATR inhibitor 1
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 µΜ.
|
-
- HY-15520
-
-
- HY-100346
-
|
PK14105
|
Others
|
Others
|
|
PK14105 is a biological evaluation as a potential radioligand for PET studies of PBBS receptors.
|
-
- HY-13902
-
|
Berzosertib
VE-822; VX-970
|
ATM/ATR
|
Cancer
|
|
Berzosertib (VE-822) is an ATR inhibitor with a Ki value of less than 0.2 nM. It also inhibits ATM with a Ki of 34 nM.
|
-
- HY-100140A
-
-
- HY-128348
-
|
PK68
|
RIP kinase
|
Cancer
Inflammation/Immunology
|
|
PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and with great potential for use in the treatment of inflammatory disorders and cancer metastasis.
|
-
- HY-100140
-
-
- HY-133119
-
|
PK150
|
Bacterial
|
Infection
|
|
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 µM, respectively.
|
-
- HY-128897
-
-
- HY-16705
-
|
BRD4770
|
Histone Methyltransferase
|
Cancer
|
|
BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence.
|
-
- HY-13816
-
|
NU6027
|
CDK
ATM/ATR
|
Cancer
|
|
NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.
|
-
- HY-128917
-
-
- HY-109517
-
-
- HY-103241
-
|
Ro 90-7501
|
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Cancer
Neurological Disease
|
|
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
|
-
- HY-19567
-
|
PK 11195
RP 52028
|
Parasite
|
Infection
|
|
PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.
|
-
- HY-128729
-
|
DNA2 inhibitor C5
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
|
-
- HY-112197
-
-
- HY-17394
-
-
- HY-15586
-
|
L67
dna Ligase Inhibitor
|
DNA/RNA Synthesis
|
Cancer
|
|
L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.
|
-
- HY-100016
-
|
AZD0156
|
ATM/ATR
Apoptosis
|
Cancer
|
|
AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis.
|
-
- HY-B0211
-
-
- HY-B0097
-
|
Floxuridine
5-Fluorouracil 2'-deoxyriboside
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
|
Cancer
Infection
|
|
Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.
|
-
- HY-19939S
-
-
- HY-12030
-
|
PIK-90
|
PI3K
DNA-PK
|
Cancer
|
|
PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
|
-
- HY-117389
-
|
Homocarbonyltopsentin
pk4C9
|
Others
|
Others
|
|
Homocarbonyltopsentin (PK4C9) is a small-molecule TSL2-binding compound, binds to pentaloop conformations of TSL2 and promotes a shift to triloop conformations that display enhanced SMN2 exon 7 (E7) splicing with EC50 value of 16 μM.
|
-
- HY-B0211A
-
-
- HY-111783
-
-
- HY-U00439
-
-
- HY-101667
-
|
LTURM34
|
DNA-PK
|
Cancer
|
|
LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.
|
-
- HY-13431
-
|
KU-0060648
|
DNA-PK
PI3K
mTOR
|
Cancer
|
|
KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively.
|
-
- HY-19341
-
|
Compound 401
|
DNA-PK
|
Cancer
|
|
Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
|
-
- HY-101570B
-
|
(Rac)-Nedisertib
(Rac)-M3814
|
DNA-PK
|
Cancer
|
|
(Rac)-Nedisertib ((Rac)-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of <3 nM.
|
-
- HY-112305
-
|
AZ32
|
ATM/ATR
|
Cancer
|
|
AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell.
|
-
- HY-101570A
-
|
(R)-Nedisertib
(R)-M3814
|
DNA-PK
|
Cancer
|
|
(R)-Nedisertib ((R)-M3814) is a less active R-enantiomer of Nedisertib, with an IC50 in the range of 7-30 nM for DNA-PK.
|
-
- HY-101570
-
|
Nedisertib
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-19939S2
-
|
(R)-VX-984
(R)-M9831
|
Others
|
Others
|
|
(R)-VX-984 ((R)-M9831) is the (R)-enantiomer of VX-984. VX-984 is a potent DNA-PK inhibitor.
|
-
- HY-15719
-
|
NU 7026
LY293646
|
DNA-PK
Apoptosis
|
Cancer
|
|
NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
|
-
- HY-101427
-
-
- HY-136292
-
|
MC-PBD
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-PBD consists a non-cleavable ADC linker MC and a cytotoxic DNA crosslinking pyrrolobenzodiazepine (PBD). MC-PBD can be used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-U00279
-
|
Nitracrine
|
DNA/RNA Synthesis
|
Cancer
|
|
Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor drug. Nitracrine has cytotoxicity towards most cells.
|
-
- HY-101162
-
-
- HY-13281
-
|
PIK-75 hydrochloride
|
DNA-PK
PI3K
Apoptosis
|
Cancer
|
|
PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
|
-
- HY-12513
-
|
Samotolisib
LY3023414
|
PI3K
DNA-PK
mTOR
Autophagy
|
Cancer
|
|
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations.
|
-
- HY-107834
-
|
PIK-75
|
DNA-PK
PI3K
Apoptosis
|
Cancer
|
|
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
|
-
- HY-19323A
-
|
(S)-Ceralasertib
(S)-AZD6738
|
ATM/ATR
|
Cancer
|
|
(S)-Ceralasertib ((S)-AZD6738) is extracted from patent WO2011154737A1, Compound II, exhibits an IC50 of 2.578 nM.
(S)-Ceralasertib is a potent and selective sulfoximine morpholinopyrimidine ATR inhibitor with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics.
(S)-Ceralasertib is developed improving aqueous solubility and eliminates CYP3A4 time-dependent inhibition.
|
-
- HY-17565A
-
-
- HY-16962A
-
|
CC-115 hydrochloride
|
DNA-PK
mTOR
|
Cancer
|
|
CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
|
-
- HY-16962
-
|
CC-115
|
DNA-PK
mTOR
|
Cancer
|
|
CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
|
-
- HY-10108
-
|
LY294002
|
PI3K
Casein Kinase
DNA-PK
Autophagy
Apoptosis
|
Cancer
Infection
|
|
LY294002 (NSC 697286; SF 1101) is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
|
-
- HY-101146
-
-
- HY-19323
-
|
Ceralasertib
AZD6738
|
ATM/ATR
|
Cancer
|
|
Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC50 of 1 nM.
|
-
- HY-12061
-
-
- HY-135122
-
-
- HY-B0077
-
|
Bendamustine hydrochloride
SDX-105
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
|
Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties.
|
-
- HY-N1150
-
|
Thymidine
DThyd; NSC 21548
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Others
|
|
Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
|
-
- HY-135146
-
-
- HY-126490
-
|
Phleomycin
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Phleomycin is a wide-spectrum glycopeptide antibiotic found in Streptomyces verticillus. Phleomycin, an effective DNA-cleaving agent, binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A).
|
-
- HY-13567
-
|
Bendamustine
SDX-105 free base
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
|
Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activats DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
|
-
- HY-B0208S
-
|
Methimazole D3
|
Others
|
Endocrinology
|
|
Methimazole D3 is a deuterium labeled Methimazole. Methimazole is an antithyroid drug used for the treatment of the hyperthyroidism in humans and animals.
|
-
- HY-15521
-
-
- HY-128337
-
|
AN7973
|
Parasite
|
Infection
|
|
AN7973 is the 6-carboxamide benzoxaborole, blocks intracellular parasite development and inhibits Cryptosporidium growth. AN7973 is orally active, possesses favorable safety, stability, and PK parameters, and is an exciting drug candidate for treating cryptosporidiosis.
|
-
- HY-111308
-
-
- HY-100399
-
|
Nevanimibe
PD-132301; Atr-101
|
Acyltransferase
Apoptosis
|
Cancer
|
|
Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
|
-
- HY-14731
-
|
VE-821
|
ATM/ATR
|
Cancer
|
|
VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
|
-
- HY-B1953
-
|
Thiacloprid
|
Parasite
|
Infection
|
|
Thiacloprid, a chloronicotinyl insecticide, is targeted chiefly to control aphid pest species in orchards and vegetables. Thiacloprid destabilizes DNA. Thiacloprid changes the structure and stability of DNA through binding into the minor groove by hydrophobic or hydrogen interactions.
|
-
- HY-69014
-
-
- HY-101566A
-
-
- HY-101566
-
|
BAY-1895344
|
ATM/ATR
|
Cancer
|
|
BAY-1895344 is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity.
|
-
- HY-126678
-
|
Dimethyl-SGD-1882
Dimethyl-PBD dimer
|
ADC Cytotoxin
|
Cancer
|
|
Dimethyl-SGD-1882 (Dimethyl-PBD dimer) is a highly potent DNA alkylator, and is used as an antibody-drug conjugate (ADC) cytotoxin. PBD Dimer is a DNA alkylator which inhibits DNA replication.
|
-
- HY-136291
-
|
Sulfo-SPDB-DGN462
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Sulfo-SPDB-DGN462 is a drug-linker conjugate for ADC. Sulfo-SPDB-DGN462 consists a toxin DGN462 (HY-101150) conjugated to the cleavable Sulfo-SPDB linker. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML).
|
-
- HY-109566
-
-
- HY-100628A
-
-
- HY-15559
-
|
Hoechst 33342
bisBenzimide H 33342; HOE 33342
|
Autophagy
|
Others
|
|
Hoechst 33342 is a DNA minor groove binder used fluorochrome for visualizing cellular DNA.
|
-
- HY-N2150
-
|
Psammaplin A
|
HDAC
DNA Methyltransferase
DNA/RNA Synthesis
Bacterial
|
Cancer
Infection
|
|
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
|
-
- HY-N7066
-
|
Difloxacin hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
|
Difloxacin hydrochloride is a broad-spectrum antibacterial drug. Difloxacin hydrochloride inhibits bacterial DNA gyrase and exhibits a concentration-dependant bactericidal effect by interference with the activity of DNA gyrase and topoisomerase IV.
|
-
- HY-N6880
-
|
Rabdosiin
(+)-Rabdosiin
|
Others
|
Infection
Inflammation/Immunology
|
|
Rabdosiin is a tetramer of caffeic acid isolated from the stem of Rabdosia japonica Hara. Rabdosiin possess anti-allergic activity, anti-HIV activity and inhibition on DNA topoisomerase.
|
-
- HY-126781
-
|
Fozivudine tidoxil
BM-211290
|
HIV
DNA/RNA Synthesis
|
Infection
|
|
Fozivudine tidoxil (BM-211290) is an orally active thioether lipid-zidovudine (ZDV) conjugate with anti-HIV activity. Fozivudine tidoxil, a member of the NRTI family of drug, is incorporated into the newly synthesized strand of DNA during intracellular viral replication and irreversibly binds viral RT which disrupts viral reverse-transcription.
|
-
- HY-130407
-
|
Lipoamido-PEG3-OH
|
PROTAC Linker
|
Cancer
|
|
Lipoamido-PEG3-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Lipoamido-PEG3-OH (compound TA-TEG-G2CN) can be used in the formation of a highly stable, dendronized gold nanoparticle (AuNP)-based drug delivery platform.
|
-
- HY-13002
-
|
Torin 2
|
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
|
Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
|
-
- HY-15557
-
|
AZ20
|
ATM/ATR
|
Cancer
|
|
AZ20 is a potent and selective inhibitor of ATR with an IC50 of 5 nM, and has 8-fold selectivity against mTOR (IC50=38 nM).
|
-
- HY-15583
-
-
- HY-B0639
-
|
Amifostine
WR2721
|
Others
|
Cancer
|
|
Amifostine is a broad-spectrum cytoprotection agent against the DNA damaging effects of ionizing radiation and chemotherapy drug.
|
-
- HY-130083
-
-
- HY-122493
-
-
- HY-136219
-
|
Protein kinase affinity probe 1
|
Others
|
Others
|
|
Protein kinase affinity probe 1 is a novel protein kinase affinity probe for the functional identification of protein kinases (PKs). Protein kinase affinity probe 1 is a modified Purvalanol B (HY-18299) probe with 50% beads loading (Compound S3).
|
-
- HY-123637
-
-
- HY-N0465
-
|
Olaquindox
|
Bacterial
|
Infection
|
|
Olaquindox, a quinoxalin derivative, is an orally active antibiotic veterinary drug. Olaquindox stimulates growth and decreases intestinal mucosal immunity of piglets.
|
-
- HY-119964
-
|
Cetaben
|
Others
|
Cardiovascular Disease
|
|
Cetaben is a PPARα-independent peroxisome proliferator. Cetaben is a non-fibrate hypolipidemic drug and potently reduces the concentration of cholesterol and triglycerides.
|
-
- HY-19829
-
|
Sandramycin
|
ADC Cytotoxin
Bacterial
Antibiotic
|
Cancer
Infection
|
|
Sandramycin ia a cyclic depsipeptide antibiotic isolated from cultured broth of a Nocardioides sp. Sandramycin is also a DNA intercalator that potently binds DNA and is an ADC cytotoxin. Sandramycin is active against Gram-positive bacteria and has potent antitumor activity.
|
-
- HY-128952
-
-
- HY-17381
-
-
- HY-128873
-
-
- HY-107770
-
-
- HY-18987
-
-
- HY-135124
-
|
DC44SMe
|
ADC Cytotoxin
|
Cancer
|
|
DC44SMe, a phosphate prodrug of cytotoxic DNA alkylator DC44, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC44SMe exhibits IC50s of 2.0 nM, 2.8 nM, and 1.9 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC44SMe can be used for the targeted treatment of cancer.
|
-
- HY-135123
-
|
DC4SMe
|
ADC Cytotoxin
|
Cancer
|
|
DC4SMe, a phosphate prodrug of cytotoxic DNA alkylator DC4, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4SMe exhibits IC50s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer.
|
-
- HY-136170
-
|
MC-SN38
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-SN38 is a drug-linker conjugate composed of a potent microtubule-disrupting agent SN38 and a non-cleavable MC linker to make antibody drug conjugate (ADC). SN-38, an active metabolite of the Topoisomerase I inhibitor Irinotecan, inhibits DNA synthesis and causes frequent DNA single-strand breaks.
|
-
- HY-113056A
-
|
N1-Acetylspermidine hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamine. N1-acetylspermine is the substrate for the polyamine oxidase (PAO). N1-Acetylspermidine hydrochloride selectively elevates its level in human colorectal adenocarcinomas. N1-acetylspermidine shows cleavage efficiency at apurinic sites in DNA.
|
-
- HY-106579
-
|
Tiaprofenic acid
|
COX
|
Inflammation/Immunology
|
|
Tiaprofenic acid is an orally active nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic potency. Tiaprofenic acid inhibits prostaglandin synthesis by suppressing cyclo-oxygenase (COX). Tiaprofenic acid can be used in the treatment of rheumatic diseases.
|
-
- HY-18944
-
|
FIT-039
|
CDK
HSV
CMV
DNA/RNA Synthesis
|
Infection
|
|
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
|
-
- HY-122590
-
|
Glabrescione B
|
Gli
|
Cancer
|
|
Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.
|
-
- HY-D1020
-
-
- HY-131005
-
-
- HY-129356A
-
-
- HY-136548
-
|
Tenofovir diphosphate
TFV-DP
|
Reverse Transcriptase
|
|
|
Tenofovir diphosphate (TFV-DP) is a competitive DNA polymerases inhibitor (with respect to dATP) and a substrate of HIV type 1 (HIV-1) reverse transcriptase (RT).
|
-
- HY-15559A
-
-
- HY-123390
-
|
DB07107
|
Bcr-Abl
Akt
|
Cancer
|
|
DB07107 is a potent drug resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
|
-
- HY-10115
-
|
PI-103
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
|
PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
|
-
- HY-10115A
-
|
PI-103 Hydrochloride
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
|
PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
|
-
- HY-130801
-
-
- HY-12892
-
|
SKI-178
|
SPHK
Apoptosis
|
Cancer
|
|
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
|
-
- HY-15560
-
-
- HY-N0925
-
|
Tetrahydroberberine
Canadine
|
Dopamine Receptor
|
Neurological Disease
|
|
Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).
|
-
- HY-135218
-
|
AV-153
|
DNA/RNA Synthesis
|
Cancer
|
|
AV-153, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 has anti-cancer activity.
|
-
- HY-15560B
-
-
- HY-B0069
-
-
- HY-17438
-
|
Cidofovir
GS 0504; HPMPC; (S)-HPMPC
|
CMV
|
Infection
Cancer
|
|
Cidofovir is an anti-CMV drug which can suppress CMV replication by selective inhibition of viral DNA polymerase and therefore prevention of viral replication and transcription.
|
-
- HY-100399A
-
|
Nevanimibe hydrochloride
PD-132301 hydrochloride; Atr101 hydrochloride
|
Acyltransferase
Apoptosis
|
Cancer
|
|
Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.
|
-
- HY-110137A
-
|
Furamidine
DB75; NSC 305831
|
Parasite
Histone Methyltransferase
|
Cancer
Infection
Inflammation/Immunology
|
|
Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively).
|
-
- HY-130802
-
|
5-Aminouridine
|
Fungal
Influenza Virus
|
Cancer
Infection
|
|
5-Aminouridine can modify nucleobases and can be incorporated into the target DNA. 5-Aminouridine exhibits a wide range of biological activity and it inhibits the growth of tumors, fungi and viruses.
|
-
- HY-113303
-
-
- HY-123032
-
|
Sorivudine
BV-araU
|
DNA/RNA Synthesis
|
Infection
|
|
Sorivudine (BV-araU) is an orally active synthetic pyrimidine nucleoside antimetabolite drug. Sorivudine derives its antiviral activity from selective conversion by a specific thymidine kinase present in certain DNA viruses to nucleotides, which can in turn interfere with viral DNA synthesis.
|
-
- HY-11002
-
|
CP-466722
|
ATM/ATR
|
Cancer
|
|
CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 4.1 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
|
-
- HY-128959
-
-
- HY-A0061
-
-
- HY-N3797A
-
|
Echitamine chloride
|
Apoptosis
|
Cancer
|
|
Echitamine chloride is the major monoterpene indole alkaloid present in Alstonia with potent anti-tumour activity. Echitamine chloride induces DNA fragmentation and cells apoptosis. Echitamine chloride inhibits pancreatic lipase with an IC50 of 10.92 µM.
|
-
- HY-18061
-
|
Ochromycinone
(Rac)-STA-21
|
STAT
Bacterial
|
Cancer
Infection
|
|
Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity.
|
-
- HY-100564
-
|
2',3'-cGAMP
2'-3'-cyclic GMP-AMP
|
Endogenous Metabolite
STING
IFNAR
|
Metabolic Disease
|
|
2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP is produced in mammalian cells in response to DNA in the cytoplasm.
|
-
- HY-100564A
-
|
2',3'-cGAMP sodium
2'-3'-cyclic GMP-AMP sodium
|
Endogenous Metabolite
STING
IFNAR
|
Metabolic Disease
|
|
2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP sodium binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP sodium is produced in mammalian cells in response to DNA in the cytoplasm.
|
-
- HY-135218A
-
|
AV-153 free base
|
DNA/RNA Synthesis
|
Cancer
|
|
AV-153 free base, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 free base intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 free base interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 free base has anti-cancer activity.
|
-
- HY-N3023
-
|
3,4-Dihydroxybenzylamine hydrobromide
NSC 263475 hydrobromide
|
DNA/RNA Synthesis
|
Cancer
|
|
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.
|
-
- HY-135797
-
|
DB1976
|
Apoptosis
|
Cancer
|
|
DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 has apoptosis-inducing effect.
|
-
- HY-B0398
-
|
Nalidixic acid
|
Bacterial
Antibiotic
Topoisomerase
|
Infection
|
|
Nalidixic acid, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria.
|
-
- HY-B0398A
-
|
Nalidixic acid sodium salt
|
Bacterial
Antibiotic
Topoisomerase
|
Infection
|
|
Nalidixic acid sodium salt, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria.
|
-
- HY-124179
-
|
IT-901
|
NF-κB
|
Cancer
|
|
IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 µM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD).
|
-
- HY-13543
-
|
Tretazicar
CB 1954
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).
|
-
- HY-121879
-
-
- HY-B1057S2
-
|
Nefopam D3
Fenazoxine D3
|
β-catenin
|
Neurological Disease
|
|
Nefopam D3 (Fenazoxine D3) is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells.
|
-
- HY-135797A
-
|
DB1976 hydrochloride
|
Apoptosis
|
Cancer
|
|
DB1976 hydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 hydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 hydrochloride has apoptosis-inducing effect.
|
-
- HY-19743
-
-
- HY-127039
-
-
- HY-127034
-
-
- HY-50936
-
|
Trabectedin
Ecteinascidin 743; ET-743
|
Reactive Oxygen Species
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Trabectedin (Ecteinascidin 743; ET-743) a tetrahydroisoquinoline alkaloid with potent antitumor activity isolated from Ecteinascidia turbinata. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment.
|
-
- HY-128957
-
-
- HY-N0181A
-
|
Lumisterol
9β,10α-Ergosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
|
-
- HY-136559
-
-
- HY-105019A
-
|
Melflufen hydrochloride
Melphalan flufenamide hydrochloride
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
|
Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
|
-
- HY-105019
-
|
Melflufen
Melphalan flufenamide
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
|
Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells.
|
-
- HY-12457
-
|
Rachelmycin
CC-1065; NSC 298223
|
Antibiotic
|
Cancer
Infection
|
|
Rachelmycin (CC-1065; NSC 298223) is a potent naturally antibiotic isolated from Streptomyces zelensis. Rachelmycin binds non-covalently and covalently (N-3 adenine adduct) in the minor groove of B-form DNA. Rachelmycin has exceptionally potent antitumor activity.
|
-
- HY-112899
-
-
- HY-114233
-
-
- HY-13631D
-
|
Dxd
Exatecan derivative for ADC
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
|
-
- HY-128915
-
|
Duocarmycin
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Duocarmycin is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity. Duocarmycin is a DNA minor groove binding alkylating agent and explored as drug–antibody conjugates (ADCs) .
|
-
- HY-119970
-
|
Helenalin
|
NF-κB
|
Cancer
Inflammation/Immunology
|
|
Helenalin is an anti-inflammatory sesquiterpene lactone. Helenalin selectively inhibits transcription factor NF-κB by directly targeting p65. Helenalin has alkylating activity, targets the cysteine sulfhydryl groups in the p65 subunit of NF-κB, thereby inhibits its DNA binding.
|
-
- HY-123604A
-
|
TH1834 dihydrochloride
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
|
-
- HY-15900
-
|
Voxtalisib
XL765; SAR245409
|
PI3K
mTOR
|
Cancer
|
|
Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
|
-
- HY-119757
-
|
Tyrphostin AG1433
SU1433; AG1433
|
PDGFR
VEGFR
|
Cancer
|
|
Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.
|
-
- HY-101150
-
|
DGN462
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-128880
-
-
- HY-136289
-
-
- HY-128881
-
-
- HY-128909
-
-
- HY-123604
-
|
TH1834
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
|
-
- HY-14519
-
|
Methotrexate
Amethopterin; CL14377; WR19039
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
|
-
- HY-10372
-
-
- HY-U00433A
-
-
- HY-136319
-
-
- HY-14519A
-
|
Methotrexate disodium
Amethopterin disodium; CL14377 disodium; WR19039 disodium
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
|
-
- HY-N1306
-
|
Sideroxylin
|
Bacterial
Reactive Oxygen Species
Apoptosis
|
Cancer
Infection
|
|
Sideroxylin is a C-methylated flavone isolated from Callistemon lanceolatus and exerts antimicrobial activity against Staphylococcus aureus. Sideroxylin inhibits ovarian cancer cell proliferation and induces apoptosis, causing DNA fragmentation, depolarization of the mitochondrial membrane, the generation of reactive oxygen species (ROS).
|
-
- HY-10619B
-
|
Niraparib tosylate
MK-4827 tosylate
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-19373
-
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-106014
-
|
Tezacitabine
|
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment.
|
-
- HY-128904
-
-
- HY-131085
-
-
- HY-10619
-
|
Niraparib
MK-4827
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-10619A
-
|
Niraparib hydrochloride
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
|
-
- HY-13580
-
|
Budesonide
|
Glucocorticoid Receptor
|
Cancer
Inflammation/Immunology
|
|
Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.
|
-
- HY-15044
-
|
NU1025
|
PARP
|
Cancer
Neurological Disease
|
|
NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity.
|
-
- HY-13703A
-
-
- HY-109654
-
|
Ensulizole
|
Others
|
Metabolic Disease
|
|
Ensulizole is a sulfonated UV absorber and can intense UVB and partial UVA absorption. Ensulizole can damage the DNA through the generation of reactive oxygen species (ROS) upon UV or sunlight irradiation. Ensulizole is a water soluble sunscreen ingredient.
|
-
- HY-126327
-
|
UNC4976
|
Histone Methyltransferase
|
Cancer
|
|
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
|
-
- HY-12246
-
|
XEN445
|
Others
|
Cardiovascular Disease
|
|
XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
|
-
- HY-135775
-
|
BMVC
|
G-quadruplex
Telomerase
DNA/RNA Synthesis
|
Cancer
|
|
BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities.
|
-
- HY-125018
-
|
QM31
SVT016426
|
Caspase
|
Cancer
|
|
QM31 (SVT016426), a cytoprotective agent, is a selective inhibitor of Apaf-1. QM31 inhibits the formation of the apoptosome (IC50=7.9μM), the caspase activation complex composed by Apaf-1, cytochrome c, dATP and caspase-9. QM31 exerts mitochondrioprotective functions and interferes with the intra-S-phase DNA damage checkpoint.
|
-
- HY-136297
-
|
DGN549-C
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
DGN549-C consists a cleavable ADC linker valine-alanine (va) and PBD dimer. DGN549 is a novel DNA-alkylating cytotoxic payload and can be used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-13753
-
-
- HY-B1002
-
-
- HY-U00439A
-
|
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-18353
-
|
mTOR inhibitor-3
|
mTOR
|
Cancer
|
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
- HY-W012037
-
|
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-131057
-
-
- HY-12342
-
|
ML216
CID-49852229
|
DNA/RNA Synthesis
|
Cancer
|
|
ML216 (CID-49852229) is a potent, selective and cell permeable inhibitor of the DNA unwinding activity of BLM helicase with IC50s of 2.98 μM and 0.97 μM for BLM full-length and BLM 636-1298, respectively. ML216 inhibits ssDNA-dependent ATPase activity of BLM with a Ki of 1.76 µM. Antitumor avtivity.
|
-
- HY-135900
-
|
Aniline-MPB-amino-C3-PBD
|
ADC Cytotoxin
Bacterial
|
Cancer
|
|
Aniline-MPB-amino-C3-PBD is a cytotoxic agent comprised non-alkylating group. Aniline-MPB-amino-C3-PBD is a sequence-selective DNA minor-groove binding agent. Aniline-MPB-amino-C3-PBD acts as the payload for ADCs. Antimicrobial activity.
|
-
- HY-113352
-
|
7-Methylguanine
|
Endogenous Metabolite
|
Others
|
|
7-Methylguanine is a metabolite of DNA methylation. It can be generated by methylating agents, and used as a probe of protein–DNA interactions and a key component of DNA sequencing method.
|
-
- HY-B0537A
-
|
Pentamidine dihydrochloride
MP-601205 dihydrochloride
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Cancer
Infection
|
|
Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-B0537
-
|
Pentamidine
MP-601205
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Cancer
Infection
|
|
Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-125331
-
|
DRF-1042
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.
|
-
- HY-135303
-
|
GLPG1205
|
GPR84
|
Inflammation/Immunology
|
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
|
-
- HY-B1355A
-
-
- HY-B0330A
-
-
- HY-13747
-
-
- HY-13811
-
|
NSC697923
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
|
-
- HY-16562
-
|
Irinotecan
(+)-Irinotecan; CPT-11
|
Topoisomerase
Autophagy
|
Cancer
|
|
Irinotecan is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
|
-
- HY-B0028
-
-
- HY-B0159
-
-
- HY-B0147A
-
|
Pefloxacin mesylate
Pefloxacinium mesylate
|
Bacterial
Antibiotic
|
Infection
|
|
Pefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)
Target: DNA gyrase
Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections.
|
-
- HY-B0147
-
|
Pefloxacin
Pefloxacinium
|
Bacterial
Antibiotic
|
Infection
|
|
Pefloxacin is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)
Target: DNA gyrase
Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections.
|
-
- HY-B0330
-
|
Levofloxacin
(-)-Ofloxacin
|
Bacterial
Antibiotic
|
Infection
|
|
Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
|
-
- HY-17565
-
-
- HY-10982
-
|
Amonafide
AS1413
|
Topoisomerase
|
Cancer
|
|
Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.
|
-
- HY-B0159A
-
-
- HY-B0537B
-
|
Pentamidine isethionate
MP-601205 isethionate
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-W033577
-
|
Tricarbonyldichlororuthenium(II) dimer
CORM-2
|
Others
|
Inflammation/Immunology
|
|
Tricarbonyldichlororuthenium(II) dimer is a pharmacological donor of CO releasing. CO releases from Tricarbonyldichlororuthenium(II) dimer prevents gastric mucosal oxidative damage induced by ischemia/reperfusion (I/R) improving gastric blood flow (GBF), decreasing DNA oxidation and inflammatory response on systemic level.
|
-
- HY-B0147B
-
|
Pefloxacin mesylate dihydrate
Pefloxacinium mesylate dihydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Pefloxacin mesylate dehydrate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)
Target: DNA gyrase
Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections.
|
-
- HY-A0098
-
|
Tunicamycin
|
Bacterial
Fungal
Influenza Virus
Antibiotic
|
Cancer
Infection
Inflammation/Immunology
|
|
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.
|
-
- HY-128036
-
|
ddATP
2',3'-Dideoxyadenosine 5'-triphosphate
|
DNA/RNA Synthesis
|
Infection
|
|
ddATP is a dideoxynucleotide, acts as a chain-elongating inhibitor of DNA polymerase, used for Sanger method for DNA sequencing.
|
-
- HY-118517
-
|
α-Hydroxytamoxifen
(E)-α-Hydroxy tamoxifen; α-OHTAM
|
Others
|
Cancer
|
|
α-Hydroxytamoxifen is a metabolite of tamoxifen, reacts with DNA in the absence of metabolizing enzymes, and causes formation of DNA adducts.
|
-
- HY-135813
-
|
LtaS-IN-1
|
Bacterial
|
Infection
|
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- HY-125957
-
|
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-107096
-
|
CH-0793076
TP3076
|
Topoisomerase
|
Cancer
|
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).
|
-
- HY-126973
-
|
BI-1230
|
HCV Protease
|
Infection
|
|
BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity.
|
-
- HY-A0004
-
|
Decitabine
5-Aza-2'-deoxycytidine; NSC 127716
|
DNA Methyltransferase
Apoptosis
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Decitabine (NSC 127716) is a deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
|
-
- HY-107845
-
|
SCR7 pyrazine
|
CRISPR/Cas9
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.
|
-
- HY-N2566
-
|
Euscaphic acid
|
DNA/RNA Synthesis
PI3K
Apoptosis
|
Cancer
|
|
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
|
-
- HY-114153
-
|
PLX5622
|
c-Fms
|
Neurological Disease
|
|
PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.
|
-
- HY-112669
-
-
- HY-16518
-
|
Voreloxin Hydrochloride
SNS-595 Hydrochloride; Vosaroxin Hydrochloride; AG 7352 Hydrochloride
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
|
-
- HY-19609
-
-
- HY-111183
-
-
- HY-17422
-
|
Acyclovir
Aciclovir; Acycloguanosine
|
HSV
Bacterial
Antibiotic
Apoptosis
|
Cancer
Infection
|
|
Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia.
|
-
- HY-117102
-
|
ANI-7
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
|
-
- HY-N0311
-
-
- HY-122727
-
|
STL127705
|
DNA-PK
|
Cancer
|
|
STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
|
-
- HY-15746
-
-
- HY-W006395
-
-
- HY-114153A
-
|
PLX5622 hemifumarate
|
c-Fms
|
Neurological Disease
|
|
PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
|
-
- HY-120118
-
|
Metarrestin
ML246
|
DNA/RNA Synthesis
|
Cancer
|
|
Metarrestin (ML246) disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis.
|
-
- HY-135960
-
|
BO-264
|
FGFR
Apoptosis
|
Cancer
|
|
BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity.
|
-
- HY-136648
-
-
- HY-135389
-
|
Desmethyl Levofloxacin
|
Drug Metabolite
|
Infection
|
|
Desmethyl Levofloxacin is a metabolite of Levofloxacin. Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
|
-
- HY-105935
-
|
Keracyanin chloride
Cyanidin 3-rutinoside chloride; Cyanidin 3-O-rutinoside chloride; Sambucin chloride
|
Others
|
Others
|
|
Keracyanin chloride (Cyanidin 3-rutinoside chloride), an anthocyanin, has antioxidant activity. Keracyanin chloride inhibits malonaldehyde formation in oxidized calf thymus DNA.
|
-
- HY-12742
-
|
SCR7
|
DNA/RNA Synthesis
CRISPR/Cas9
Apoptosis
|
Cancer
|
|
SCR7 is an unstable form that can be autocyclized into a stable form SCR7 pyrazine. SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity.
|
-
- HY-A0170
-
|
Trovafloxacin
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
|
-
- HY-103399
-
|
Trovafloxacin mesylate
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
|
-
- HY-14573
-
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-18728
-
-
- HY-135125
-
|
DC4
|
ADC Cytotoxin
|
Cancer
|
|
DC4, a ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4 can be used for the targeted treatment of cancer.
|
-
- HY-101647
-
-
- HY-128943
-
|
MAC glucuronide phenol-linked SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) drug linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.
|
-
- HY-B0879
-
-
- HY-13424
-
-
- HY-101400
-
-
- HY-136648A
-
-
- HY-W012078
-
-
- HY-123523
-
-
- HY-N1620
-
|
1-Cinnamoylpyrrolidine
|
Others
|
Cardiovascular Disease
|
|
1-Cinnamoylpyrrolidine (Compound 3), a crude extract prepared from Piper caninum, is a DNA strand scission agent, induces the relaxation of supercoiled pBR322 plasmid DNA.
1-Cinnamoylpyrrolidine (Compound 4) inhibits platelet aggregation induced by PAF with an IC50 of 37.3 μM.
|
-
- HY-10586
-
-
- HY-125276
-
|
TH5487
|
Others
|
Inflammation/Immunology
|
|
TH5487 is a potent 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC50 of 342 nM. TH5487 stops OGG1 from recognizing its DNA substrate, inhibits DNA repair and modifies OGG1 chromatin dynamics, which results in the inhibition of proinflammatory pathway genes.
|
-
- HY-17393
-
-
- HY-13605
-
-
- HY-10534
-
|
Voreloxin
SNS-595; Vosaroxin; AG 7352
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
|
-
- HY-13605A
-
-
- HY-12484
-
|
BMH-21
|
DNA/RNA Synthesis
|
Cancer
|
|
BMH-21 is a small molecule DNA intercalator that binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription; does not cause phosphorylation of H2AX.
|
-
- HY-126321
-
|
RORγt agonist 1
|
ROR
|
Cancer
|
|
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy.
|
-
- HY-B0879A
-
|
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-17371
-
|
Oxaliplatin
|
DNA Alkylator/Crosslinker
Autophagy
|
Cancer
|
|
Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
|
-
- HY-107999
-
|
CADD522
|
Others
|
Cancer
|
|
CADD522 is a potent inhibitor of runt-related transcription factor-2 (RUNX2)-DNA binding with an IC50 of 10 nM. CADD522 exhibits antitumor activity.
|
-
- HY-13567S
-
|
Bendamustine D4
SDX-105 D4 free base
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Bendamustine D4 (SDX-105 D4 free base) is the deuterium labeled Bendamustine. Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
|
-
- HY-100951
-
-
- HY-17574
-
-
- HY-18174A
-
|
Prexasertib dihydrochloride
LY2606368 dihydrochloride
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity.
|
-
- HY-18174B
-
|
Prexasertib Mesylate Hydrate
LY2606368 Mesylate Hydrate; LY2940930
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.
|
-
- HY-18174
-
|
Prexasertib
LY2606368
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.
|
-
- HY-112081
-
|
BAY-707
|
DNA/RNA Synthesis
|
Cancer
|
|
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy.
|
-
- HY-15552
-
-
- HY-13727
-
-
- HY-112060
-
-
- HY-111375
-
-
- HY-16560
-
-
- HY-10206
-
|
Amuvatinib
MP470; Hpk 56
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
Apoptosis
|
Cancer
|
|
Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
|
-
- HY-10206A
-
|
Amuvatinib hydrochloride
MP470 hydrochloride; Hpk 56 hydrochloride
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
|
Cancer
|
|
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
|
-
- HY-128946
-
|
CL2A-SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
Inflammation/Immunology
|
|
CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
|
-
- HY-18174E
-
|
Prexasertib dimesylate
LY2606368 dimesylate
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
|
-
- HY-12344
-
|
UNC2025
|
FLT3
|
Cancer
|
|
UNC2025 is a potent and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.
|
-
- 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 prodrug 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-12344A
-
|
UNC2025 hydrochloride
|
FLT3
|
Cancer
|
|
UNC2025 hydrochloride is a potent and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.
|
-
- HY-B0313
-
-
- HY-13669
-
-
- HY-13700
-
-
- HY-13727A
-
-
- HY-14798
-
-
- HY-13585
-
-
- HY-129938
-
-
- HY-12455
-
|
Duocarmycin A
|
ADC Cytotoxin
Apoptosis
Caspase
|
Cancer
|
|
Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels.
|
-
- HY-13744
-
|
Rubitecan
RFS 2000; 9-Nitrocamptothecin
|
Topoisomerase
|
Cancer
|
|
Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
|
-
- HY-112898
-
|
DC1SMe
|
ADC Cytotoxin
|
Cancer
|
|
DC1Sme, a DC1 derivative, exhibits IC50 values of 22 pM, 10 pM, 32 pM and 250 pM for Ramos, Namalwa, HL60/s and COLO 205 cancer cells, respectively. DC1, an analogue of the minor groove-binding DNA alkylator CC-1065, is a ADC Cytotoxin. DC1 can be used in synthesis of antibody-drug conjugates for the targeted treatment of cancer.
|
-
- HY-19977
-
|
YU238259
|
DNA-PK
|
Cancer
|
|
YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
|
-
- HY-A0005
-
-
- HY-15753
-
-
- HY-B0126
-
-
- HY-15753A
-
-
- HY-U00337
-
-
- HY-B0126A
-
-
- HY-107769
-
-
- HY-122470
-
|
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-W002585
-
|
O6-Benzylguanine
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity.
|
-
- HY-129355
-
-
- HY-13758
-
-
- HY-13758A
-
-
- HY-133234
-
|
BMVC-8C3O
|
G-quadruplex
|
Others
|
|
BMVC-8C3O is a DNA G-quadruplexe (G4) ligand which can induce topological conversion of non-parallel to parallel forms in human telomeric DNA G4s.
|
-
- HY-128760
-
|
COH34
|
Others
|
Cancer
|
|
COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors.
|
-
- HY-109052
-
|
Atabecestat
JNJ-54861911
|
Beta-secretase
|
Neurological Disease
|
|
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat (JNJ-54861911) is tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment.
|
-
- HY-14776
-
|
Quarfloxin
CX-3543
|
DNA/RNA Synthesis
|
Cancer
|
|
Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template.
|
-
- HY-16513
-
-
- HY-129356
-
-
- HY-W040329
-
-
- HY-16496
-
-
- HY-13618
-
|
Edotecarin
J 107088; PF 804950
|
Topoisomerase
|
Cancer
|
|
Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
|
-
- HY-N6828
-
-
- HY-129379
-
|
DC0-NH2
|
ADC Cytotoxin
|
Cancer
|
|
DC0-NH2 is an effector moiety for ADC and a simplified analog of DC1 with better stability. DC0-NH2 is about 1000-fold more cytotoxic than commonly used anticancer drugs (ex. Doxorubicin). DC0-NH2 can bind to the minor groove of DNA, followed by alkylation of adenine residues by its propabenzindole (CBI) component.
|
-
- HY-126350
-
|
CL2-SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor. The anti-Trop-2 hRS7-CL2A-SN-38 ADC provides significant and specific antitumor effects against a range of human solid tumor types.
|
-
- HY-19826
-
-
- HY-W009109
-
-
- HY-17025
-
|
Rifabutin
Ansamycin; LM-427
|
Bacterial
Antibiotic
|
Infection
|
|
Rifabutin (Ansamycin) is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits DNA-dependent RNA polymerase.
|
-
- HY-15588
-
-
- HY-B0125
-
-
- HY-11007
-
|
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-113306
-
-
- HY-16261B
-
-
- HY-112680A
-
-
- HY-16261A
-
-
- HY-100549
-
|
(S)-Crizotinib
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
(S)-Crizotinib is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models.
|
-
- HY-15233
-
|
Letermovir
AIC246
|
CMV
|
Infection
|
|
Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
|
-
- HY-13631
-
|
Exatecan
DX-8951
|
Topoisomerase
|
Cancer
|
|
Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
|
-
- HY-13631A
-
-
- HY-N4321
-
|
Glucotropaeolin potassium
Benzylglucosinolate potassium
|
Others
|
Others
|
|
Glucotropaeolin potassium (Benzylglucosinolate potassium) , a glucosinolate contained in cruciferous vegetables, causes a moderate decrease in spontaneous DNA damage in animals.
|
-
- HY-13420
-
-
- HY-13562A
-
-
- HY-101127
-
|
SGD-1882
PBD dimer
|
ADC Cytotoxin
|
Cancer
|
|
SGD-1882 is a cytotoxic, DNA minor-groove crosslinking agent pyrrolobenzodiazepine (PBD) dimer, acting as the payload for ADCs.
|
-
- HY-B0497B
-
-
- HY-N6733
-
|
Aphidicolin
|
DNA/RNA Synthesis
HSV
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering with the activity of DNA polymerase.
Aphidicolin is an antibiotic produced by the mold Cephalosporium aphidicola. Aphidicolin is a potent inhibitor of cellular deoxyribonucleic acid synthesis and inhibits the growth of herpes simplex virus.
Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line.
|
-
- HY-U00248
-
|
LMP744
MJ-III65; NSC706744
|
Topoisomerase
|
Cancer
|
|
LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
|
-
- HY-107004A
-
-
- HY-13551
-
|
Amsacrine
m-AMSA; acridinyl anisidide
|
Topoisomerase
Autophagy
|
Cancer
|
|
Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
|
-
- HY-N0739
-
|
Betaine hydrochloride
Betaine chloride
|
Others
|
Others
|
|
Betaine hydrochloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
|
-
- HY-131102
-
-
- HY-13551A
-
|
Amsacrine hydrochloride
m-AMSA hydrochloride; acridinyl anisidide hydrochloride
|
Topoisomerase
Autophagy
|
Cancer
|
|
Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
|
-
- HY-U00248A
-
|
LMP744 hydrochloride
MJ-III65 hydrochloride; NSC706744 hydrochloride
|
Topoisomerase
|
Cancer
|
|
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
|
-
- HY-12747
-
-
- HY-16700
-
|
PNU-159682
|
ADC Cytotoxin
|
Cancer
|
|
PNU-159682, a highly potent metabolite of the anthracycline nemorubicin (DNA topoisomerase II inhibitor) with outstanding cytotoxicity, is a potent ADCs cytotoxin.
|
-
- HY-12746
-
-
- HY-B1079
-
-
- HY-109056
-
|
Elsulfavirine
|
HIV
|
Infection
|
|
Elsulfavirine is a reverse transcriptase inhibitors for HIV-1 infection and is a new anti-HIV drug.
|
-
- HY-100358
-
-
- HY-114750
-
-
- HY-B1124
-
-
- HY-17554
-
|
(R)-Oxiracetam
(R)-(+)-Oxiracetam
|
Others
|
Neurological Disease
|
|
(R)-Oxiracetam is the (R)-enantiomer of the nootropic drug oxiracetam. Oxiracetam (ISF 2522) is a nootropic drug of the racetam family and stimulant.
|
-
- HY-17364
-
|
Temozolomide
NSC 362856; CCRG 81045; TMZ
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
|
-
- HY-W040129
-
|
Chromomycin A3
|
Bacterial
Fungal
Antibiotic
|
Cancer
Infection
|
|
Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg 2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor.
|
-
- HY-119372
-
-
- HY-N2033
-
-
- HY-15910
-
|
5-BrdU
5-Bromo-2'-deoxyuridine; BrDU; BUdR
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
5-BrdU is a nucleoside analog that competes with thymidine for incorporation into DNA. 5-BrdU is commonly used in the detection of proliferating cells.
|
-
- HY-N0629
-
-
- HY-14808
-
|
Adarotene
ST1926
|
Apoptosis
|
Cancer
|
|
Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.
|
-
- HY-15457
-
-
- HY-N7452
-
-
- HY-N6954
-
|
Garcinone C
|
ATM/ATR
STAT
CDK
|
Cancer
|
|
Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia Champ that is used as an anti-inflammatory, analgesia, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner.
|
-
- HY-128962
-
-
- HY-N6809
-
-
- HY-117482
-
|
BPN-15606
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
|
-
- HY-122198
-
|
ML367
|
Others
|
Cancer
|
|
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
|
-
- HY-A0077AS
-
-
- HY-18714
-
|
BRD7116
|
Others
|
Others
|
|
BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity.
|
-
- HY-15349
-
|
Trovirdine
LY300046
|
HIV
|
Infection
|
|
Trovirdine inhibits HIV-1 RT with an IC50 of 7 nM when employing heteropolymeric primer/template (oligo-DNA/ribosomal RNA)and dGTP as substrate.
|
-
- HY-B0546
-
-
- HY-B1777
-
-
- HY-111806
-
-
- HY-16637
-
-
- HY-136649
-
-
- HY-14714
-
-
- HY-B0546A
-
-
- HY-128916
-
|
dmDNA31
|
Bacterial
|
Infection
|
|
dmDNA31 is a rifamycin-class antibiotic that inhibits bacterial DNA-dependent RNA polymerase with potent bactericidal activity against S. aureus.
|
-
- HY-136110
-
-
- HY-17438A
-
|
Cidofovir dihydrate
HPMPC dihydrate; (S)-HPMPC dihydrate
|
CMV
|
Infection
|
|
Cidofovir dehydrate is an injectable antiviral medication for the treatment of cytomegalovirus (CMV) retinitis, which suppresses virus replication by selective inhibition of viral DNA synthesis.
|
-
- HY-17036
-
-
- HY-B1396
-
-
- HY-101660
-
-
- HY-101828
-
-
- HY-19440
-
-
- HY-100126
-
|
Tubercidin
7-Deazaadenosine
|
Bacterial
DNA/RNA Synthesis
Influenza Virus
Antibiotic
|
Infection
|
|
Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC50 of 0.02 μM. Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis. Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP. Tubercidin has antiviral activity.
|
-
- HY-15142
-
|
Doxorubicin hydrochloride
Hydroxydaunorubicin hydrochloride
|
Topoisomerase
ADC Cytotoxin
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Bacterial
Antibiotic
|
Cancer
Infection
|
|
Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy. Doxorubicin hydrochloride inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
|
-
- HY-130853
-
|
Thalidomide-NH-PEG2-C2-NH-Boc
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology.
|
-
- HY-12695B
-
-
- HY-122099
-
|
Riddelline
|
DNA/RNA Synthesis
|
Others
|
|
Riddelline, a pyrrolizidine alkaloid, is a potent genotoxic agent. Riddelline induces significant elevations in unscheduled DNA synthesis and S-phase synthesis in rat liver.
|
-
- HY-15229
-
|
Guadecitabine sodium
SGI-110 sodium; S-110 sodium
|
DNA Methyltransferase
|
Cancer
|
|
Guadecitabine sodium (SGI-110 sodium) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).
|
-
- HY-Y1055
-
-
- HY-13542
-
|
Guadecitabine
SGI-110
|
DNA Methyltransferase
|
Cancer
|
|
Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).
|
-
- HY-19770
-
|
GSK2981278
|
ROR
|
Inflammation/Immunology
|
|
GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
|
-
- HY-B0132A
-
|
Norfloxacin hydrochloride
MK-0366 hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
|
Norfloxacin hydrochloride (MK-0366 hydrochloride) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.
|
-
- HY-B0132
-
-
- HY-13701
-
-
- HY-B0947
-
-
- HY-B0402A
-
-
- HY-B0246
-
-
- HY-N0093
-
-
- HY-U00071
-
-
- HY-B0994
-
-
- HY-B1099
-
-
- HY-106634
-
|
Mitoguazone
Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
|
HIV
Apoptosis
|
Cancer
Infection
|
|
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.
|
-
- HY-136287
-
-
- HY-W015490
-
|
1,4-Naphthoquinone
|
Others
|
Cancer
|
|
1,4-Naphthoquinone is a potential pharmacophore for inhibition of both MAO (monoamine oxidase) and DNA topoisomerase activities, this latter associated with antitumor activity.
|
-
- HY-16667
-
|
HLM006474
|
Others
|
Cancer
|
|
HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
|
-
- HY-108261
-
|
Tomeglovir
BAY 38-4766
|
CMV
|
Infection
|
|
Tomeglovir is a potent anti-CMV agent, inhibiting processing of viral DNA-concatemers, with IC50s of 0.34 μM and 0.039 μM for HCMV and MCMV.
|
-
- HY-13668
-
-
- HY-N6046
-
-
- HY-W004924
-
|
5-Hydroxymethyluracil
|
Endogenous Metabolite
|
Others
|
|
5-Hydroxymethyluracil is a product of oxidative DNA damage. 5-Hydroxymethyluracil can be used as a potential epigenetic mark enhancing or inhibiting transcription with bacterial RNA polymerase.
|
-
- HY-14781
-
-
- HY-117482A
-
|
BPN-15606 besylate
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
|
-
- HY-19902
-
-
- HY-111606
-
-
- HY-120836
-
|
AOH1160
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells.
|
-
- HY-N6800A
-
|
Netropsin dihydrochloride
|
DNA/RNA Synthesis
Bacterial
Influenza Virus
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Netropsin (dihydrochloride) is a small-molecule MGB (minor-groove binder), inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei. Netropsin (dihydrochloride) has potential antibiotic and antiviral properties by binding to dsDNA in a non-intercalative manner, it improves survival from murine endotoxaemia by attenuating NOS2 induction through interference with HMGA1 DNA binding to the core NOS2 promoter. Netropsin (dihydrochloride) in solutions of DNA has radioprotective ability against radiation-induced damage due to its high binding affinity and high structural stabilization, hydroxyl radical (OH*) generated by ionizing radiation cannot radiolyse the netropsin-DNA complex.
|
-
- HY-136650
-
-
- HY-13767
-
|
Tirapazamine
SR259075; SR4233; Win59075
|
Others
|
Cancer
|
|
Tirapazamine is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death.
|
-
- HY-10074
-
-
- HY-112754A
-
|
DOTAP chloride
1,2-Dioleoyl-3-trimethylammonium-propane chloride
|
Others
|
Others
|
|
DOTAP chloride is a useful and effective cationic lipid for transient and stable transfection DNA (plasmids, bacmids) and modified nucleic acids (antisense oligonucleotides) with out the use of helper lipid.
|
-
- HY-N7225
-
|
Yuanhuacine
Gnidilatidin
|
Others
|
Cancer
|
|
Yuanhuacine (Gnidilatidin), a daphnane diterpenoid from the flowers of Daphne genkwa with extensive anti-tumor activity. Yuanhuacine is a DNA-damaging agent with orally active.
|
-
- HY-W010450
-
-
- HY-100139
-
-
- HY-B0338A
-
-
- HY-B0252
-
-
- HY-B0089
-
-
- HY-B1118
-
-
- HY-B0379A
-
-
- HY-B1137
-
-
- HY-101751
-
-
- HY-101829
-
-
- HY-B1442
-
-
- HY-14290A
-
-
- HY-B2087
-
-
- HY-128960
-
-
- HY-U00241
-
|
Carburazepam
RGH 3331; Uxepam
|
GABA Receptor
|
Neurological Disease
|
|
Carburazepam is a drug which derives from benzodiazepine. Benzodiazepines (BZD, BZs) are a class of psychoactive drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring.
|
-
- HY-135660
-
-
- HY-N7025
-
-
- HY-N6701
-
|
Dihydrocytochalasin B
|
Arp2/3 Complex
|
Cancer
|
|
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport. Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis. Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca 2+increase in the mucosal scrapings.
|
-
- HY-128930
-
-
- HY-101954
-
|
Inarigivir
ORI-9020; SB-9000
|
HBV
|
Infection
|
|
Inarigivir (ORI-9020;SB-9000) is a dinucleotide which can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus.
|
-
- HY-B1318
-
|
Foscarnet sodium
Trisodium phosphonoformate; Phosphonoformic acid trisodium salt
|
Virus Protease
DNA/RNA Synthesis
|
Infection
|
|
Foscarnet sodium (Trisodium phosphonoformate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet sodium is an antiherpesvirus agent used in cytomegalovirus retinitis.
|
-
- HY-18258
-
-
- HY-B0963
-
-
- HY-100262
-
-
- HY-U00101
-
-
- HY-B1407
-
-
- HY-B0338
-
-
- HY-B0803
-
-
- HY-B0989
-
|
Carzenide
4-Sulfamoylbenzoic acid
|
Others
|
Others
|
|
Carzenide is an organic synthesis intermediate, for synthetic drug.
|
-
- HY-U00274
-
-
- HY-100146
-
-
- HY-B0416
-
-
- HY-101714
-
-
- HY-B1047
-
-
- HY-B0578
-
-
- HY-13859
-
-
- HY-B0921
-
-
- HY-B0089A
-
-
- HY-101748
-
-
- HY-101603
-
-
- HY-101670
-
-
- HY-B1245
-
-
- HY-B0766
-
-
- HY-N2897
-
-
- HY-136286
-
-
- HY-103236
-
|
NSC232003
|
E1/E2/E3 Enzyme
|
Cancer
|
|
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
|
-
- HY-14771A
-
-
- HY-112901
-
|
DC41
|
ADC Cytotoxin
|
Cancer
|
|
DC41 is a DC1 derivative. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.
|
-
- HY-100690
-
|
NSC16168
|
Others
|
Cancer
|
|
NSC16168 is a specific inhibitor of ERCC1-XPF, with an IC50 value of 0.42 μM. NSC16168 inhibits DNA repair and potentiates CDDP efficacy in cancer.
|
-
- HY-N3308
-
|
Medicarpin
|
Apoptosis
|
Cancer
|
|
Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of drugs.
|
-
- HY-115066
-
-
- HY-W011819
-
|
Tetradecanedioic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Tetradecanedioic acid is an endogenous metabolite and belongs to the class of organic compounds known as long-chain fatty acids. Tetradecanedioic acid can act as a candidate biomarker for organic anion-transporting polypeptide mediated drug-drug interactions .
|
-
- HY-A0057
-
-
- HY-B1015
-
-
- HY-17490
-
-
- HY-12769
-
-
- HY-B1086
-
-
- HY-A0057A
-
-
- HY-B0343A
-
-
- HY-B1346
-
-
- HY-10821
-
-
- HY-B0357
-
-
- HY-U00403
-
-
- HY-B0380A
-
-
- HY-B0380
-
-
- HY-126664
-
-
- HY-17581
-
-
- HY-108316
-
-
- HY-U00055
-
-
- HY-U00025
-
-
- HY-115066A
-
-
- HY-100599
-
-
- HY-13062A
-
-
- HY-B2028
-
|
Propargite
|
Parasite
|
Infection
|
|
Propargite is a pesticide used to kill mites. Propargite induces β-cell necrosis preceded by DNA damage. Propargite induces MIN6 cell death with an IC50 of 1 μM.
|
-
- HY-50735
-
|
Fiacitabine
NSC 382097; FIAC; FOAC
|
HSV
|
Infection
|
|
Fiacitabine(NSC 382097; FIAC; FOAC) is a selective inhibitior of DNA replication of herpes simplex virus(HSV) with IC50 values of 2.5 nM and 12.6 nM for HSV1 and HSV2, respectively.
|
-
- HY-13062
-
-
- HY-W002272
-
|
Isocytosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
Isocytosine is a non-natural nucleobase and an isomer of cytosine. It is used in combination with Isoguanine in studies of unnatural nucleic acid analogues of the normal base pairs in DNA and used as a nucleobase of hachimoji RNA.
|
-
- HY-135336
-
|
(R)-Verapamil hydrochloride
(R)-(+)-Verapamil hydrochloride
|
P-glycoprotein
Apoptosis
|
Cancer
|
|
(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
|
-
- HY-128954
-
-
- HY-107798
-
|
Potassium guaiacolsulfonate hemihydrate
|
Bacterial
|
Infection
|
|
Potassium guaiacolsulfonate hemihydrate is an orally active expectorant used for acute respiratory tract infections. Potassium guaiacolsulfonate hemihydrate helps loosen mucus and used for a cough caused by the common cold, infections or allergies in combination with other drugs.
|
-
- HY-17449
-
|
Fosbretabulin disodium
CA 4DP; CA 4P; Combretastatin A4 disodium phosphate
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.
|
-
- HY-B1016
-
-
- HY-B0401
-
-
- HY-100150
-
-
- HY-B0336
-
-
- HY-B0012A
-
-
- HY-B0523A
-
-
- HY-12770
-
-
- HY-16398
-
-
- HY-B1382
-
-
- HY-100572
-
-
- HY-13682
-
-
- HY-B0405A
-
-
- HY-B1074
-
-
- HY-N0118
-
-
- HY-107433
-
-
- HY-16445A
-
-
- HY-G0010
-
-
- HY-B0301
-
-
- HY-101472
-
|
Closthioamide
|
Bacterial
|
Infection
|
|
Closthioamide is a potent inhibitor of bacterial DNA gyrase and highly active against Ec, MRSA, VRE and Mv), with MICs of 9.00 μM, 0.58 μM, 0.58 μM and 72.03 μM respectively.
|
-
- HY-107790
-
|
5-Methoxyflavone
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
|
-
- HY-W015892
-
|
γ-Hexalactone
|
Others
|
Others
|
|
γ-Hexalactone is a gamma-lactone found in ripe fruits. γ-Hexalactone induces DNA damage and acts a substrate of paraoxonase 1 (PON1).
|
-
- HY-17577
-
-
- HY-16293
-
-
- HY-12512
-
|
cGAMP
Cyclic GMP-AMP; 3',3'-cGAMP
|
STING
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMP; 3',3'-cGAMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.
|
-
- HY-19825
-
|
Rebeccamycin
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.
|
-
- HY-111746
-
|
CWHM-1008
|
Parasite
|
Infection
|
|
CWHM-1008 is a potent and orally active antimalarial agent, with EC50 values of 46 and 21 nM against drug-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains, respectively.
|
-
- HY-135325
-
-
- HY-101070
-
-
- HY-112951
-
|
ChX710
|
STING
|
Cancer
|
|
ChX710 could prime the type I interferon response to cytosolic DNA, which induces the ISRE promoter sequence, specific cellular Interferon-Stimulated Genes (ISGs), and the phosphorylation of Interferon Regulatory Factor (IRF) 3.
|
-
- HY-13562S
-
|
Banoxantrone D12
AQ4N D12
|
Topoisomerase
|
Cancer
|
|
Banoxantrone D12 (AQ4N D12) is the deuterium labeled banoxantrone. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
|
-
- HY-13562AS
-
|
Banoxantrone D12 dihydrochloride
AQ4N D12 dihydrochloride
|
Topoisomerase
|
Cancer
|
|
Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) is the deuterium labeled banoxantrone dihydrochloride. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
|
-
- HY-111617
-
|
BTR-1
|
Apoptosis
|
Cancer
|
|
BTR-1 is an active anti-cancer agent, causes S phase arrest, and affects DNA replication in leukemic cells. BTR-1 activates apoptosis and induces cell death.
|
-
- HY-15750
-
-
- HY-17437A
-
-
- HY-B0421
-
-
- HY-15581
-
-
- HY-B0803S
-
-
- HY-B1138
-
-
- HY-12771
-
-
- HY-B0779
-
-
- HY-B1177
-
|
Crotamiton
|
Parasite
|
Infection
|
|
Crotamiton is a drug that is used both as a scabicidal (for treating scabies) and as a general antipruritic.
|
-
- HY-B0012
-
-
- HY-130107
-
-
- HY-B2102
-
|
Oxyphenisatine
Oxyphenisatin
|
Others
|
Cancer
|
|
Oxyphenisatine (Oxyphenisatin) is a laxative. Oxyphenisatin acetate is the pro-drug of oxyphenisatin with anticancer activity.
|
-
- HY-B1287
-
-
- HY-A0293
-
|
Pyrvinium pamoate
Pyrvinium embonate
|
Wnt
|
Cancer
|
|
Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
|
-
- HY-B0507A
-
-
- HY-129365
-
|
SNPB
|
ADC Linker
|
Cancer
|
|
SNPB is a cleavable linker that is used for making antibody-drug conjugate (ADC).
|
-
- HY-15374
-
-
- HY-101710
-
-
- HY-B0634
-
-
- HY-B0703
-
-
- HY-121817
-
-
- HY-135846
-
|
PDD00031705
|
Others
|
Cancer
|
|
PDD00031705 is a benzimidazolone core cell-inactive inhibitor of Poly (ADP-ribose) glycohydrolase (PARG).
|
-
- HY-125098
-
-
- HY-101033
-
|
GPR35 agonist 1
|
Others
|
Cancer
Endocrinology
|
|
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
|
-
- HY-103504
-
-
- HY-W010737
-
-
- HY-N2217
-
-
- HY-14771
-
-
- HY-13704
-
|
SN-38
NK012
|
Topoisomerase
ADC Cytotoxin
Autophagy
|
Cancer
|
|
SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
|
-
- HY-111320
-
|
Chrysomycin B
|
Bacterial
Antibiotic
|
|
|
Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
|
-
- HY-N0716B
-
-
- HY-B2087S
-
-
- HY-B2087S1
-
-
- HY-42146
-
|
BMPS
|
ADC Linker
|
Cancer
|
|
BMPS is a nonclaevable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-129376
-
-
- HY-B1185
-
|
Beclamide
N-Benzyl-3-chloropropionamide
|
Others
|
Neurological Disease
|
|
Beclamide is a drug that possesses anticonvulsant activity, has been used as a sedative and as an anticonvulsant.
|
-
- HY-B0083
-
|
Leflunomide
HWA486; RS-34821; SU101
|
Others
|
Cancer
|
|
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
|
-
- HY-B0505
-
-
- HY-109111
-
-
- HY-19318
-
-
- HY-16216
-
-
- HY-15856B
-
-
- HY-B0801S
-
-
- HY-B0992
-
-
- HY-N0666
-
-
- HY-B1196
-
-
- HY-17484
-
-
- HY-100875
-
-
- HY-B0557
-
-
- HY-14187
-
-
- HY-17594
-
|
Oxyclozanide
|
Parasite
|
Infection
|
|
Oxyclozanide is a salicylanilide anthelmintic drug that mainly acts by uncoupling oxidative phosphorylation in flukes.
|
-
- HY-U00073
-
|
Benin
Butocin; Butocine
|
Others
|
Cancer
|
|
Benin is a potent cytostatic drug that can be used for the treatment of generalized carcinoma of the breast.
|
-
- HY-19839
-
-
- HY-14188
-
-
- HY-B0270
-
-
- HY-17475
-
-
- HY-B0024
-
-
- HY-B1115
-
-
- HY-B0223
-
-
- HY-B1236
-
-
- HY-B0806S
-
-
- HY-126519
-
-
- HY-136288
-
-
- HY-106235
-
|
LB80317
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
LB80317 is an active metabolite of LB80380 and suppresses the DNA synthesis of HBV with an EC50 of 0.5 μM. LB80317 has antiviral effect and has the potential for chronic hepatitis B treatment.
|
-
- HY-N0769
-
-
- HY-50071
-
-
- HY-B1516
-
|
3'-Fluoro-3'-deoxythymidine
Alovudine
|
Others
|
Cancer
|
|
3'-Fluoro-3'-deoxythymidine (Alovudine) is a marker of DNA synthesis that is less susceptible to inflammatory changes than 18F-Fluorodeoxyglucose (FDG) and thus is a better biomarker in pancreatic cancer.
|
-
- HY-131343
-
|
HBV-IN-4
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.
|
-
- HY-13629
-
-
- HY-D1070
-
|
DBCO-PEG4-TAMRA
|
Others
|
Others
|
|
DBCO-PEG4-TAMRA is a PEG-based TARMA dye and contains a DBCO group, which enables Click Chemistry. The TAMRA dye is a dye widely used in oligonucleotide labeling and automated DNA sequencing applications.
|
-
- HY-13962
-
-
- HY-B0482
-
|
Acemetacin
TVX 1322
|
COX
|
Inflammation/Immunology
|
|
Acemetacin (TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
|
-
- HY-B0101B
-
-
- HY-B0101A
-
-
- HY-129366
-
|
PDB-Pfp
|
ADC Linker
|
Cancer
|
|
PDB-Pfp is a reducible ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-B1279
-
-
- HY-B0682A
-
-
- HY-B1223
-
-
- HY-U00414
-
-
- HY-129375
-
-
- HY-44235
-
-
- HY-129373
-
-
- HY-B0284
-
-
- HY-B0101
-
-
- HY-B1011
-
|
Edoxudine
EUDR
|
Bacterial
|
Infection
|
|
Edoxudine is an antiviral drug, is an analog of thymidine, shows effectiveness against herpes simplex virus.
|
-
- HY-16397A
-
-
- HY-17361
-
-
- HY-17425
-
-
- HY-B0920
-
-
- HY-126667
-
-
- HY-B0778
-
-
- HY-17425A
-
-
- HY-100265
-
-
- HY-12684
-
|
CH-223191
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR).
CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
|
-
- HY-B0497
-
|
Niclosamide
BAY2353
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
|
Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
|
-
- HY-128346
-
|
PQM130
|
Amyloid-β
|
Neurological Disease
|
|
PQM130, a Feruloyl-Donepezil Hybrid compound with brain penatration, is a multitarget drug candidate against the neurotoxicity induced by Aβ1-42 oligomer (AβO) and shows anti-inflammatory activity. PQM130 acts as a neuroprotective compound for anti-AD drug development.
|
-
- HY-14881
-
|
Bedaquiline
TMC207; R207910
|
Bacterial
Antibiotic
|
Infection
|
|
Bedaquiline (TMC207) is a diarylquinoline drug and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-drug resistant tuberculosis.
|
-
- HY-118716
-
|
PhIP
|
Others
|
Cancer
|
|
PhIP is the most abundant of generation of heterocyclic amines (HCA), resulted in the cooking of meat. DNA damaging and mutagenic activities. PhIP also has oestrogenic activity that could contribute to its tissue specific carcinogenicity.
|
-
- HY-136251
-
|
BRD0539
|
CRISPR/Cas9
|
Infection
|
|
BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.
|
-
- HY-108640
-
|
HLI373
|
MDM-2/p53
Parasite
Apoptosis
|
Cancer
Infection
|
|
HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
|
-
- HY-130515
-
|
Cdc7-IN-3
|
CDK
|
Cancer
|
|
Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-108640A
-
|
HLI373 dihydrochloride
|
MDM-2/p53
Parasite
Apoptosis
|
Cancer
Infection
|
|
HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
|
-
- HY-100758
-
|
FUBP1–IN-1
|
Others
|
Cancer
|
|
FUBP1–IN-1 is a potent FUSE binding protein 1 (FUBP1) inhibitor which interferes with the binding of FUBP1 to its single stranded target DNA FUSE sequence , with an IC50 value of 11.0 μM.
|
-
- HY-B2194
-
-
- HY-N6576
-
|
Hellebrigenin
|
Apoptosis
|
Cancer
|
|
Hellebrigenin, one of bufadienolides belonging to cardioactive steroids, is isolated from traditional Chinese medicine Venenum Bufonis. Hellebrigenin induces DNA damage and cell cycle G2/M arrest. Hellebrigenin triggers mitochondria-mediated apoptosis.
|
-
- HY-126498
-
-
- HY-129369
-
|
SPDMB
|
ADC Linker
|
Cancer
|
|
SPDMB is a glutathione cleavable ADC linker used for the antibody-drug conjugate (ADCs).
|
-
- HY-12448
-
|
SPDB
|
ADC Linker
|
Cancer
|
|
SPDB is a glutathione cleavable ADC linker used for the antibody-drug conjugate (ADCs).
|
-
- HY-17625
-
-
- HY-129368
-
|
SPDMV
|
ADC Linker
|
Cancer
|
|
SPDMV is a glutathione cleavable ADC linker used for the antibody-drug conjugate (ADCs).
|
-
- HY-19376
-
|
NAMI-A
|
FAK
|
Cancer
|
|
NAMI-A is a ruthenium-based drug characterised by the selective activity against tumour metastases, inhibits the adhesion and migration.
|
-
- HY-14946
-
|
Amifampridine
3,4-Diaminopyridine
|
Others
|
Others
|
|
Amifampridine (3,4-Diaminopyridine) is a drug, predominantly in the treatment of a number of rare muscle diseases.
|
-
- HY-B0373
-
|
Tiopronin
|
Others
|
Metabolic Disease
|
|
Tiopronin is a prescription thiol drug used to control the rate of cystine precipitation and excretion in the disease cystinuria.
|
-
- HY-104004
-
-
- HY-126511
-
-
- HY-17426
-
|
Famciclovir
BRL 42810
|
HSV
|
Infection
|
|
Famciclovir(BRL 42810) is a guanine analogue antiviral drug used for the treatment of various herpesvirus infections.
|
-
- HY-B0124A
-
-
- HY-126530
-
-
- HY-19017
-
-
- HY-B0530
-
-
- HY-133540
-
-
- HY-B1048
-
|
Pasiniazid
Paraniazide; Pasiniazide; Isonicotinic acid hydrazide p-aminosalicylate
|
Others
|
Inflammation/Immunology
|
|
Pasiniazid is an anti-TB and anti-leprosy drug, used to treat various types of TB and leprosy.
|
-
- HY-B0481
-
|
Miglitol
BAY1099; BAY-m1099
|
Others
|
Metabolic Disease
|
|
Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose.
|
-
- HY-126512
-
-
- HY-B0174
-
-
- HY-B0391
-
-
- HY-B1033
-
-
- HY-129370
-
-
- HY-B1104
-
-
- HY-100379
-
-
- HY-128927
-
-
- HY-10932
-
-
- HY-111354
-
-
- HY-101810
-
-
- HY-78961
-
-
- HY-B2141
-
-
- HY-B0124
-
-
- HY-112822
-
|
ON-013100
|
CDK
|
Cancer
|
|
ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
|
-
- HY-B0277
-
-
- HY-12930
-
|
SPR719
VXc-486
|
Topoisomerase
Bacterial
|
Infection
|
|
SPR719 (VXc-486) is a gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively.
|
-
- HY-100513A
-
|
Dehydroaltenusin
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM).
Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis.
Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
|
-
- HY-N6865
-
|
Groenlandicine
|
Topoisomerase
|
Cancer
Metabolic Disease
|
|
Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR). Groenlandicine selectively induces topoisomerase I-mediated DNA cleavage.
|
-
- HY-130516
-
|
Cdc7-IN-4
|
CDK
|
Cancer
|
|
Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-117650A
-
|
RG7834
RO 7020322
|
HBV
|
Infection
|
|
RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells.
|
-
- HY-106101
-
|
Echinomycin
Quinomycin A; NSC-13502
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
|
-
- HY-111756
-
|
BLM-IN-1
|
Apoptosis
|
Cancer
|
|
BLM-IN-1 (compound 29) is an effective Bloom syndrome protein (BLM) inhibitor, with a strong BLM binding KD of 1.81 μM and an IC50 of 0.95 μM for BLM. Induces DNA damage response, as well as apoptosis and proliferation arrest in cancer cells.
|
-
- HY-130517
-
|
Cdc7-IN-5
|
CDK
|
Cancer
|
|
Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-130519
-
|
Cdc7-IN-7
|
CDK
|
Cancer
|
|
Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-128920
-
|
Phortress free base
|
Cytochrome P450
|
Cancer
|
|
Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
|
-
- HY-N2342
-
|
Procyanidin C1
|
Apoptosis
|
Cancer
|
|
Procyanidin C1 is a natural polyphenol, causes DNA damage, cell cycle arrest, and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells.
|
-
- HY-111646
-
-
- HY-135967
-
|
MTH1-IN-2
|
DNA/RNA Synthesis
|
Cancer
|
|
MTH1-IN-2 is a MutT homolog 1 (MTH1) inhibitor extracted from patent WO2016135138A1, Compound (6), MTH1-IN-2 can be used for the research of cancer. Anti-tumor activity.
|
-
- HY-P2312
-
|
Human β-defensin-3
HβD-3
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC90 values of 6-25 μg/ml.
|
-
- HY-136095
-
-
- HY-130111
-
-
- HY-B0306
-
-
- HY-B0139
-
-
- HY-41919
-
-
- HY-140014
-
|
Val-Cit
|
ADC Linker
|
Cancer
|
|
Val-Cit is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-B0965
-
-
- HY-101151
-
-
- HY-100561
-
|
Tempol
4-Hydroxy-TEMPO
|
Autophagy
|
Cancer
|
|
Tempol is a general superoxide dismutase (SOD)-mimetic drug that efficiently neutralizes reactive oxygen species (ROS).
|
-
- HY-128970
-
-
- HY-116270
-
-
- HY-17006
-
-
- HY-G0001A
-
-
- HY-126349
-
-
- HY-140098
-
-
- HY-129353
-
-
- HY-14655
-
-
- HY-126496
-
-
- HY-76772A
-
-
- HY-129367
-
-
- HY-B1895
-
-
- HY-14895
-
-
- HY-118759
-
-
- HY-42973
-
-
- HY-133550
-
-
- HY-18237
-
|
KX1-004
|
Src
|
Others
|
|
KX1-004 is a potent small molecule inhibitor of Src-PTK as a potential protective drug for NIHL.
|
-
- HY-126405
-
|
SMPT
|
ADC Linker
|
Cancer
|
|
SMPT is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-B0367
-
-
- HY-129352
-
-
- HY-15255
-
|
Zosuquidar
LY335979
|
P-glycoprotein
|
Cancer
|
|
Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
|
-
- HY-133542
-
-
- HY-17509
-
-
- HY-A0142A
-
-
- HY-117050
-
-
- HY-126531
-
-
- HY-76210
-
-
- HY-136104
-
-
- HY-B0808S
-
-
- HY-W000423
-
-
- HY-W071006
-
|
PPC-NHS ester
2,5-Dioxopyrrolidin-1-yl 3-(pyridin-2-yldisulfanyl)butanoate
|
ADC Linker
|
Cancer
|
|
PPC-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-133543
-
-
- HY-20560
-
-
- HY-126295
-
-
- HY-114697
-
-
- HY-119602
-
-
- HY-76772B
-
-
- HY-B0568
-
-
- HY-B1613A
-
-
- HY-122872
-
|
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- HY-16261
-
|
Aldoxorubicin
INNO-206; DOXO-EMCH
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
|
-
- HY-N6725
-
-
- HY-109045
-
|
Teslexivir
BTA074; AP 611074
|
Others
|
Infection
|
|
Teslexivir (BTA074; AP 611074) is a topical antiviral agent that is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an interaction that is a necessary step for Human Papilloma Virus (HPV) 6 and 11 DNA replication and thus viral production.
|
-
- HY-135336S
-
|
(R)-Verapamil D7 hydrochloride
(R)-(+)-Verapamil D7 hydrochloride
|
P-glycoprotein
Apoptosis
|
Cancer
|
|
(R)-Verapamil D7 hydrochloride ((R)-(+)-Verapamil D7 hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs.
|
-
- HY-112853
-
-
- HY-136033
-
-
- HY-140987
-
-
- HY-140313
-
-
- HY-130110
-
-
- HY-140306
-
-
- HY-W019543
-
-
- HY-23641
-
-
- HY-B1080
-
-
- HY-140105
-
-
- HY-B0735
-
-
- HY-141158
-
-
- HY-136031
-
-
- HY-140100
-
-
- HY-W008772
-
-
- HY-13995A
-
|
Sevelamer hydrochloride
|
FXR
Autophagy
|
Others
|
|
Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
|
-
- HY-140296
-
-
- HY-U00148
-
-
- HY-130099
-
-
- HY-135973
-
-
- HY-136032
-
-
- HY-135978
-
-
- HY-135972
-
-
- HY-41189
-
-
- HY-140096
-
-
- HY-126851
-
-
- HY-B0735A
-
-
- HY-B0017
-
|
Telbivudine
Epavudine; L-Thymidine; NV 02B
|
HBV
|
Infection
|
|
Telbivudine, a specific inhibitor of hepatitis B virus (HBV) replication, is an antiviral drug used in the treatment of hepatitis B infection.
|
-
- HY-130928
-
-
- HY-N0666C
-
-
- HY-B0206
-
-
- HY-116063
-
-
- HY-128929
-
-
- HY-44221
-
-
- HY-140122
-
-
- HY-135418
-
-
- HY-123687
-
-
- HY-140104
-
-
- HY-B0967
-
|
Phthalylsulfacetamide
|
Bacterial
|
Infection
|
|
Phthalylsulfacetamide is a sulfa drug, after oral administration, slowly decompose in the intestine,and release sulfacetamide ,generating antibacterial effect.
|
-
- HY-129360
-
-
- HY-17579
-
-
- HY-17583
-
-
- HY-U00402
-
-
- HY-B2177
-
|
Apronal
Allylisopropylacetylurea; Apronalide
|
Others
|
Neurological Disease
|
|
Apronal (Allylisopropylacetylurea, Apronalide) is a hypnotic and sedative drug that has been withdrawn in several countries due to side effects.
|
-
- HY-135977
-
-
- HY-131084
-
-
- HY-101596
-
-
- HY-12454
-
|
DM4
|
Microtubule/Tubulin
|
Cancer
|
|
DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
|
-
- HY-U00105
-
-
- HY-W011541
-
-
- HY-W002213
-
-
- HY-140129
-
-
- HY-13995
-
|
Sevelamer
|
FXR
Autophagy
|
Endocrinology
|
|
Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
|
-
- HY-W044078
-
-
- HY-136039
-
-
- HY-14603
-
-
- HY-N6779
-
|
Patulin
Terinin
|
Bacterial
Apoptosis
Antibiotic
|
Infection
|
|
Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin (Terinin) induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.
|
-
- HY-116954
-
|
Metribuzin
|
DNA/RNA Synthesis
|
Others
|
|
Metribuzin is a low-cost non-selective herbicide that belongs to the chemical class of triazinones. Metribuzin hinders DNA synthesis in treated plants and acts on photosystem II, ultimately inhibiting photosynthesis. Metribuzin provides good control of important annual grass and broad-leaf weeds.
|
-
- HY-N4058
-
|
Helichrysetin
|
Others
|
Cancer
|
|
Helichrysetin, isolated from the flowers of Helichrysum odoratissimum, is an ID2 (inhibitor of DNA binding 2) inhibitor, and suppresses DCIS (ductal carcinoma in situ) formation. Helichrysetin possess strong inhibitory effects on cell growth and is capable of inducing apoptosis in A549 cells.
|
-
- HY-126241
-
|
RV01
|
Aldehyde Dehydrogenase (ALDH)
|
Inflammation/Immunology
|
|
RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.
|
-
- HY-N0716
-
-
- HY-135731
-
|
4-Methylamino antipyrine
|
COX
Drug Metabolite
|
Inflammation/Immunology
|
|
4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.
|
-
- HY-135731A
-
|
4-Methylamino antipyrine hydrochloride
|
COX
Drug Metabolite
|
Inflammation/Immunology
|
|
4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine hydrochloride has analgesic, antipyretic, and relatively weak antiinflammatory properties.
|
-
- HY-N0908
-
-
- HY-13945
-
|
NVP 231
|
Apoptosis
|
Cancer
|
|
NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
|
-
- HY-17647
-
|
Zoliflodacin
ETX0914; AZD0914
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus with the MIC90 of 0.25 μg/mL.
|
-
- HY-112902
-
|
OGG1-IN-08
|
Others
|
Inflammation/Immunology
|
|
OGG1-IN-08 is a potent 8-oxoguanine DNA glycosylase-1 (OGG1) inhibitor with an IC50 value of 0.22 μM. OGG1-IN-08 decreases both the glycosylase and lyase activities of OGG1.
|
-
- HY-18982
-
|
Anisomycin
Flagecidin; Wuningmeisu C
|
DNA/RNA Synthesis
JNK
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK. Anisomycin is a bacterial antibiotic isolated from Streptomyces griseolus.
|
-
- HY-19447A
-
|
Besifovir Dipivoxil maleate
LB80380 maleate
|
HBV
|
Infection
|
|
Besifovir Dipivoxil maleate (LB80380 maleate) is an oral prodrug of LB80317. Besifovir Dipivoxil maleate (LB80380 maleate) is effective in hepatitis B virus (HBV) DNA suppression for both treatment-naive and lamivudine-resistant chronic hepatitis B (CHB) patients in preliminary studies[2]
|
-
- HY-B0388
-
|
Probucol
DH-581
|
Virus Protease
|
Metabolic Disease
|
|
Probucol (DH-581) is an anti-hyperlipidemic drug by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
|
-
- HY-136138
-
-
- HY-15336
-
-
- HY-130112
-
-
- HY-13702
-
|
Nilutamide
Nilandron; RU 23908
|
Androgen Receptor
|
Cancer
|
|
Nilutamide (Nilandron) is a non-steroidal anti-androgen drug proposed in the treatment of metastatic prostatic carcinoma.
|
-
- HY-124329
-
-
- HY-B0022
-
|
Flutamide
SCH 13521
|
Androgen Receptor
|
Cancer
|
|
Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
|
-
- HY-130935
-
-
- HY-14895A
-
-
- HY-B1153A
-
-
- HY-101153
-
-
- HY-126364
-
-
- HY-140138
-
-
- HY-B1059
-
-
- HY-B1216
-
-
- HY-B0197A
-
-
- HY-20336
-
|
Mc-Val-Cit-PABC-PNP
Maleimidocaproyl-L-valine-L-citrulline-p-aminobenzyl alcohol p-nitrophenyl carbonate
|
ADC Linker
|
Cancer
|
|
Mc-Val-Cit-PABC-PNP is a cathepsin cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-136102
-
-
- HY-140102
-
-
- HY-W023121
-
-
- HY-B0193
-
-
- HY-141141
-
-
- HY-126524
-
-
- HY-140140
-
-
- HY-B0193A
-
-
- HY-130810
-
-
- HY-129362
-
-
- HY-B1114
-
|
Gliquidone
AR-DF 26
|
Others
|
Metabolic Disease
|
|
Gliquidone (AR-DF 26) is an anti-diabetic drug in the sulfonylurea class, used in the treatment of diabetes mellitus type 2.
|
-
- HY-42745
-
-
- HY-B2206
-
-
- HY-B0197
-
-
- HY-B0225
-
-
- HY-101634
-
|
ABT-072
|
HCV
|
Infection
|
|
ABT-072 is a nonnucleoside NS5B polymerase inhibitor and a candidate drug evaluated for treatment of hepatitis C virus.
|
-
- HY-B0256
-
-
- HY-129349
-
-
- HY-78738
-
-
- HY-W038702
-
-
- HY-104025
-
-
- HY-133504
-
-
- HY-114430
-
-
- HY-W001187
-
|
Tempo
|
DNA/RNA Synthesis
ROS
|
Cancer
|
|
Tempo is a classic nitroxide radical and is a selective scavenger of mitochondrial ROS that dismutases superoxide in the catalytic cycle. Tempo induces DNA-strand breakage. Tempo can be used as an organocatalyst for the oxidation of primary alcohols to aldehydes. Tempo has mutagenic and antioxidant effects.
|
-
- HY-W016420
-
|
Fosfomycin sodium
MK-0955 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Fosfomycin sodium (MK-0955 sodium) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-17592
-
|
Bithionol
|
Parasite
|
Cancer
|
|
Bithionol is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.
|
-
- HY-N0239
-
-
- HY-126353
-
-
- HY-44234
-
-
- HY-130089
-
-
- HY-130090
-
-
- HY-15742
-
-
- HY-140116
-
-
- HY-130937
-
-
- HY-100662
-
-
- HY-U00187
-
|
NCX1022
|
Others
|
Inflammation/Immunology
|
|
NCX1022 is an NO-releasing derivative of Hydrocortisone, which is the most widely used anti-inflammatory drug for the treatment of skin inflammation.
|
-
- HY-17398
-
-
- HY-133412
-
-
- HY-130936
-
-
- HY-141145
-
-
- HY-44222
-
-
- HY-17427
-
-
- HY-B0225B
-
-
- HY-130932
-
-
- HY-B0225A
-
-
- HY-I0447A
-
-
- HY-N4183
-
|
Licoflavone C
|
Others
|
Cancer
|
|
Licoflavone C is a prenyl-flavone extracted from Genista ephedroides, reduces the genotoxicity of cancer drugs in human peripheral lymphocytes.
|
-
- HY-136136
-
-
- HY-140118
-
-
- HY-B2060A
-
|
Tiamulin fumarate
Thiamutilin fumarate
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Tiamulin fumarate (Thiamutilin fumarate) is a diterpenic veterinary drug widely used in swine for the control of infectious diseases, including swine dysentery and enzootic pneumonia.
|
-
- HY-17573
-
|
Carbetocin
|
Oxytocin Receptor
|
Endocrinology
|
|
Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.
|
-
- HY-133413
-
-
- HY-15740
-
-
- HY-126533
-
-
- HY-141144
-
-
- HY-N3373
-
|
Loganetin
|
Bacterial
|
Infection
|
|
Loganetin is a non-toxic natural product that may be applied in the antibacterial drug development for treating multidrug-resistant Gram negative infections.
|
-
- HY-126513
-
-
- HY-126670
-
-
- HY-141142
-
-
- HY-130098
-
-
- HY-140117
-
-
- HY-130930
-
-
- HY-130088
-
-
- HY-131261
-
-
- HY-140120
-
-
- HY-A0091A
-
-
- HY-140125
-
-
- HY-112299
-
|
TAS6417
|
EGFR
|
Cancer
|
|
TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
|
-
- HY-136139
-
-
- HY-18706
-
-
- HY-106855
-
-
- HY-126497
-
-
- HY-126516
-
-
- HY-W011561
-
-
- HY-W008216
-
|
HMMNI
Hydroxy Dimetridazole
|
Drug Metabolite
|
Others
|
|
HMMNI (Hydroxy dimetridazole) is a hydroxy metabolite of Dimetridazole. Dimetridazole is a nitroimidazole class drug that combats protozoan infections.
|
-
- HY-136107
-
-
- HY-130383
-
-
- HY-41541
-
-
- HY-130386
-
-
- HY-126663
-
-
- HY-136329
-
-
- HY-130087
-
-
- HY-135975
-
-
- HY-130086
-
-
- HY-W071007
-
-
- HY-108556
-
|
RWJ-56110
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
|
-
- HY-108556A
-
|
RWJ-56110 dihydrochloride
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
|
-
- HY-W004520
-
|
Phenazine methylsulfate
5-Methylphenazinium methylsulfate
|
Bacterial
Antibiotic
Apoptosis
|
|
|
Phenazine methylsulfate is a free radical generator. Phenazine methylsulfate has been used as an electron transfer reactant in cell viability assays. Phenazine methylsulfate induces ssDNA break formation in the presence of the reducing agent NADPH. Phenazine methylsulfate induces oxidative DNA damage in an alkaline comet assay and apoptosis.
|
-
- HY-111558A
-
|
Bobcat339 hydrochloride
|
DNA Methyltransferase
|
Cancer
|
|
Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
|
-
- HY-W008091
-
|
5-Methylcytosine
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Others
|
|
5-Methylcytosine is a well-characterized DNA modification, and is also predominantly in abundant non-coding RNAs in both prokaryotes and eukaryotes. 5-Methylcytosine in mRNA is a new epitranscriptome marker inArabidopsis, and that regulation of this modification is an integral part of gene regulatory networks underlying plant development.
|
-
- HY-B0152A
-
|
Adenine hydrochloride
6-Aminopurine hydrochloride; Vitamin B4 hydrochloride
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Cancer
|
|
Adenine hydrochloride (6-Aminopurine hydrochloride) is a purine derivative with a variety of roles in biochemistry, including cellular respiration, in the form of both the energy-rich adenosine triphosphate (ATP) and the cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD), and protein synthesis, as a chemical component of DNA and RNA.
|
-
- HY-135780
-
-
- HY-111558
-
|
Bobcat339
|
DNA Methyltransferase
|
Cancer
|
|
Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription.
|
-
- HY-B0609
-
|
Fosfomycin tromethamine
MK-0955 tromethamine
|
Bacterial
Antibiotic
|
Infection
|
|
Fosfomycin tromethamine (MK-0955 tromethamine) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-126493
-
|
DM4-SPDP
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
|
DM4-SPDP is a drug-linker conjugate composed of a potent antitubulin agent DM4 and a linker SMCC to make antibody drug conjugate. SPDP is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls.
|
-
- HY-126974
-
-
- HY-W040236
-
-
- HY-130528
-
-
- HY-126885
-
-
- HY-133547
-
-
- HY-14941
-
|
Elacytarabine
CP 4055
|
Others
|
Cancer
|
|
Elacytarabine (CP 4055) is a lipid-conjugated derivative of the nucleoside analog cytarabine. Elacytarabine (CP 4055) is an antineoplastic drug with cytotoxicity in solid tumors.
|
-
- HY-141170
-
-
- HY-130388
-
-
- HY-102075B
-
|
TMP780
|
ROR
|
Inflammation/Immunology
|
|
TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.
|
-
- HY-130408
-
-
- HY-W008150
-
-
- HY-130457
-
-
- HY-W018174
-
-
- HY-129351
-
-
- HY-120237
-
-
- HY-17428
-
-
- HY-133548
-
-
- HY-B0672
-
-
- HY-130346
-
-
- HY-100160
-
-
- HY-117009
-
-
- HY-136132
-
-
- HY-129350
-
-
- HY-B1148A
-
|
Furaltadone
Altafur
|
Bacterial
|
Infection
|
|
Furaltadone, a nitrofuran drug, has the potential for the study in infections of chickens with salmonella enteritidis. Furaltadone is inhibitory and bactericidal in vitro for staphylococci .
|
-
- HY-141167
-
-
- HY-126889
-
-
- HY-116186
-
-
- HY-W040222
-
-
- HY-W040214
-
-
- HY-130547
-
-
- HY-129378
-
-
- HY-136125
-
-
- HY-130825
-
-
- HY-B1715
-
-
- HY-130381
-
-
- HY-B0421S
-
|
Mycophenolic acid D3
Mycophenolate D3
|
Others
|
Others
|
|
Mycophenolic acid D3 (Mycophenolate D3) is deuterium labeled Mycophenolic acid, which is an an immunosuppresant drug and has potent anti-proliferative activity.
|
-
- HY-17455
-
|
Pramiracetam
|
Others
|
Neurological Disease
|
|
Pramiracetam is a nootropic drug derived from piracetam, and is more potent. Pramiracetam reportedly improved cognitive deficits associated with traumatic brain injuries.
|
-
- HY-133549
-
-
- HY-111494
-
-
- HY-B1153
-
|
Glafenine
Glafenin
|
Others
|
Inflammation/Immunology
|
|
Glafenine is a non-steroidal anti-inflammatory drug (NSAID), is a non-narcotic analgesic agent, widely used for the treatment of pains of various origins.
|
-
- HY-W008429
-
-
- HY-135356
-
-
- HY-B1148
-
-
- HY-140119
-
-
- HY-10127
-
|
AZD1152
Barasertib
|
Aurora Kinase
|
Cancer
|
|
AZD1152 is a pro-drug of Barasertib-hQPA, which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.
|
-
- HY-130827
-
-
- HY-140310
-
-
- HY-B0320A
-
-
- HY-130166
-
-
- HY-120770
-
-
- HY-130385
-
-
- HY-126886
-
-
- HY-130571
-
-
- HY-130933
-
-
- HY-130826
-
-
- HY-U00122
-
-
- HY-130828
-
-
- HY-126502
-
-
- HY-130376
-
-
- HY-126890
-
-
- HY-12396
-
|
Aminothiazole
2-Aminothiazole; 2-Thiazolylamine
|
Bacterial
Fungal
Virus Protease
|
Others
|
|
Aminothiazole (2-Aminothiazole) is a beginning point for synthesis of many compounds including sulfur drugs, biocides, fungicides, dyes and chemical reaction accelerators.
|
-
- HY-130824
-
-
- HY-117031
-
-
- HY-130410
-
-
- HY-100538A
-
|
DTP3 TFA
|
DNA/RNA Synthesis
JNK
|
Cancer
|
|
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
|
-
- HY-13630
-
-
- HY-109785A
-
|
(R)-Gyramide A hydrochloride
|
|
|
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-111406
-
|
Omidenepag isopropyl
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering drug.
|
-
- HY-B0003
-
-
- HY-112764
-
|
DMG-PEG 2000
|
Others
|
Metabolic Disease
|
|
DMG-PEG 2000 is used for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles.
|
-
- HY-B0152B
-
|
Adenine hemisulfate
6-Aminopurine hemisulfate; Vitamin B4 hemisulfate
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Cancer
|
|
Adenine hemisulfate (6-Aminopurine hemisulfate) is a purine derivative with a variety of roles in biochemistry, including cellular respiration, in the form of both the energy-rich adenosine triphosphate (ATP) and the cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD), and protein synthesis, as a chemical component of DNA and RNA.
|
-
- HY-129241
-
|
AGX51
|
Others
|
Cancer
|
|
AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits pathologic ocular neovascularization.
|
-
- HY-B0245S
-
|
Busulfan-D8
|
DNA Alkylator/Crosslinker
Apoptosis
|
|
|
Busulfan-D8 is a deuterium labeled Busulfan. Busulfan is an alkyl sulfonate that acts as an alkylating antineoplastic agent. Busulfan forms both intra- and interstrand crosslinks on DNA. In mammals, Busulfan causes profound and prolonged reduction in the generation of hematopoietic progenitors without significantly affecting lymphocyte levels or humoral antibody responses.
|
-
- HY-120702
-
-
- HY-W006445
-
-
- HY-116427
-
-
- HY-130328
-
|
NH-bis-PEG2
|
ADC Linker
|
Cancer
|
|
NH-bis-PEG2 is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-126523
-
-
- HY-130372
-
-
- HY-136154
-
-
- HY-126521
-
-
- HY-130505
-
-
- HY-141143
-
-
- HY-126495A
-
-
- HY-B0223S
-
|
Albendazole D3
|
Parasite
|
Infection
|
|
Albendazole D3 is the deuterium labeled Albendazole, which is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
|
-
- HY-131086
-
-
- HY-13677
-
-
- HY-W071584
-
-
- HY-130097
-
-
- HY-126522
-
-
- HY-17435
-
|
4'-Demethylepipodophyllotoxin
4'-O-demethylepipodophyllotoxin; 4'-DMEP
|
Microtubule/Tubulin
|
Cancer
|
|
4'-Demethylepipodophyllotoxin(4'-DMEP) is a key intermediate compound for the preparation of podophyllotoxin-type anti-cancer drugs; a potent inhibitor of microtubule assembly.
|
-
- HY-W046471
-
-
- HY-130503
-
-
- HY-133584
-
-
- HY-130591
-
-
- HY-130475
-
-
- HY-126520
-
-
- HY-126676
-
-
- HY-130377
-
-
- HY-18257
-
|
Rolitetracycline
|
Bacterial
Antibiotic
|
Infection
|
|
Rolitetracycline, a derivative of tetracycline, is a broad-spectrum antibiotic. Rolitetracyclin has a role as a protein synthesis inhibitor, an antiprotozoal drug and a prodrug.
|
-
- HY-16672
-
|
AVX 13616
|
Bacterial
|
Infection
|
|
AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens.
|
-
- HY-W071583
-
-
- HY-126960
-
-
- HY-B2247
-
|
PLGA
poly(lactic-co-glycolic acid)
|
Others
|
Others
|
|
PLGA is a copolymer of poly lactic acid (PLA) and poly glycolic acid (PGA) which can be used to fabricate devices for drug delivery and tissue engineering applications.
|
-
- HY-140126
-
-
- HY-125541
-
-
- HY-16291
-
|
APTO-253
LOR-253; LT-253
|
c-Myc
KLF
Apoptosis
|
Cancer
|
|
APTO-253 is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor.
|
-
- HY-13642
-
|
RG108
N-Phthalyl-L-tryptophan
|
DNA Methyltransferase
|
Cancer
|
|
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.
|
-
- HY-12456
-
|
Duocarmycin SA
|
ADC Cytotoxin
DNA Alkylator/Crosslinker
|
Cancer
|
|
Duocarmycin SA is a potent antitumor antibiotic with an IC50 of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.
|
-
- HY-136261
-
|
DM1-PEG4-DBCO
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
DM1-(PEG)4-DBCO is a drug-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody drug conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
|
-
- HY-B1075
-
|
Fosfomycin calcium
MK-0955 calcium
|
Bacterial
Antibiotic
|
Infection
|
|
Fosfomycin calcium (MK-0955 calcium) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium (MK-0955 calcium) shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria.
|
-
- HY-136260
-
|
DBCO-PEG4-Ahx-DM1
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
DBCO-PEG4-Ahx-DM1 is a drug-linker conjugate composed of a potent microtubulin inhibitor DM1 and a linker DBCO-PEG4-Ahx to make antibody drug conjugate (ADC). Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
|
-
- HY-P1449
-
|
Boc-Gly-Gly-Phe-Gly-OH
|
ADC Linker
|
Cancer
|
|
Boc-Gly-Gly-Phe-Gly-OH, a self-assembly of N- and C-protected tetrapeptide, is a protease cleavable linker used for the antibody-drug conjugate (ADC).
|
-
- HY-130165
-
-
- HY-141355
-
-
- HY-17507
-
|
Pantoprazole
BY1023; SKF96022
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
|
|
Pantoprazole (BY1023; SKF96022) is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.
|
-
- HY-120845
-
-
- HY-19371
-
|
Lorediplon
|
GABA Receptor
|
Neurological Disease
|
|
Lorediplon is a novel non-benzodiazepine, hypnotic drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
|
-
- HY-B1378
-
-
- HY-126883
-
-
- HY-14749A
-
-
- HY-17592A
-
|
Bithionol sulfoxide
|
Parasite
|
Cancer
|
|
Bithionol sulfoxide(Bitin-S) is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.
|
-
- HY-136106
-
-
- HY-136432
-
-
- HY-141123
-
-
- HY-130222
-
-
- HY-133408
-
-
- HY-17507B
-
|
Pantoprazole sodium hydrate
BY1023 sodium hydrate; SKF96022 sodium hydrate
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
|
|
Pantoprazole sodium hydrate (BY1023 sodium hydrate; SKF96022 sodium hydrate) is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.
|
-
- HY-135410
-
|
ABZ-amine
Amino albendazole
|
Others
|
Infection
|
|
ABZ-amine (Amino albendazole) is an impurity of Albendazole. Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
|
-
- HY-106579S
-
-
- HY-126884
-
-
- HY-126525
-
-
- HY-W042654
-
-
- HY-129311
-
-
- HY-17507A
-
|
Pantoprazole sodium
BY1023 sodium; SKF96022 sodium
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
|
|
Pantoprazole sodium (BY1023 sodium; SKF96022 sodium) is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.
|
-
- HY-B0777
-
|
Moxidectin
CL301423
|
Parasite
Antibiotic
|
Infection
|
|
Moxidectin(ProHeart 6; CL301423; Cydectin) is an anthelmintic drug which kills parasitic worms (helminths), and is used for the prevention and control of heartworm and intestinal worms.
|
-
- HY-133585
-
-
- HY-16472
-
|
Sulfacytine
|
Antibiotic
Bacterial
|
Infection
|
|
Sulfacytine is a short-acting sulfonamide antibiotic. Sulfacytine is active against bacteria and is an effective drug for the research of acute uncomplicated urinary tract infections.
|
-
- HY-133066
-
-
- HY-120258
-
-
- HY-115374
-
-
- HY-141353
-
-
- HY-19214
-
-
- HY-15741
-
-
- HY-135971
-
-
- HY-W019793
-
-
- HY-18572A
-
|
2,4-D sodium salt
Sodium 2,4-dichlorophenoxyacetate; 2,4-Dichlorophenoxyacetic acid sodium salt
|
DNA/RNA Synthesis
|
Others
|
|
2,4-D sodium salt (Sodium 2,4-dichlorophenoxyacetate) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D sodium salt acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D sodium salt inhibits DNA and protein synthesis and thereby prevents normal plant growth and development.
|
-
- HY-124614
-
|
GLP-26
|
HBV
|
Infection
|
|
GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC50=3 nM), and reduces cccDNA by >90% at 1 μM.
GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools.
|
-
- HY-18572
-
|
2,4-D
2,4-Dichlorophenoxyacetic acid
|
DNA/RNA Synthesis
|
Others
|
|
2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development.
|
-
- HY-13630A
-
|
Etoposide phosphate disodium
BMY-40481 disodium
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
Neurological Disease
|
|
Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
|
-
- HY-15045
-
|
INO-1001
|
PARP
|
Cancer
|
|
INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death. INO-1001 has anti-tumor effects.
|
-
- HY-14521
-
|
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity.
|
-
- HY-14521B
-
|
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity.
|
-
- HY-117433
-
-
- HY-12458
-
|
Pyrindamycin A
|
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
|
-
- HY-16745
-
|
Lascufloxacin
KRP-AM1977X
|
Bacterial
|
Infection
|
|
Lascufloxacin (KRP-AM1977X) is a potent and orally active fluoroquinolone antibacterial agent. Lascufloxacin potently inhibits infections caused by various pathogens, including quinolone-resistant strains. Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections.
|
-
- HY-N7523
-
|
Neoxanthin
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Neoxanthin is a major xanthophyll carotenoid and a precursor of the plant hormone abscisic acid in dark green leafy vegetables. Neoxanthin is a potent antioxidant and light-harvesting pigment. Neoxanthin induces apoptosis and has anticancer actions.
|
-
- HY-135901
-
-
- HY-112005
-
-
- HY-107485
-
-
- HY-N6022
-
|
Byakangelicin
|
Others
|
Metabolic Disease
|
|
Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
|
-
- HY-126958
-
-
- HY-136051
-
-
- HY-100640
-
-
- HY-136099
-
-
- HY-136044
-
-
- HY-118764
-
-
- HY-136309
-
-
- HY-130080
-
|
DM3
Maytansinoid DM3
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
DM3 (Maytansinoid DM3) is a maytansine analog bearing disulfide or thiol groups and a tubulin inhibitor, and is a cytotoxic moiety of antibody-drug conjugates (ADCs).
|
-
- HY-140115
-
-
- HY-30235A
-
-
- HY-136091
-
-
- HY-130449
-
-
- HY-140454
-
-
- HY-136052
-
-
- HY-135961
-
-
- HY-N7028
-
|
Withanolide A
|
Others
|
Neurological Disease
|
|
Withanolide A, isolated from the indian herbal drug Ashwagandha (root of Withania somnifera), could regenerate neurites and reconstruct synapses in severely damaged neurons.
|
-
- HY-136086
-
-
- HY-136049
-
-
- HY-116655
-
-
- HY-A0241
-
|
Dalfopristin
RP54476
|
Bacterial
Antibiotic
|
Infection
|
|
Dalfopristin is a semi-synthetic streptogramin antibiotic. Quinupristin/Dalfopristin (Q/D) is a valuable alternative antibiotic to vancomycin for the treatment of multi-drug resistant Enterococcus faecium infections.
|
-
- HY-114415
-
|
AWZ1066S
|
Parasite
|
Infection
|
|
AWZ1066S is a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis, with an EC50 of 2.5 nM in cell assay.
|
-
- HY-135974
-
-
- HY-140244
-
-
- HY-A0069
-
-
- HY-B1041
-
|
Aminoguanidine hydrochloride
Pimagedine hydrochloride; GER-11; Aminoguanidinium chloride
|
Others
|
Endocrinology
|
|
Aminoguanidine hydrochloride is a diamine oxidase and NO synthase inhibitor, reduces levels of advanced glycation end products (AGEs) through interacting with 3-deoxyglucosone, is an investigational drug for the treatment of diabetic nephropathy.
|
-
- HY-136046
-
-
- HY-B0106A
-
-
- HY-W019799
-
-
- HY-140097
-
-
- HY-136045
-
-
- HY-B2060
-
|
Tiamulin
Thiamutilin
|
Bacterial
Antibiotic
|
Infection
|
|
Tiamulin (Thiamutilin) is a diterpenic veterinary drug widely used in swine for the control of infectious diseases, including swine dysentery and enzootic pneumonia.
|
-
- HY-18719A
-
-
- HY-136067
-
-
- HY-136048
-
-
- HY-P1449A
-
-
- HY-136127
-
-
- HY-B0647
-
|
Butylphthalide
3-n-Butylphthalide; 3-Butylphthalide
|
Others
|
Neurological Disease
|
|
Butylphthalide(3-n-Butylphthalide) is an anti-cerebral-ischemia drug; first isolated from the seeds of celery, showed efficacy in animal models of stroke.
|
-
- HY-117104
-
-
- HY-101141
-
-
- HY-136077
-
-
- HY-136061
-
-
- HY-135964
-
-
- HY-136050
-
-
