Search Result
Results for "Atr atm dna pk drug Inhibitors" in MCE Product Catalog:
9852
Inhibitors & Agonists
43
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- 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-100948B
-
-
- 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-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-U00447
-
-
- 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-15520
-
-
- 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-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-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-100140A
-
-
- HY-100346
-
|
PK14105
|
Others
|
Others
|
|
PK14105 is a biological evaluation as a potential radioligand for PET studies of PBBS receptors.
|
-
- 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-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-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-128897
-
-
- HY-100140
-
-
- HY-128917
-
-
- 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-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-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-109517
-
-
- HY-B0097
-
|
Floxuridine
5-Fluorouracil 2'-deoxyriboside
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
Apoptosis
|
Cancer
Infection
|
|
Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.
|
-
- HY-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-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-B0211
-
-
- HY-B0211A
-
-
- HY-19939S
-
-
- HY-17394
-
-
- 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-U00439
-
-
- 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-111783
-
-
- 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-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-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-112197
-
-
- 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-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-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-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-126020
-
|
Bractoppin
|
DNA/RNA Synthesis
RAD51
|
Cancer
|
|
Bractoppin is a potent and selective drug-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response.
|
-
- HY-D1020
-
-
- 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-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-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-101427
-
-
- 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-137697
-
|
ddCTP
|
DNA/RNA Synthesis
|
Others
|
|
ddCTP is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing.
|
-
- HY-137694
-
|
ddTTP
|
DNA/RNA Synthesis
|
Others
|
|
ddTTP is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing.
|
-
- HY-17565A
-
-
- HY-10108
-
|
LY294002
|
PI3K
Casein Kinase
DNA-PK
Autophagy
Apoptosis
|
Cancer
Infection
|
|
LY294002 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-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-12061
-
-
- 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-134103
-
|
ddGTP
2′,3′-Dideoxyguanosine 5′-triphosphate
|
DNA/RNA Synthesis
|
Others
|
|
ddGTP (2′,3′-Dideoxyguanosine 5′-triphosphate) is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing.
|
-
- HY-101162
-
|
SGD-1910
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
SGD-1910 is a drug-linker conjugate for ADC by using the antitumor antibiotic, pyrrolobenzodiazepine (PBD, a cytotoxic DNA crosslinking), linked via the cleavable linker MC-Val-Ala.
|
-
- HY-W013068
-
-
- HY-130978
-
|
Duocarmycin DM
|
DNA Alkylator/Crosslinker
ADC Cytotoxin
|
Cancer
|
|
Duocarmycin DM, a DNA minor-groove alkylator, is an antibody drug conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity.
|
-
- HY-W013059
-
-
- HY-W008849
-
-
- HY-W008848
-
-
- HY-15521
-
-
- 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-137843
-
|
NSC 80467
|
DNA/RNA Synthesis
|
Cancer
|
|
NSC 80467, a DNA damaging agent, selectively inhibits survivin. NSC 80467 preferentially inhibits DNA synthesis and results in induction of γH2AX and pKAP1, two markers of DNA damage.
|
-
- HY-132136
-
-
- 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-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-101146
-
-
- 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-128915
-
-
- HY-101566A
-
|
Elimusertib hydrochloride
BAY 1895344 hydrochloride
|
ATM/ATR
|
Cancer
|
|
Elimusertib (BAY 1895344) hydrochloride is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity.
|
-
- HY-11006
-
|
KU-57788
NU7441
|
DNA-PK
CRISPR/Cas9
|
Cancer
|
|
KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively.
|
-
- HY-135146
-
-
- HY-109566
-
-
- HY-101566
-
|
Elimusertib
BAY 1895344
|
ATM/ATR
|
Cancer
|
|
Elimusertib (BAY-1895344) is a potent, orally available and selective ATR inhibitor with an IC50 of 7 nM. Anti-tumor activity.
|
-
- 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-125930
-
|
T-2513
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
|
-
- HY-114147
-
-
- 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-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-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-N0872
-
-
- HY-128952
-
|
Tesirine
SG3249
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Tesirine (SG3249) is a drug-linker conjugates for ADC which is used in the treatment of several cancers. PBD Dimer is a DNA alkylating which inhibits DNA replication.
|
-
- HY-15583
-
-
- HY-19024
-
|
Merbarone
NSC 336628
|
Topoisomerase
|
Cancer
|
|
Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.
|
-
- 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-137316
-
-
- HY-B0738
-
|
Dithranol
Anthralin
|
Others
|
Inflammation/Immunology
|
|
Dithranol (Anthralin) is an anthraquinone derivative, with potent anti-psoriatic effects. Dithranol can inhibit DNA replication and repair.
|
-
- HY-131005
-
-
- HY-137316A
-
-
- 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-17381
-
-
- HY-111308
-
-
- HY-12484
-
|
BMH-21
|
DNA/RNA Synthesis
|
Cancer
|
|
BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity.
|
-
- HY-109190
-
|
Seralutinib
GB002; pk10571
|
PDGFR
|
Cardiovascular Disease
|
|
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
|
-
- HY-B0152
-
|
Adenine
6-Aminopurine; Vitamin B4
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Cancer
|
|
Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA.
Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
|
-
- HY-B0152A
-
|
Adenine hydrochloride
6-Aminopurine hydrochloride; Vitamin B4 hydrochloride
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Cancer
|
|
Adenine hydrochloride (6-Aminopurine hydrochloride), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine hydrochloride acts as a chemical component of DNA and RNA. Adenine hydrochloride also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
|
-
- 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-130083
-
-
- HY-131955
-
-
- 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-123637
-
-
- 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-128357
-
|
Ibezapolstat
ACX-362E; GLS-362E
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Ibezapolstat (ACX-362E) is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a Ki of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat is developed for the research of C. difficile infection(CDI).
|
-
- 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-B0152B
-
|
Adenine hemisulfate
6-Aminopurine hemisulfate; Vitamin B4 hemisulfate
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Cancer
|
|
Adenine hemisulfate (6-Aminopurine hemisulfate), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine hemisulfate acts as a chemical component of DNA and RNA. Adenine hemisulfate also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis.
|
-
- HY-101400
-
-
- 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-126490
-
|
Phleomycin
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Phleomycin is an anticancer glycopeptide antibiotic found in Streptomyces verticillus, which cause DNA cleavage. Phleomycin binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A).
|
-
- HY-17469
-
|
Gimeracil
Gimestat
|
Others
|
Cancer
|
|
Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD).
|
-
- 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 activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
|
-
- HY-101400A
-
-
- HY-B0069
-
-
- 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-132137
-
-
- HY-132138
-
-
- HY-12892
-
|
SKI-178
|
SPHK
Apoptosis
|
Cancer
|
|
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
|
-
- HY-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-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-136548
-
-
- HY-B1497
-
|
Silver sulfadiazine
AgSD
|
Bacterial
DNA/RNA Synthesis
Antibiotic
|
Infection
|
|
Silver sulfadiazine (AgSD), a sulfonamide antibiotic, effects a dual inhibitory action on bacterial growth by its sulfa moiety (SD-SDZ) that prevents bacterial folate absorption and subsequent DNA synthesis. The silver that is released from Silver sulfadiazine binds and disrupts the DNA structure, precluding bacterial DNA replication.
|
-
- HY-69014
-
-
- 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-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-128959
-
-
- HY-133598
-
-
- 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-136548A
-
-
- HY-121879
-
-
- HY-A0061
-
-
- 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-135797A
-
|
DB1976 dihydrochloride
|
Apoptosis
|
Cancer
|
|
DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 dihydrochloride has apoptosis-inducing effect.
|
-
- HY-110137A
-
|
Furamidine
DB75; NSC 305831
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
|
Furamidine (DB75) is a selective 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). 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 an antiparasite agent.
|
-
- HY-110137
-
|
Furamidine dihydrochloride
DB75 dihydrochloride; NSC 305831 dihydrochloride
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
|
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
|
-
- 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-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-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-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-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-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-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-15290
-
|
AIM-100
|
Ack1
|
Cancer
|
|
AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr 267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect.
|
-
- HY-127039
-
-
- HY-127034
-
-
- HY-136559
-
-
- 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-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-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-D0226
-
|
Quinizarin
1,4-Dihydroxyanthraquinone
|
DNA/RNA Synthesis
Fungal
|
Cancer
Infection
|
|
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth.
|
-
- HY-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-14532
-
|
Brincidofovir
CMX001; HDP-CDV
|
CMV
HSV
|
Infection
|
|
Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections.
|
-
- HY-122493
-
-
- HY-130569
-
|
7-Hydroxymethotrexate
|
Drug Metabolite
|
Cancer
Inflammation/Immunology
|
|
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
-
- 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-19743
-
-
- HY-B0268A
-
|
Enoxacin hydrate
Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate
|
Bacterial
DNA/RNA Synthesis
MicroRNA
Antibiotic
|
Infection
Cancer
|
|
Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
|
-
- HY-B0268
-
|
Enoxacin
AT 2266; CI 919
|
Bacterial
DNA/RNA Synthesis
MicroRNA
Antibiotic
|
Cancer
Infection
|
|
Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
|
-
- 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-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-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-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-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-114233
-
-
- HY-128909
-
-
- HY-129356A
-
-
- 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-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-15559A
-
-
- HY-10372
-
-
- 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-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-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-19373
-
-
- HY-W008990
-
|
Xanthosine 5'-monophosphate sodium salt
5'-Xanthylic acid sodium salt
|
Others
|
Metabolic Disease
|
|
Xanthosine 5'-monophosphate sodium salt (5'-Xanthylic acid sodium salt) is an intermediate in purine metabolism. Xanthosine 5'-monophosphate sodium salt can be used for genetic code, nucleic acid structure, and DNA, RNA and protein synthesis research.
|
-
- HY-15560
-
-
- 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-133646
-
|
Bromochloroacetonitrile
|
DNA/RNA Synthesis
|
Others
|
|
Bromochloroacetonitrile is a by-product of the chlorine disinfection of water containing natural organic material. Bromochloroacetonitrile possesses direct acting mutagenic activity and is capable of inducing DNA strand breakage.
|
-
- HY-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-137067
-
|
IMT1B
LDC203974
|
Others
|
Cancer
|
|
IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.
|
-
- HY-N0720
-
|
Neobavaisoflavone
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Neobavaisoflavone, a flavonoid, is isolated from the seeds of Psoralea corylifolia. Neobavaisoflavone exhibits anti-inflammatory, anti-cancer and anti-oxidation activities. Neobavaisoflavone inhibits DNA polymerase at moderate to high concentrations. Neobavaisoflavone also inhibits platelet aggregation.
|
-
- HY-124325
-
|
PIP-199
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.
|
-
- HY-13637
-
|
Ganciclovir
BW 759; 2'-Nor-2'-deoxyguanosine
|
CMV
HSV
Antibiotic
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1).
|
-
- HY-13637A
-
|
Ganciclovir sodium
BW 759 sodium; 2'-Nor-2'-deoxyguanosine sodium
|
CMV
HSV
Antibiotic
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Ganciclovir (BW 759) sodium, a nucleoside analogue and an orally active antiviral agent, shows activity against CMV. Ganciclovir sodium also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir sodium inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir sodium has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1).
|
-
- HY-12333
-
|
G-749
|
FLT3
Apoptosis
|
Cancer
|
|
G-749 is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. G-749 can be used for the research of drug resistance for acute myeloid leukemia (AML).
|
-
- HY-15560B
-
-
- 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-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-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-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-130801
-
-
- HY-15176
-
|
Pyridostatin
RR82
|
G-quadruplex
|
Cancer
|
|
Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
|
-
- HY-15176A
-
|
Pyridostatin hydrochloride
RR82 hydrochloride
|
G-quadruplex
|
Cancer
|
|
Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
|
-
- HY-W014622
-
|
CRT0044876
|
DNA/RNA Synthesis
|
Cancer
|
|
CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds.
|
-
- 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-101042
-
|
AG-494
Tyrphostin AG 494
|
EGFR
CDK
|
Cancer
|
|
AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
|
-
- HY-10080
-
|
Teglarinad chloride
GMX1777; EB-1627
|
NAMPT
|
Cancer
|
|
Teglarinad chloride (GMX1777) is a prodrug of GMX1778 (a nicotinamide phosphoribosyl transferase inhibitor). Teglarinad chloride exhibits antitumor activity in mice can be attributed to inhibition of NAMPT. Teglarinad chloride also enhances radiation efficacy, mediated by interference with DNA repair and antiangiogenesis.
|
-
- 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-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-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-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-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-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-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-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-15176B
-
|
Pyridostatin TFA
RR82 TFA
|
G-quadruplex
|
Cancer
|
|
Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
|
-
- 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-113303
-
-
- HY-B1355A
-
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-13703A
-
-
- HY-128957
-
-
- HY-131057
-
-
- HY-115292
-
|
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-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-N8533
-
|
Sodium Camptothecin
|
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and, intracellularly, causes breaks in preformed viral DNA.
|
-
- 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-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-112899
-
-
- HY-19609
-
-
- HY-B0330A
-
-
- 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-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-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-B0028
-
-
- 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-134723
-
-
- 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-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-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-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-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-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-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-17565
-
-
- 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-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-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-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-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-16562
-
|
Irinotecan
(+)-Irinotecan; CPT-11
|
Topoisomerase
Autophagy
|
Cancer
|
|
Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
|
-
- HY-128904
-
-
- 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-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-U00433A
-
-
- 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-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-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-18728
-
-
- HY-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-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-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-107096B
-
|
CH-0793076 TFA
TP3076 TFA
|
Topoisomerase
|
Cancer
|
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein).
|
-
- HY-101647
-
-
- 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-17393
-
-
- HY-13605
-
-
- HY-13605A
-
-
- HY-123523
-
-
- 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-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-A0098
-
|
Tunicamycin
|
Bacterial
Fungal
Influenza Virus
Antibiotic
|
Cancer
Infection
Inflammation/Immunology
|
|
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.Tunicamycin increases exosome release in cervical cancer cells.
|
-
- HY-N0057
-
|
3,4-Dicaffeoylquinic acid
3,4-Di-O-caffeoylquinic acid; Isochlorogenic acid B
|
Glucosidase
Influenza Virus
Apoptosis
Endogenous Metabolite
|
Cancer
Infection
|
|
3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL.
|
-
- 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-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-B0879A
-
|
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
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 is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-B0879
-
|
Suramin
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- 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-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-16700
-
|
PNU-159682
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
PNU-159682, a metabolite of the anthracycline nemorubicin, is a highly potent DNA topoisomerase I inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome drug resistance.
|
-
- HY-131394
-
|
5-Hydroxymethyl-2’-deoxycytidine
5hmdC
|
Others
|
Cancer
|
|
5-Hydroxymethyl-2’-deoxycytidine (5hmdC) is an oxidation derivative of 5-methyl-2'-deoxycytidine (5-mdC) in DNA. 5-Hydroxymethyl-2’-deoxycytidine may serve as a marker of irreversibly damaged cells.
|
-
- HY-13599
-
|
Cladribine
2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA
|
Adenosine Deaminase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
|
-
- HY-A0004
-
|
Decitabine
5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716
|
DNA Methyltransferase
Apoptosis
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Decitabine (NSC 127716) is an orally active 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-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-13424
-
-
- 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-W010342
-
|
6-Aminonicotinamide
|
Others
|
Cancer
|
|
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP +-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells.
|
-
- HY-17422
-
|
Acyclovir
Aciclovir; Acycloguanosine
|
HSV
Bacterial
Apoptosis
Antibiotic
|
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-17371
-
|
Oxaliplatin
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Autophagy
|
Cancer
|
|
Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
|
-
- HY-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-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-15552
-
-
- HY-13727
-
-
- 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-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-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-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-13753
-
-
- HY-10586
-
-
- HY-B0313
-
-
- HY-13727A
-
-
- HY-16560
-
-
- 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-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-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-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-19977
-
|
YU238259
|
DNA-PK
|
Cancer
|
|
YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.
|
-
- HY-A0005
-
-
- HY-15753
-
-
- HY-15753A
-
-
- 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-15627A
-
-
- 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-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-128962
-
-
- 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-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-13758
-
-
- HY-13758A
-
-
- HY-B1099
-
|
Hycanthone
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
|
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
|
-
- HY-15588
-
-
- HY-B0497B
-
-
- HY-119372
-
-
- HY-12344
-
|
UNC2025
|
FLT3
|
Cancer
|
|
UNC2025 is a potent, ATP-competitive 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-12344A
-
|
UNC2025 hydrochloride
|
FLT3
|
Cancer
|
|
UNC2025 hydrochloride is a potent, ATP-competitive, 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-13747
-
-
- 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-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-13420
-
-
- HY-15746
-
-
- 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-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-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-N2033
-
-
- HY-W008915
-
|
Cytidine 5'-diphosphate trisodium salt
CDP
|
Others
|
Metabolic Disease
|
|
Cytidine 5'-diphosphate trisodium salt (CDP) is produced by the transfer of phosphoryl group from ATP to cytidine monophosphate (CMP) catalyzed by uridine monophosphate kinase (UMPK). Cytidine 5′-diphosphate can be used to produce Cytidine triphosphate (CTP) for synthesis of DNA and RNA.
|
-
- 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-109056
-
|
Elsulfavirine
|
HIV
|
Infection
|
|
Elsulfavirine is a reverse transcriptase inhibitors for HIV-1 infection and is a new anti-HIV drug.
|
-
- 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-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-16261B
-
-
- HY-16261A
-
-
- HY-15233
-
|
Letermovir
AIC246
|
CMV
|
Infection
|
|
Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
|
-
- HY-13062
-
-
- HY-15457
-
-
- HY-N7452
-
-
- 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-16398
-
|
Pipobroman
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Pipobroman is a bromide derivative of piperazine and acts as an alkylating agent. Pipobroman plays its role by inhibiting DNA and RNA polymerase or by reducing pyrimidine nucleotide incorporation into DNA. Pipobroman can be used for the cancer research, including polycythemia vera, myeloproliferative neoplasm, and AML et.al.
|
-
- 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-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-19826
-
-
- 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-136110
-
-
- 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-112669
-
-
- 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-111183
-
-
- HY-126124
-
|
AP39
|
Others
|
Neurological Disease
Cardiovascular Disease
|
|
AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H2S) donor. AP39 increases intracellular H2S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury and protects against Alzheimer's disease in mice model.
|
-
- 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-N0311
-
-
- HY-U00248
-
|
LMP744
MJ-III65; NSC706744
|
Topoisomerase
|
Cancer
|
|
LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
|
-
- 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-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-13562A
-
-
- HY-12746
-
-
- 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-W006395
-
-
- 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-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-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-136648
-
-
- HY-101603
-
-
- HY-10074
-
-
- HY-14573
-
-
- 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-13631
-
|
Exatecan
DX-8951
|
Topoisomerase
|
Cancer
|
|
Exatecan (DX-8951) 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-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-136648A
-
-
- HY-W012078
-
-
- 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-108316
-
-
- HY-B0003
-
-
- 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-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-13631A
-
|
Exatecan mesylate
DX8951f
|
Topoisomerase
|
Cancer
|
|
Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
|
-
- 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-17026
-
-
- HY-B0132
-
-
- HY-13701
-
-
- 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-128960
-
-
- HY-135660
-
-
- 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-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-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-10821
-
-
- HY-B1074
-
-
- 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-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-N0629
-
-
- HY-13062A
-
-
- 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-W008661
-
|
Deoxyguanosine triphosphate trisodium salt
dGTP trisodium salt; 2'-Deoxyguanosine-5'-triphosphate trisodium salt
|
DNA/RNA Synthesis
|
Others
|
|
Deoxyguanosine triphosphate (dGTP) trisodium salt is a nucleotide precursor in cells for DNA synthesis. Deoxyguanosine triphosphate trisodium salt is used in reverse transcription-polymerase chain reaction (RT-PCR) for DNA amplification.
|
-
- 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-N2897
-
-
- 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-129938
-
-
- HY-15750
-
-
- HY-15581
-
-
- HY-B1287
-
-
- HY-A0293
-
|
Pyrvinium pamoate
Pyrvinium embonate
|
Wnt
|
Cancer
|
|
Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
|
-
- HY-136650
-
-
- HY-N6046
-
-
- HY-112822
-
|
ON-013100
|
CDK
|
Cancer
|
|
ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
|
-
- HY-100951
-
-
- HY-17574
-
-
- 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-N6638
-
|
Retrorsine
|
Others
|
Metabolic Disease
|
|
Retrorsine is a naturally occurring toxic pyrrolizidine alkaloid. Retrorsine can bind with DNA and inhibits the proliferative capacity of hepatocytes. Retrorsine can be used for the research of hepatocellular injury.
|
-
- 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-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-17484
-
-
- HY-15374
-
-
- HY-112060
-
-
- HY-111375
-
-
- 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-133624
-
|
1,1,3-Tribromoacetone
|
Others
|
Cancer
|
|
1,1,3-Tribromoacetone is an impurity of Methotrexate (HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.
|
-
- 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-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-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-B1279
-
-
- HY-100669
-
|
Mycro 3
|
c-Myc
Autophagy
|
Cancer
|
|
Mycro 3 is a potent and selective inhibitor of Myc-associated factor X (MAX) dimerization. Mycro 3 also inhibit DNA binding of c-Myc. Mycro 3 could be used for the research of pancreatic cancer.
|
-
- 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-13669
-
-
- HY-13700
-
-
- HY-14798
-
-
- HY-13585
-
-
- 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-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-100599
-
-
- HY-13631AS
-
|
Exatecan D5 mesylate
DX8951f-D5; D5-Exatecan mesylate
|
Topoisomerase
|
Cancer
|
|
Exatecan D5 mesylate (DX8951f-D5) is deuterium labeled Exatecan Mesylate. Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL.
|
-
- HY-135325
-
-
- 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-17625
-
-
- 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-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-13624A
-
|
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13624
-
|
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-103504
-
-
- 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-U00441
-
|
DPBQ
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
|
-
- HY-17577
-
-
- HY-16293
-
-
- HY-129356
-
-
- HY-U00337
-
-
- HY-107769
-
-
- HY-135846
-
|
PDD00031705
|
Others
|
Cancer
|
|
PDD00031705 is a benzimidazolone core cell-inactive inhibitor of Poly (ADP-ribose) glycohydrolase (PARG).
|
-
- 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-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-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-B2194
-
-
- HY-17509
-
-
- 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-W009109
-
-
- HY-129355
-
-
- 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-14398
-
-
- HY-B1895
-
-
- HY-B0367
-
-
- 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-B0703
-
-
- 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-N6725
-
-
- 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-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-16513
-
-
- HY-W040329
-
-
- HY-16496
-
-
- HY-N6828
-
-
- HY-137658
-
|
Purine riboside triphosphate
PTP
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
Purine riboside triphosphate is a triphosphate derivative of purine riboside. Purine riboside is a naturally occurring base analog which closely resembles adenosine. Purine riboside inhibits carcinogenic growth. Purine riboside strongly inhibits RNA and DNA synthesis in different cancer ascites cells.
|
-
- HY-N4058
-
|
Helichrysetin
|
Apoptosis
|
Cancer
|
|
Helichrysetin, isolated from the flowers of Helichrysum odoratissimum, is an ID2 (inhibitor of DNA binding 2) inhibitor, and suppresses DCIS (ductal carcinoma in situ) formation. Helichrysetin possess strong inhibitory effects on cell growth and is capable of inducing apoptosis in A549 cells.
|
-
- HY-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-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-111320
-
|
Chrysomycin B
|
Bacterial
Antibiotic
|
Cancer
|
|
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-13962
-
-
- HY-B1153A
-
-
- HY-17006
-
-
- 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-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-B1002
-
|
Oxolinic acid
|
Bacterial
Antibiotic
DNA/RNA Synthesis
|
Infection
|
|
Oxolinic acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid is a DNA/RNA synthesis inhibitor. Oxolinic acid acts a dopamine uptake inhibitor and stimulants locomotor effect in mice.
|
-
- HY-103710
-
|
IBR2
|
RAD51
Apoptosis
|
Cancer
|
|
IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis.
|
-
- HY-B0125
-
-
- HY-131991
-
|
Benzyl selenocyanate
|
DNA Methyltransferase
|
Cancer
|
|
Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. Benzyl selenocyanate is an inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an with an IC50 of 8.4 µM.
|
-
- 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-15742
-
-
- HY-17427
-
-
- HY-15740
-
-
- HY-17579
-
-
- 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-13859
-
|
Clevudine
L-FMAU
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase.
|
-
- HY-107485
-
-
- HY-B1079
-
-
- HY-100358
-
-
- HY-114750
-
-
- HY-113306
-
-
- HY-112680A
-
-
- 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-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-135780
-
-
- HY-106855
-
-
- 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-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-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-14908
-
-
- 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-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-15336
-
|
AG 555
Tyrphostin AG 555
|
EGFR
Reverse Transcriptase
|
Cancer
|
|
AG 555 (Tyrphostin AG 555), a potent antiretroviral drug, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation.
|
-
- HY-B0320A
-
-
- HY-103673
-
-
- HY-B1418
-
|
Tazobactam
CL-298741; YTR-830H
|
Bacterial
Antibiotic
|
Infection
|
|
Tazobactam is a beta Lactamase Inhibitor with antibacterial activity
Target: Antibacterial
Tazobactam is a pharmaceutical drug that inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups.
|
-
- HY-134320
-
-
- 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-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-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-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-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-15741
-
-
- 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-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-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-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-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-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-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-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-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-15523A
-
|
Braco-19 trihydrochloride
|
DNA/RNA Synthesis
CMV
|
Cancer
Infection
|
|
Braco-19 trihydrochloride is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor.
|
-
- HY-15523
-
|
Braco-19
|
CMV
DNA/RNA Synthesis
|
Cancer
|
|
Braco-19 is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor.
|
-
- HY-A0077AS
-
-
- 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-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-107004A
-
-
- 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-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-101660
-
-
- HY-101828
-
-
- 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-108556
-
|
RWJ-56110
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
|
-
- HY-66004
-
|
4-Acetamidophenyl acetate
|
Others
|
Inflammation/Immunology
|
|
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
|
-
- HY-136287
-
-
- HY-N0908
-
-
- 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-B0546
-
-
- HY-B1777
-
-
- HY-111806
-
-
- HY-16637
-
-
- HY-136649
-
-
- HY-B0546A
-
-
- HY-15910
-
|
5-BrdU
BrdU; 5-Bromo-2'-deoxyuridine; BUdR
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
5-BrdU (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-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-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-100640
-
-
- HY-121721
-
|
Inz-5
|
Fungal
|
Infection
|
|
Inz-5 is a fungal-selective mitochondrial cytochrome bc1 inhibitor. Inz-5 impairs fungal virulence and prevents the evolution of drug resistance.
|
-
- 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-116364
-
|
AZT triphosphate
3'-Azido-3'-deoxythymidine-5'-triphosphate
|
HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species
Apoptosis
|
Infection
|
|
AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway.
|
-
- HY-N0093
-
-
- HY-U00071
-
-
- HY-B0994
-
-
- HY-111606
-
-
- 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-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-13630
-
-
- HY-107407
-
|
SB-218078
|
Checkpoint Kinase (Chk)
CDK
PKC
Apoptosis
|
Cancer
|
|
SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest.
|
-
- HY-103687
-
|
Abiraterone metabolite 1
3β-OH-5α-Abi
|
Drug Metabolite
|
Cancer
|
|
Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
|
-
- HY-N1403
-
|
Tigogenin
|
Others
|
Metabolic Disease
|
|
Tigogenin, one of steroidal sapogenins, is widely used for synthesizing steroid drugs. Tigogenin inhibits adipocytic differentiation and induces osteoblastic differentiation in mouse bone marrow stromal cells.
|
-
- HY-12460
-
-
- HY-B0439
-
|
Sulfadoxine
Sulphadoxine
|
Parasite
HIV
Antibiotic
|
Infection
|
|
Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.
|
-
- HY-128896
-
-
- HY-112786
-
-
- HY-15582
-
|
Auristatin E
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates. Auristatin E inhibits cell division by blocking the polymerisation of tubulin.
|
-
- 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-N7025
-
-
- HY-15295
-
|
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-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-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-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-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-100202
-
|
TPEN
TPEDA
|
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
|
TPEN (TPEDA) is a specific cell-permeable heavy metal chelator. TPEN has a higher affinity for Zn 2+, but a lower affinity for Mg 2+ and Ca 2+. TPEN induces DNA damage and increases intracellular ROS production. TPEN also inhibits cell proliferation and induces apoptosis.
|
-
- HY-B0116
-
-
- HY-B0116A
-
-
- HY-138280
-
|
DTHIB
|
HSP
|
Cancer
|
|
DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research.
|
-
- HY-100139
-
-
- HY-B0338A
-
-
- HY-B0246
-
-
- HY-101751
-
-
- HY-101829
-
-
- HY-14290A
-
-
- HY-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-136457
-
|
2-NP-AHD
|
Others
|
Others
|
|
2-NP-AHD is a 2-nitrophenyl derivative of AHD (a metabolite of nitrofurans type of antibiotics), can be used as indicator of the illegal usage of nitrofuran drugs.
|
-
- HY-128930
-
-
- HY-19902
-
-
- HY-100513A
-
|
Dehydroaltenusin
|
Apoptosis
DNA/RNA Synthesis
Antibiotic
|
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-136317
-
-
- HY-15579S
-
|
D8-MMAF
Monomethylauristatin F D8
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
D8-MMAF hydrochloride is a deuterated form of MMAF hydrochloride. MMAF Hydrochloride, a potent tubulin polymerization inhibitor, is used as a antitumor agent and a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-128906
-
-
- 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-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-Y1055
-
-
- HY-14714
-
-
- HY-14781
-
-
- HY-I0626
-
|
Cytosine
|
Endogenous Metabolite
|
Others
|
|
Cytosine is one of the four main bases found in DNA and RNA. Cytosine modifications exhibit circadian oscillations that are involved in epigenetic diversity and aging.
|
-
- HY-19639
-
|
E-982
|
Others
|
Others
|
|
E-982 is a steroid used for the on-line screening of the DNA unwinding element binding protein (DUE-B) immobilized protein column.
|
-
- HY-13721
-
|
Phenoxodiol
Idronoxil; Dehydroequol; Haginin E
|
Caspase
Apoptosis
Topoisomerase
|
Cancer
|
|
Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner.
|
-
- HY-118411
-
|
5-Ethynyl-2'-deoxyuridine
|
PROTAC Linker
|
Cancer
|
|
5-Ethynyl-2'-deoxyuridine (EdU), a thymidine analogue, is incorporated into cellular DNA during DNA replication and the subsequent reaction of EdU with a fluorescent azide in a “Click” reaction. EdU staining is a fast, sensitive and reproducible method to study cell proliferation. 5-Ethynyl-2'-deoxyuridine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-19747
-
|
HPOB
|
HDAC
Apoptosis
|
Cancer
|
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.
|
-
- HY-109785A
-
|
(R)-Gyramide A hydrochloride
|
|
Infection
|
|
(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-14521
-
|
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-14521B
-
|
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-136286
-
-
- 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-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-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-B0921
-
-
- HY-101748
-
-
- HY-101670
-
-
- HY-B0766
-
-
- HY-116364A
-
|
AZT triphosphate TEA
3'-Azido-3'-deoxythymidine-5'-triphosphate TEA
|
HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species
Apoptosis
|
Infection
|
|
AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway.
|
-
- HY-128903
-
-
- HY-128907
-
-
- HY-128902
-
-
- HY-19811
-
-
- HY-128961
-
-
- HY-100374
-
|
Val-Cit-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization.
|
-
- HY-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-B0171
-
|
Antipyrine
Phenazone; Phenazon
|
Others
|
Inflammation/Immunology
|
|
Antipyrine (Phenazone) is an antipyretic and analgesic. Antipyrine can be used as a probe drug for oxidative drug metabolism. Antipyrine has been widely used in assessment of hepatic oxidative capacity.
|
-
- HY-B0986
-
|
Hexylresorcinol
4-Hexylresorcinol
|
Parasite
Bacterial
Apoptosis
Glucosidase
|
Cancer
Infection
Metabolic Disease
|
|
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
|
-
- HY-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-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-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-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-U00337A
-
-
- 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-15162
-
|
Monomethyl auristatin E
MMAE; SGD-1010
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
|
-
- HY-B2087
-
-
- HY-111414
-
|
Hsp90-Cdc37-IN-1
|
HSP
|
Cancer
|
|
Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse drug resistance, with an IC50 of 140 nM.
|
-
- HY-128871
-
|
VCP-Eribulin
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
VCP-Eribulin consists the ADCs linker (VCP) and Eribulin. Eribulin is a mechanistically unique microtubule inhibitor for cancer. VCP-Eribulin is an Eribulin-based drug for antibody conjugates.
|
-
- HY-128955
-
-
- HY-128893
-
-
- HY-133492
-
-
- HY-12331
-
|
KRCA-0008
|
Ack1
ALK
|
Cancer
|
|
KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.
|
-
- HY-130603
-
|
DCZ0415
|
NF-κB
Apoptosis
|
Cancer
|
|
DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.
|
-
- 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-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-A0057
-
-
- HY-12769
-
-
- HY-B1086
-
-
- HY-A0057A
-
-
- HY-B0343A
-
-
- HY-B1346
-
-
- HY-U00403
-
-
- HY-17581
-
-
- HY-U00055
-
-
- HY-U00025
-
-
- 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-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-N2513
-
|
β-Boswellic acid
|
Lipoxygenase
DNA/RNA Synthesis
|
Cancer
|
|
β-Boswellic acid is isolated from the gum resin of Boswellia serrate.
β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells.
|
-
- HY-10571A
-
|
Delavirdine mesylate
U 90152 mesylate; BHAP-U 90152 mesylate
|
HIV
Reverse Transcriptase
|
Infection
|
|
Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
|
-
- HY-122502
-
|
Pyrazofurin
|
DNA/RNA Synthesis
|
Cancer
|
|
Pyrazofurin, a pyrimidine nucleoside analogue with antineoplastic activity, inhibits cell proliferation and DNA synthesis in cells by inhibiting uridine 5'-phosphate (UMP) synthase. Pyrazofurin is an active, sensitive orotate-phosphoribosyltransferase inhibitor with IC50s between 0.06-0.37 µM in the three squamous cell carcinoma (SCC) cell lines Hep-2, HNSCC-14B and HNSCC-14C.
|
-
- HY-12270
-
|
T-5224
|
MMP
|
Others
|
|
T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
|
-
- HY-10571
-
|
Delavirdine
U 90152; BHAP-U 90152
|
HIV
Reverse Transcriptase
|
Infection
|
|
Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
|
-
- 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-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-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-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-128908
-
-
- HY-126492
-
-
- HY-B0890
-
|
Zomepirac sodium salt
McN-2783-21-98
|
PGE synthase
|
Inflammation/Immunology
|
|
Zomepirac sodium salt (McN-2783-21-98) is a potent prostaglandin biosynthesis inhibitor. Zomepirac sodium salt is a non-steroidal anti-inflammatory drug (NSAID). Zomepirac sodium salt can cause immune-mediated liver injury.
|
-
- HY-100079
-
|
9-Propenyladenine
Mutagenic Impurity of Tenofovir Disoproxil; Tenofovir Impurity 2
|
HIV
|
Infection
|
|
9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase inhibitors, which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
|
-
- HY-B0253
-
|
Piroxicam
CP-16171
|
COX
|
Inflammation/Immunology
Cancer
|
|
Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively.
|
-
- HY-16191
-
|
ELR510444
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
|
-
- HY-16478
-
-
- HY-115066A
-
-
- 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-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-100150
-
-
- HY-B0012A
-
-
- HY-B0523A
-
-
- HY-12770
-
-
- HY-B1382
-
-
- HY-13682
-
-
- HY-B0380A
-
-
- HY-B0380
-
-
- HY-N0118
-
-
- HY-16445A
-
-
- HY-G0010
-
-
- HY-B0301
-
-
- HY-B1370A
-
-
- 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-101070
-
-
- HY-131031
-
|
KCC-07
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
|
-
- HY-130250
-
|
SR-4835
|
CDK
Apoptosis
|
Cancer
|
|
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.
|
-
- HY-10496
-
|
SC75741
|
NF-κB
Influenza Virus
|
Infection
Cancer
|
|
SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65. SC75741 blocks influenza viruses (IV) replication. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins.
|
-
- HY-10221
-
|
Vorinostat
SAHA; Suberoylanilide hydroxamic acid
|
HDAC
Autophagy
Mitophagy
Filovirus
Apoptosis
|
Cancer
Infection
|
|
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
|
-
- HY-B1320
-
|
Meclofenamate sodium
Meclofenamic acid sodium
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Meclofenamic acid sodium is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.
|
-
- HY-17401
-
|
Ranolazine dihydrochloride
CVT 303 dihydrochloride; RS 43285
|
Calcium Channel
Sodium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.
|
-
- HY-125586
-
|
β-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-B0439S1
-
|
Sulfadoxine D3
Sulphadoxine D3
|
Parasite
HIV
Antibiotic
|
Infection
|
|
Sulfadoxine D3 is a deuterium labeled Sulfadoxine. Sulfadoxine is a long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.
|
-
- HY-126693
-
-
- HY-128894
-
-
- HY-100566
-
-
- HY-10392
-
|
Sutezolid
PNU-100480; U-100480; PF-02341272
|
Bacterial
Antibiotic
|
Infection
|
|
Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis.
|
-
- HY-N0842
-
|
Bevirimat
PA-457; MPC-4326; YK FH312
|
HIV
|
Infection
|
|
Bevirimat (PA-457; MPC-4326; YK FH312) is an anti-HIV drug derived from a betulinic acid-like compound; is believed to inhibit HIV by a novel mechanism, so-called maturation inhibition.
|
-
- HY-15435
-
|
CHAPS
|
Others
|
Others
|
|
CHAPS, a derivative of Cholic acid, is a zwitterionic detergent for solubilizing membrane proteins. CHAPS is used for stabilization of various protein-DNA complexes and can retain biochemical activity of proteins in solution.
|
-
- 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-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-B1370B
-
-
- 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-17437A
-
-
- HY-B0421
-
-
- HY-B1016
-
-
- HY-B0803S
-
-
- HY-B0401
-
-
- HY-12771
-
-
- 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-100572
-
-
- HY-129365
-
|
SNPB
|
ADC Linker
|
Cancer
|
|
SNPB is a cleavable linker that is used for making antibody-drug conjugate (ADC).
|
-
- HY-101710
-
-
- HY-121817
-
-
- HY-15579A
-
|
MMAF hydrochloride
Monomethylauristatin F hydrochloride
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A.
|
-
- HY-17485
-
|
Alminoprofen
EB-382
|
Phospholipase
COX
|
Inflammation/Immunology
|
|
Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2.
|
-
- HY-N0618
-
|
Sanggenon D
|
Others
|
Inflammation/Immunology
|
|
Sanggenon D is a Diels-Alder-type adduct from Chinese crude drug root bark of Morus cathayana. Sanggenon D possesses antioxidant and inhibits Pancreatic lipase (PL) with the an IC50 of 0.77 μM.
|
-
- HY-124040
-
|
BI-1950
|
Integrin
|
Inflammation/Immunology
|
|
BI-1950 is a highly potent lymphocyte function associated antigen-1 (LFA-1) inhibitor. LFA-1 is an essential component in normal immune system function and a target for drug discovery.
|
-
- HY-10127
-
|
Barasertib
AZD1152
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.
|
-
- HY-101653
-
|
MHP 133
|
AChE
mAChR
5-HT Receptor
|
Neurological Disease
|
|
MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
|
-
- 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-101925
-
|
CM-272
|
Histone Methyltransferase
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death. Anti-tumour Activity.
|
-
- HY-W000838
-
-
- 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-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-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-B0280
-
|
Ranolazine
CVT 303; RS 43285-003
|
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor.
|
-
- HY-15028
-
|
ATB-346
|
COX
Apoptosis
|
Inflammation/Immunology
|
|
ATB-346 an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2) ATB-346 possesses antiinflammatory and antinociceptive activities.
|
-
- HY-B0128
-
|
Diphylline
Diprophylline
|
Adenosine Receptor
Phosphodiesterase (PDE)
|
Infection
|
|
Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator drug and has the potential for chronic bronchitis and emphysema.
|
-
- HY-126681
-
|
SC-VC-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
SC-VC-PAB-MMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker SC-VC-PAB.
|
-
- HY-126683
-
-
- HY-15575
-
|
VcMMAE
mc-vc-PAB-MMAE
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
|
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
|
-
- HY-100079A
-
|
(Z)-9-Propenyladenine
(Z)-Mutagenic Impurity of Tenofovir Disoproxil
|
HIV
|
Infection
|
|
(Z)-9-Propenyladenine is a mutagenic impurity in tenofovir disoproxil fumarate. Tenofovir is an antiretroviral drug known as nucleotide analogue reverse transcriptase (NtART) inhibitor, which blocks reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.
|
-
- HY-15142
-
-
- 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-B0505
-
-
- HY-B0779
-
-
- HY-19318
-
-
- HY-16216
-
-
- HY-15856B
-
-
- HY-B0992
-
-
- HY-N0666
-
-
- HY-100875
-
-
- HY-B0507A
-
-
- 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-B0270
-
-
- HY-17475
-
-
- HY-B1115
-
-
- HY-B1236
-
-
- HY-B0806S
-
-
- HY-126519
-
-
- HY-W013715A
-
|
Thymidine-5'-triphosphate trisodium salt
dTTP trisodium salt
|
DNA/RNA Synthesis
|
Others
|
|
Thymidine-5'-triphosphate (dTTP) trisodium salt is one of the four natural deoxynucleotides. Thymidine-5'-triphosphate trisodium salt is used for the biosynthesis of deoxyribonucleic acid by DNA polymerase and reverse transcriptase.
|
-
- 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-12803
-
|
Fulvene-5
|
NADPH Oxidase
Reactive Oxygen Species
|
Cancer
|
|
Fulvene-5 is a potent NADPH oxidase 4 (NOX4) inhibitor with antioxidant properties. Fulvene-5 is a reactive oxygen species (ROS) modifying agent and a potent radioprotector. Fulvene-5 has antitumor activity.
|
-
- HY-113914
-
|
9-ING-41
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
|
9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.
|
-
- HY-100195
-
|
SAR-020106
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer drugs.
|
-
- HY-N0498
-
|
Nitidine chloride
|
Parasite
Apoptosis
STAT
Topoisomerase
ERK
FAK
p38 MAPK
NF-κB
|
Cancer
Inflammation/Immunology
|
|
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
|
-
- HY-105028
-
|
Tenidap
CP-66248
|
COX
|
Inflammation/Immunology
|
|
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor.
|
-
- HY-15579B
-
|
MMAF sodium
Monomethylauristatin F sodium
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
MMAF sodium (Monomethylauristatin F sodium) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF sodium (Monomethylauristatin F sodium) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A.
|
-
- HY-15579
-
|
MMAF
Monomethylauristatin F
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A.
|
-
- HY-17361
-
|
Etofenamate
|
Others
|
Inflammation/Immunology
|
|
Etofenamate, a non-steroid anti-inflammatory drug (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Etofenamate is used in the research for osteoarthritis, arthritis and other inflammatory diseases.
|
-
- HY-111012
-
-
- HY-124131
-
|
DS-437
|
Histone Methyltransferase
|
Cancer
Inflammation/Immunology
|
|
DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
|
-
- 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-N2217
-
-
- HY-14771
-
-
- HY-B0101B
-
-
- HY-B0101A
-
-
- HY-129366
-
|
PDB-Pfp
|
ADC Linker
|
Cancer
|
|
PDB-Pfp is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-U00414
-
-
- HY-109111
-
-
- HY-129375
-
-
- HY-44235
-
-
- HY-129373
-
-
- HY-B1196
-
-
- HY-14187
-
-
- 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-14188
-
-
- HY-B0920
-
-
- HY-126667
-
-
- HY-100265
-
-
- HY-B2087S
-
-
- HY-B2087S1
-
-
- HY-10581A
-
|
Gatifloxacin hydrochloride
AM-1155 hydrochloride; BMS-206584 hydrochloride; PD135432 hydrochloride
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-10581B
-
|
Gatifloxacin mesylate
AM-1155 mesylate; BMS-206584 mesylate; PD135432 mesylate
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-B1826
-
|
Adefovir
GS-0393; PMEA
|
HBV
Reverse Transcriptase
|
Infection
|
|
Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses.
|
-
- HY-119447
-
|
Mavacoxib
|
COX
|
Inflammation/Immunology
|
|
Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.
|
-
- HY-111532
-
|
(3R,4R)-A2-32-01
|
Bacterial
|
Infection
|
|
(3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
|
-
- HY-19792
-
|
Mertansine
DM1; Maytansinoid DM1
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
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. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).
|
-
- HY-114395
-
|
NVS-ZP7-4
|
Others
|
Inflammation/Immunology
|
|
NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
|
-
- HY-W010737
-
-
- 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-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-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-W010706
-
|
N4-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxycytidine
5'-O-DMT-N4-Bz-dC
|
Others
|
Others
|
|
N4-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxycytidine (5'-O-DMT-N4-Bz-dC) can be used for synthesis oligodeoxynucleotides containing a 3'-S-phosphorothiolate (3'-PS) linkage. N4-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-2'-deoxycytidine is an useful tool for probing enzyme-catalyzed cleavage processes in DNA.
|
-
- 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-B0682A
-
-
- HY-129368
-
|
SPDMV
|
ADC Linker
|
Cancer
|
|
SPDMV is a glutathione cleavable ADC linker used for the antibody-drug conjugate (ADCs).
|
-
- 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-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-19017
-
-
- 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-B0284
-
-
- HY-126512
-
-
- HY-B0174
-
-
- HY-129370
-
-
- HY-B1104
-
-
- HY-100379
-
-
- HY-128927
-
-
- HY-111354
-
-
- HY-101810
-
-
- HY-126686
-
-
- HY-B1799
-
|
Tolmetin
|
COX
|
Cancer
Inflammation/Immunology
|
|
Tolmetin is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID).
|
-
- HY-19212
-
|
S-2474
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
|
-
- HY-17425
-
|
Valacyclovir
Valaciclovir
|
HSV
Antibiotic
|
Infection
|
|
Valacyclovir (Valaciclovir) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir is a prodrug of Aciclovir (HY-17422) .
|
-
- HY-17425A
-
|
Valacyclovir hydrochloride
Valaciclovir hydrochloride
|
HSV
Antibiotic
|
Infection
|
|
Valacyclovir hydrochloride (Valaciclovir hydrochloride) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir hydrochloride inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir hydrochloride is a prodrug of Aciclovir (HY-17422) .
|
-
- 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-Y0189
-
|
Methyl Salicylate
Wintergreen oil
|
COX
|
Inflammation/Immunology
|
|
Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products. A systemic acquired resistance (SAR) signal in tobacco. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor.
|
-
- HY-N0095
-
|
(S)-10-Hydroxycamptothecin
10-HCPT; 10-Hydroxycamptothecin
|
Topoisomerase
Apoptosis
|
Cancer
|
|
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
|
-
- HY-10581
-
|
Gatifloxacin
AM-1155; BMS-206584; PD135432
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
|
Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-N6937
-
|
(R,R)-Secoisolariciresinol diglucoside
(R,R)-SDG; (R,R)-LGM2605
|
Others
|
Inflammation/Immunology
|
|
(R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) is the minor isomer of Secoisolariciresinol diglucoside in flaxseed. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) possesses antioxidant and free radical scavenging activities and DNA-radioprotective properties. (R,R)-Secoisolariciresinol diglucoside ((R,R)-SDG) inhibits myeloperoxidase (MPO) activity by suppressing both the peroxidase and chlorination cyclesin inflammatory cells.
|
-
- HY-N0769
-
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-B0968
-
|
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-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-117407
-
|
ALLO-2
|
Smo
|
Cancer
|
|
ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
|
-
- HY-130989
-
-
- HY-N6866
-
|
Gomisin N
|
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Gomisin N, isolated from Schisandra chinensis, produces beneficial sedative and hypnotic bioactivity. Gomisin N has the potential for use in the treatment of allergy. Gomisin N is an anti-cancer drug candidate capable of inhibiting the proliferation and inducing the apoptosis in cancer.
|
-
- HY-N6791
-
|
KT5823
|
PKA
PKC
Bacterial
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
|
KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
|
-
- HY-78931
-
|
Boc-Dap-NE
|
ADC Linker
|
Cancer
|
|
Boc-Dap-NE, a dipeptide, is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-136095
-
-
- HY-130111
-
-
- HY-B0306
-
-
- HY-B0139
-
-
- HY-44246
-
-
- 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-104004
-
-
- HY-101151
-
-
- HY-100561
-
-
- HY-128970
-
-
- HY-116270
-
-
- HY-19318A
-
-
- HY-G0001A
-
-
- HY-126349
-
-
- HY-140098
-
-
- HY-129353
-
-
- HY-126496
-
-
- HY-129367
-
-
- HY-14895
-
-
- HY-118759
-
-
- HY-42973
-
-
- HY-133550
-
-
- HY-19318B
-
-
- HY-79584
-
-
- HY-126405
-
|
SMPT
|
ADC Linker
|
Cancer
|
|
SMPT is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-129352
-
-
- HY-133542
-
-
- HY-126531
-
-
- HY-76210
-
-
- HY-136104
-
-
- HY-10932
-
-
- HY-B2141
-
-
- 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-B0568
-
-
- HY-B1613A
-
-
- 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-133590
-
|
Heliotrine N-oxide
|
Others
|
Cancer
|
|
Heliotrine N-oxide is the corresponding PA (pyrrolizidine alkaloid) N-oxide of Heliotrine (HY-126128). Heliotrine N-oxide leads to the formation of pyrrolic DNA adducts and potential initiation of PA-induced liver tumors in vivo.
|
-
- 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-125098
-
|
Illudin S
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
Infection
|
|
Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cell cycle in human leukemia cells.
|
-
- HY-B1489
-
-
- HY-130082
-
|
DM4-SMe
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
|
DM4-SMe is a metabolite of antibody-maytansin conjugates (AMCs) and a tubulin inhibitor, and also a cytotoxic moiety of antibody-drug conjugates (ADCs), which can be linked to antibody through disulfide bond or stable thioether bond. DM4-SMe inhibits KB cells with an IC50 of 0.026 nM.
|
-
- HY-16291
-
|
APTO-253
LOR-253; LT-253
|
c-Myc
KLF
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
APTO-253 (LOR-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. APTO-253 has antiarthritic activity.
|
-
- HY-10581C
-
|
Gatifloxacin sesquihydrate
AM-1155 sesquihydrate; BMS-206584 sesquihydrate; PD135432 sesquihydrate
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-112616
-
|
NAMPT inhibitor-linker 2
|
NAMPT
Drug-Linker Conjugates for ADC
|
Cancer
|
|
NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
|
-
- HY-18071A
-
|
BI-9627 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
|
|
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
|
-
- HY-18071
-
|
BI-9627
|
Sodium Channel
|
Cardiovascular Disease
|
|
BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
|
-
- HY-112853
-
-
- HY-136033
-
-
- HY-140987
-
-
- HY-140313
-
-
- HY-130110
-
-
- HY-140306
-
-
- HY-W019543
-
-
- HY-23641
-
-
- HY-140105
-
-
- 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.
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- HY-140296
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- HY-138327
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- HY-U00148
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- HY-130099
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- HY-135973
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- HY-136032
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- HY-135978
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- HY-135972
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- HY-41189
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- HY-140096
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- HY-126851
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- HY-126518
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- HY-76772A
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- HY-W096127
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- HY-130928
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- HY-N0666C
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- HY-B0206
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- HY-116063
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- HY-128929
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- HY-44221
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- HY-140122
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- HY-135418
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- HY-123687
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- HY-140104
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- HY-19318C
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- HY-A0142A
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- HY-B0967
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Phthalylsulfacetamide
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Bacterial
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Infection
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Phthalylsulfacetamide is a sulfa drug, after oral administration, slowly decompose in the intestine,and release sulfacetamide ,generating antibacterial effect.
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- HY-138506
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- HY-129360
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- HY-126517
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- HY-B0101
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Fluconazole
UK-49858
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Fungal
Antibiotic
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Infection
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Fluconazole (UK-49858) is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.
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- HY-17583
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- HY-B2177
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Apronal
Allylisopropylacetylurea; Apronalide
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Others
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Neurological Disease
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Apronal (Allylisopropylacetylurea, Apronalide) is a hypnotic and sedative drug that has been withdrawn in several countries due to side effects.
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- HY-135977
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- HY-131084
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- HY-101596
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- HY-U00105
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- HY-W011541
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- HY-76772B
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- HY-W002213
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- HY-140129
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- HY-13995
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Sevelamer
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FXR
Autophagy
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Endocrinology
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Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
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- HY-136039
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- HY-79129
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- HY-128920
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Phortress free base
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Cytochrome P450
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Cancer
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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.
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- HY-N2342
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Procyanidin C1
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Apoptosis
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Cancer
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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.
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-
- HY-B0253S
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Piroxicam D3
CP-16171 D3
|
COX
|
Cancer
Inflammation/Immunology
|
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Piroxicam D3 (CP-16171 D3) is deuterium labeled Piroxicam. Piroxicam is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively .
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- HY-B0258
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- HY-19812
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- HY-112615
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NAMPT inhibitor-linker 1
|
NAMPT
Drug-Linker Conjugates for ADC
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Cancer
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NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
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-
- HY-106161
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Rupintrivir
AG7088
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Virus Protease
Enterovirus
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Infection
Inflammation/Immunology
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Rupintrivirvr (AG7088), an antiviral drug, is a potent, selective and irreversible inhibitor of human rhinovirus (HRV) 3C protease. Rupintrivirvr inhibits replication of a panel of 48 different HRV serotypes in H1-HeLA and MRC-5 cell protection assays, with a mean EC50 of 0.023 μM. Rupintrivirvr shows immune-modulatory effect.
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-
- HY-N6779
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Patulin
Terinin
|
Bacterial
Apoptosis
Autophagy
Antibiotic
|
Infection
|
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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 induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.
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- HY-111646
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-
- HY-124697
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BMP signaling agonist sb4
|
TGF-β Receptor
|
Cancer
|
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BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
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-
- HY-B0388
-
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Probucol
DH-581
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Virus Protease
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Metabolic Disease
|
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Probucol (DH-581) is an anti-hyperlipidemic drug by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
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- HY-136138
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-
- HY-B1080
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-
- HY-130112
-
-
- HY-B0735
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-
- HY-13702
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Nilutamide
Nilandron; RU 23908
|
Androgen Receptor
|
Cancer
|
|
Nilutamide (Nilandron) is a non-steroidal anti-androgen drug proposed in the treatment of metastatic prostatic carcinoma.
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- HY-124329
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-
- HY-130935
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- HY-14895A
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-
- HY-101153
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-
- HY-126364
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-
- HY-140138
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-
- HY-B1216
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-
- HY-20336
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Mc-Val-Cit-PABC-PNP
Maleimidocaproyl-L-valine-L-citrulline-p-aminobenzyl alcohol p-nitrophenyl carbonate
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ADC Linker
|
Cancer
|
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Mc-Val-Cit-PABC-PNP is a cathepsin cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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- HY-136102
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-
- HY-140102
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- HY-W023121
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-
- HY-B0735A
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-
- HY-141141
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- HY-117409
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- HY-126524
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- HY-140140
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- HY-130810
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