Search Result
Results for "
compound 17
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-147229
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Ras
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Cancer
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GDC-6036-NH is from patent WO2020097537A2, and a precursor of compound 17 a/b. Compound 17 a/b is a RAS inhibitor and can be used in cancer research .
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- HY-164768
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Integrin
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Cancer
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LT25 (compound 17) is a agonist of α5β1 integrin with EC50 value of 9.9 nM .
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-
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- HY-151231
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Aldose Reductase
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Others
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6-Hydroxyluteolin (Compound 17) is a flavonoid compound. 6-Hydroxyluteolin has an inhibitory effect on aldose reductase (AR) .
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-
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- HY-126787
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YP-02259L-C
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Bacterial
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Infection
Inflammation/Immunology
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17-Hydroxyventuricidin A (YP-02259L-C) is an antimicrobial compound.17-Hydroxyventuricidin A inhibits the growth of the two tested filamentous fungi (Verticillium dahlia and Fusarium sp.) and of Candida tropicalis R2 CIP203 .
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-
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- HY-135619
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-
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- HY-N8602
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Others
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Others
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Ganoderenic acid F (compound 17) is a triterpenoid that can be found in ganoderma lucidum .
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-
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- HY-149895
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Syk
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Cancer
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Syk-IN-7 (compound 17) is an inhibitor of spleen tyrosine kinase (SYK) .
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-
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- HY-148442
-
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MetAP
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Infection
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ecMetAP-IN-1 (compound 17) is a potent ecMetAP inhibitor with an IC50 value of 2.086 µM .
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-
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- HY-158135
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ADC Linker
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Cancer
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Val-Cit-PAB-DEA-COOH (compound 17) is an ADC linker that can be used in the synthesis of ADCs .
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-
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- HY-N10974
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Others
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Others
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Abiesadine Q (compound 17) is a diterpene compound that can be isolated from the aboveground parts of Abies georgei Orr .
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- HY-125872
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Ras
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Cancer
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KRas G12C inhibitor 14 (Compound 17) is a potent KRAS G12C inhibitor (IC50 = 18 nM).
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- HY-N10844
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Others
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Inflammation/Immunology
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Triptohairic acid (compound 17) is nature product that could be isolated from the stems of Tripterygium wilfordii. Triptohairic acid has anti-inflammatory activity .
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-
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- HY-139384
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FAAH
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Neurological Disease
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FAAH inhibitor 2 (Compound 17b) is an irreversible fatty acid amide hydrolase (FAAH) inhibitor, with an IC50 of 0.153 μM .
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-
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- HY-163575
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TDP-43-IN-2
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Amyloid-β
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Neurological Disease
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TDP-43-IN-2 (compound 17) is a TDP-43 inhibitor, and can be used for study of neurodegenerative disease .
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-
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- HY-W011996
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Microtubule/Tubulin
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Cancer
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2-Methylthiophenothiazine (compound 17) is a precursor of tubulin inhibitor with potential anticancer activity and can inhibit tubulin aggregation .
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- HY-144985
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway .
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- HY-155333
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Bacterial
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Infection
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Antibiofilm agent-1 is an antibacterial agent that inhibits growth of Gram-positive pathogens (WO2017011725A1; compound 17) .
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- HY-N1843
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Bacterial
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Infection
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3-Isomangostin hydrate (Compound 17) is an xanthone that can be isolated from Cratoxylum formosum ssp. pruniflorum and exhibits antibacterial activity .
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- HY-138317
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JAK
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Cancer
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Tyk2-IN-10 (compound 17.5) is a tyrosine kinase 2-mediated signaling inhibitor involved in inflammation regulation .
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- HY-160587
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SRPK
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Cardiovascular Disease
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Antiangiogenic agent 5 (compound 17) has anti-angiogenic activity. Antiangiogenic agent 5 show inhibition to SRPK1, with IC50 of 1.3 nM .
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- HY-154839
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c-Myc
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Cancer
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c-Myc inhibitor 10 (compound 17), a c-Myc inhibitor, exhibits increased cellular potency, consistent with an increase in permeability with methylation of the morpholine nitrogen .
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- HY-124790
-
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Kinesin
Mitosis
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Cancer
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KSP-IA (compound 17) is a potent kinesin spindle protein (KSP) inhibitor with an IC50 value of 3.6 nM. KSP-IA inhibits cell mitosis .
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- HY-172607
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Carbonic Anhydrase
|
Infection
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Carbonic anhydrase inhibitor 30 (compound 17) is an inhibitor of carbonic anhydrase with Ki values of 2.13 μM and 0.161 nM for hCA I and hCA II, respectively [1] .
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- HY-160981
-
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ADC Linker
|
Cancer
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Mal-PEG4-VCP-NB (Compound 17) is a degradable ADC linker containing a maleimide group, 4 PEG units and VCP NB .
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- HY-155583A
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DNA/RNA Synthesis
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Infection
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RNase L-IN-1 (compound 17a) trihydrochloride is an inhibitor of RNase L or ribonuclease L. RNase L degrades RNA to prevent viral replication and mediates innate immune responses and inflammation .
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- HY-155583
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DNA/RNA Synthesis
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Infection
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RNase L-IN-1 (compound 17a) is an inhibitor of RNase L, or Ribonuclease L. RNase L degrades RNAs to prevent viral replication, and mediates the innate immune responses and inflammation .
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- HY-168900
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Bacterial
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Infection
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Antibiofilm agent-15 (Compound 17) is an antibacterial agent. Antibiofilm agent-15 inhibits biofilm formation in Gram-positive and Gram-negative bacteria .
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- HY-144258
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PD-1/PD-L1
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Inflammation/Immunology
Cancer
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PD-1/PD-L1-IN-14 (compound 17) is a bifunctional inhibitor of PD-1/PD-L1 interactions, with an IC50 of 27.8 nM. PD-1/PD-L1-IN-14 (compound 17) inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1 .
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- HY-159484
-
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HSP
Guanylate Cyclase
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Cardiovascular Disease
|
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Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression .
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- HY-170312
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Bacterial
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Infection
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Antimicrobial-IN-1 (compound 17) exhibits strong antibacterial activity against S. aureus and E. coli, with the inhibition zone diameter of 18 , 16 mm/mg, respectively .
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- HY-123799
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Raf
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Cardiovascular Disease
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B-699393 (Compound 17) is a BRAF inhibitor (Kd = 7.2 nM) that can cross the blood-brain barrier. SB-699393 can be used for research on stroke .
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- HY-162833
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Parasite
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Infection
|
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Antileishmanial agent-30 (compound 17k) is a potent inhibitor of leishmania, with the IC50, CC50, and SI of 0.2 μM, >100 μM and >500 for L. donovani .
|
-
-
- HY-163152
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-
-
- HY-158241
-
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Bacterial
|
Infection
|
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GmhA-IN-1 (compound 17) is an inhibitor of GmhA with an IC50 value of 2.4 nM. GmhA-IN-1 enhances the activity of erythromycin and rifampicin on wild-type E. coli .
|
-
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- HY-146418
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Flavivirus
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Infection
|
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Antiviral agent 20 (Compound 17b) is a selective inhibitor against Zika virus infection with an EC50 of 4.5 µM. Antiviral agent 20 has low cytotoxicity .
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- HY-N12195
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Fungal
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Infection
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Cytochalasin R (compound 17) is a cytochalasin analogue that can be isolated from the endophytic fungus Phomopsis sp. xz-18. Cytochalasin R shows potential antifungal activity .
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- HY-149015
-
|
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Farnesyl Transferase
|
Cancer
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FTase-IN-1 (compound 17a) is a potent and specific inhibitor of fanesyl transferase (FTase) with an IC50 of 0.35 μM. FTase-IN-1 displays cytotoxicity potential and antitumor activity .
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- HY-175463
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Molecular Glues
Src
|
Cancer
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LCK degrader-2 (Compound 17) is a Lck Molecular glue degrader. LCK degrader-2 can be used for cancers like acute lymphoblastic leukemia (ALL) research .
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-
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- HY-142687
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SGK
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Inflammation/Immunology
|
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SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research .
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- HY-153051
-
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Others
|
Cancer
|
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Antitumor agent-90 (Compound 17) has cytotoxicity against PC 14 cell and MKN 45 cell. Antitumor agent-90 can be used for cancer research .
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-
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- HY-149339
-
|
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NO Synthase
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Neurological Disease
|
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hnNOS-IN-2 (compound 17) is a human neuronal nitric oxide synthase (hnNOS) inhibitor with good metabolic stability. hnNOS-IN-2 can be used for research in neurodegenerative diseases .
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- HY-160502
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PROTACs
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Cancer
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CST967 (Compound 17) is a USP7 PROTAC degrader, and increasing the PROTAC concentration can enhance the degradation rate of USP7. CST967 can be used in cancer research .
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- HY-N12035
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Others
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Cancer
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Picropodophyllin-4-O-β-D-glucopyranosyl-(1→6)-β-D-glucopyranoside (compound 17) is a lignan isolated from the roots and rhizomes of Podophyllum sinensis .
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- HY-130049
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Bacterial
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Infection
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Lucidin ω-ethyl ether (compound 17) is an anthraquinone metabolite isolated from the root part of Prismatomeris filamentosa with some antibacterial activity against Gram-positive and Gram-negative bacteria .
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- HY-153262
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(7R)-D3S-001
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Ras
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Cancer
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KRASG12C IN-2 (compound 17) is an orally active KRAS G12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice .
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- HY-162244
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COX
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Inflammation/Immunology
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COX-2-IN-40 (compound 17) is a COX-2 inhibitor with the IC50 of 14.86 μM. COX-2-IN-40 can be used for study of chronic pain .
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- HY-170617
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STING
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Inflammation/Immunology
|
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hSTING agonist-1 (compound 17) is a potent agonist of hSTING. hSTING agonist-1 has poor oral availability. hSTING agonist-1 plays an important role in inflammation research .
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- HY-170830
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Bacterial
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Infection
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Mtb against-1 (compound 17af) is an inhibitor of Mycobacterium tuberculosis, with IC90 values of 1.2 μM and 0.9 μM for the wild-type and LepB low-deformation strains, respectively .
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- HY-161920
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Sirtuin
Apoptosis
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Cancer
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SIRT3-IN-1 (compound 17f) is a SIRT3 inhibitor, with IC50 of 0.043 μM. SIRT3-IN-1 can be used in the research of acute leukemia (AML) .
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- HY-143460
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Carbonic Anhydrase
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Cancer
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CAXII-IN-1 (Compound 17) is a selective CA XII inhibitor with Ki values of 3.8 nM and 56.0 nM against hCA XII and hCA IX, respectively. CAXII-IN-1 shows antitumor activity .
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- HY-W713855
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Bacterial
Folate Receptor (FR)
|
Infection
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(4-Aminobenzoyl)-D-glutamic acid (Compound 17) exhibits competitive inhibitory activity against H2-pteroate synthesis system, which affects the synthesis of folate, thereby inhibiting growth of bacteria .
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- HY-153761
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- HY-151372
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PKD
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Cancer
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Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC50 values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation .
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- HY-156175
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Toll-like Receptor (TLR)
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Inflammation/Immunology
|
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TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations .
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- HY-172794
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Insecticide
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Infection
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Insecticidal agent 23 (compound 17) has antischistosomal efficacy and low toxicity. Insecticidal agent 23 exhibits potent in vitro activity against adult S. japonicum, with an LC50 (72 h) value of 25.31 μM.
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- HY-161093
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PROTACs
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Cancer
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PROTAC BRD4 Degrader-23 (compound 17) is an
effective visible-light-controlled degrader. PROTAC BRD4 Degrader-23 can
inhibit tumor cell proliferation under 405 nm light irradiation .
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- HY-149650
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- HY-134596
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E1/E2/E3 Enzyme
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Cancer
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SENP1-IN-3 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 17. SENP1-IN-3 is developed for tumor radiosensitivity enhancement .
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- HY-149869
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PSMA
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Cancer
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PSMA-IN-3 (compound 17) is a novel high-affinity PSMA inhibitor with an IC50 value of 13 nM. PSMA-IN-3 is suitable for developing an 18F-labeled radioligand for PET imaging of PSMA in prostate cancer .
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- HY-149650A
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- HY-171981
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mAChR
|
Neurological Disease
|
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VU6002703 (Compound 17) is a BBB-penetrable M4 mAChR positive allosteric modulator (PAM) with an EC50 of 0.6 μM for hM4. VU6002703 can be used for neuropsychiatric and rare genetic CNS disorders research .
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- HY-50862
-
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Akt
|
Cancer
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Akt1/Akt2-IN-1 (Compound 17) is an allosteric inhibitor of Akt1 (IC50=3.5 nM) and Akt2 (IC50=42 nM), with potent and balanced activity .
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- HY-15214
-
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Histone Methyltransferase
|
Cancer
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CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
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- HY-15214A
-
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Histone Methyltransferase
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Cancer
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CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
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- HY-125012
-
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MAP4K
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Metabolic Disease
|
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MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay. Antidiabetic agent .
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- HY-174237
-
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Epigenetic Reader Domain
|
Cancer
|
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PBRM1/SMARCA2,4 binder-1 (Compound 17) is a binder of PBRM1, SMARCA2, and SMARCA4 (IC50: 0.083, 0.153, and 0.046 μM, respectively) .
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- HY-147726
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability .
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- HY-155547
-
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HBV
|
Infection
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HBV-IN-34 (compound 17i) is a potent HBsAg production inhibitor. HBV-IN-34 exhibits excellent in vitro anti-HBV potency, with an EC50 of 0.018 μM and 0.044 μM for HBV DNA and HBsAg, respectively .
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- HY-173394
-
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Carbonic Anhydrase
Apoptosis
|
Cancer
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hCAIX/XII-IN-15 (Compound 17β) is an inhibitor of hCA IX and hCA XII, with Kis of 0.42 and 4.37 μM respectively. hCAIX/XII-IN-15 has pro-apoptotic effect in multiple myeloma cells .
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- HY-161443
-
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YAP
|
Cancer
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TEAD-IN-9 (compound 17) is a TEAD1 inhibitor with an IC50 of 0.29 μM. TEAD-IN-9 targets the palmitoyl pocket of TEAD, thereby effectively inhibiting the binding of YAP-TEAD and blocking the transcriptional function of YAP-TEAD .
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- HY-170504
-
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SARS-CoV
Virus Protease
|
Infection
|
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ZHAWOC25153 (Compound 17o) is a SARS-CoV-2 papain-like cysteine protease (PLpro) inhibitor, with an IC50 of 7 μM. ZHAWOC25153 exhibits antiviral activity and can be used in research within the field of anti-infection .
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- HY-138971
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17,18-EEQ-EA; (±)17,18-EEQ-ethanolamide; (±)17(18)-EpETE-EA
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Interleukin Related
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Others
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(±)17(18)-EpETE-ethanolamide (17,18-EEQ-EA) (compound 17) is an ω-3 endocannabinoid epoxide with cytokine modulation in neuroinflammation studies, antiangiogenic effects in vascular endothelial cells, and vasodilatory effects on coronary arteries.
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- HY-155722
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Bacterial
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Infection
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Mtb-IN-5 (compound (-)17j) is an isoxazole, with anti-Mycobacterium tuberculosis (Mtb) activity. Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant .
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- HY-157222
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Apoptosis
Ferroptosis
|
Cancer
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Antitumor agent-125 (compound 17A) is a novel platinum(IV) prodrug. Antitumor agent-125 can activate the mitochondrion-dependent apoptosis pathway. Antitumor agent-125 induces ferroptosis in HCT-116/OXA .
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- HY-147775
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Ceramidase
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Inflammation/Immunology
|
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NAAA-IN-3 (Compound 17a) is a potent and selective inhibitor of NAAA with an IC50 of 50 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-3 has the potential for the research of inflammation and pain .
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- HY-173073
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Insecticide
nAChR
|
Infection
|
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Insecticidal agent 20 (Compound 17) is an insecticide that can bind to AChBP. Insecticidal agent 20 exhibits good insecticidal activity against the larvae (LC50: 1.57 ppm) and pupae (LC50: 4.17 ppm) of Culex pipiens .
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- HY-147987
-
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Free Fatty Acid Receptor
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Metabolic Disease
|
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FFA1 agonist-1 (Compound 17a) is an orally active fatty acid receptor 1 (FFA1) agonist with an EC50 of 0.75 μM. FFA1 agonist-1 can be used for type 2 diabetes mellitus research .
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- HY-147011
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Fat Mass and Obesity-associated Protein (FTO)
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Cancer
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FTO-IN-7 (compound 17) is an inhibitor of FTO (fat mass and obesity-associated protein) with an IC50 of <1 μM. FTO-IN-7 can be used for the study of small-cell lung cancers and human bone marrow striated muscle cancer .
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- HY-161891
-
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EGFR
Akt
|
Cancer
|
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EGFR/Akt-IN-1 (compound 17) is a potent inhibitor of EGFR/Akt, with the IC50s of 12.89 μM and 10.88 μM in A549 cells, respectively. EGFR/Akt-IN-1 arrestes the cell cycle at the S phase .
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- HY-163376
-
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17-CF3PTPG2α EA
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Prostaglandin Receptor
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Metabolic Disease
|
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17-Trifluoromethylphenyl trinor prostaglandin F2α ethyl amide (compound 17-CF3PTPG2α EA) is a lipophilic analog of 17-trifluoromethylphenyl trinor PGF2α .
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- HY-149849
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Thymidylate Synthase
|
Cancer
|
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TS-IN-2 (compound 17) is a thymidylate synthase (TS) inhibitor with an IC50 of 0.81 μM. TS-IN-2 induces cancer cell apoptosis and cell cycle arrest in S phase, and also inhibit DNA synthesis, resulting in DNA damage .
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- HY-147724
-
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Microtubule/Tubulin
|
Cancer
|
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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-
- HY-157326
-
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Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-6 (compound 17d) is a potent and selective inhibitor of hMAO-B with an IC50 of 67.02 nM. hMAO-B-IN-6 significantly improves Scopolamine (HY-N0296)-induced cognitive impairment in AD mice .
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-
- HY-146457
-
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Adenosine Receptor
|
Inflammation/Immunology
|
|
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations .
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- HY-147728
-
|
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Microtubule/Tubulin
|
Cancer
|
|
Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
|
-
- HY-149016
-
|
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Microtubule/Tubulin
Farnesyl Transferase
|
Cancer
|
|
Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity .
|
-
- HY-177041
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-35 (Compound 17) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-35 can be studied in anticancer research. (Pink: BRD4 ligand (HY-78695); Black: linker; Blue: ligase) .
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-
- HY-114300
-
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GABA Receptor
|
Neurological Disease
|
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DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic agent (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin .
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-
- HY-15357
-
|
|
Anaplastic lymphoma kinase (ALK)
FAK
|
Cancer
|
|
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM) .
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-
- HY-175280
-
|
|
Molecular Glues
Src
|
Cancer
|
|
Lck degrader-1 (Compound 17) is a molecular glue degrader targeting lymphocyte-specific protein tyrosine kinase (LCK) (DC50=23.1 nM). Lck degrader-1 is promising for research of T-cell acute lymphoblastic leukemia (T-ALL) .
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-
- HY-147895
-
|
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase .
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-
- HY-161180
-
|
|
NAMPT
|
Cancer
|
|
Antitumor Agent-136 (Compound 17) is a potent broad-spectrum antitumor agent and a NAMPT inhibitor with an IC50 of 9.5 nM. Antitumor Agent-136 can reduce the levels of intracellular and extracellular NAMPT protein through the ubiquitin proteasome pathway, thus achieving tumor inhibition .
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-
- HY-157477
-
|
|
SARS-CoV
Cathepsin
|
Infection
|
|
SARS-CoV-2 3CLpro-IN-22 (Compound 17) is a cathepsin L (CTSL ) inhibitor with an IC50 value of 32.5 nM. SARS-CoV-2 3CLpro-IN-22 can be used for the study of SARS-CoV-2 virus .
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-
- HY-161861
-
|
|
VEGFR
Akt
|
Cancer
|
|
VEGFR-2/AKT-IN-1 (compound 17) is a dual inhibitor of VEGFR-2 and AKT, with the IC50s of 0.164 μM and 0.452 μM, respectively. VEGFR-2/AKT-IN-1 has antitumor activity .
|
-
- HY-157563
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D4 receptor ligand 2 (compound 17) is a potent and selective dopamine D4 ligand with IC50 values of 0.057, >1000, 220, 270 nM for D4, D2, 5-HT1A, α1, respectively .
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-
- HY-157990
-
|
|
Wnt
β-catenin
|
Cancer
|
|
Wnt/β-catenin-in-1 (compounds 17) is a Wnt/β-catenin signaling pathway inhibitor. Wnt/β-catenin-IN-1 can induce apoptosis of colon cancer cells, has broad-spectrum anticancer activity, and can be used for the reseach of a variety of solid tumors .
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-
- HY-143409
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 10 (Compound 17b) is an aminoalcohol quinoline compound. Antimalarial agent 10 is an antimalarial agent with IC50 values of 14.9 nM and 11.0 nM against respectively Pf3D7 and PfW2 and a selectivity index higher than 770 whatever the cell line is .
|
-
- HY-138996
-
|
|
GCGR
|
Metabolic Disease
|
|
GLP-1 receptor agonist 8 is a potent agonist of GLP-1 R. GLP-1 receptor agonist 8 has the potential for the research of diabetes, obesity, and nonalcoholic fatty liver disease (NAFLD) (extracted from patent WO2019239319A1, compound 17) .
|
-
- HY-162026
-
|
|
11β-HSD
|
Metabolic Disease
|
|
11β-HSD1-IN-14 (Compound 17) is a selective inhibitor for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1), with IC50 of 74 nM for human HSD1, and 603 nM for HSD1 expressed HEK293 cell .
|
-
- HY-169651
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABA-IN-4 (Compound 17) is a N-(indol-3-ylglyoxylyl)benzylamine derivative. GABA-IN-4 exhibits high affinity for the benzodiazepine receptor (BzR) (binding site in GABAA receptor complex) with Ki value of 67 nM. Benzodiazepines are widely used as antianxiety, sedative-hypnotic and anticonvulsant agents .
|
-
- HY-142777
-
|
|
Phospholipase
|
Neurological Disease
|
|
Lp-PLA2-IN-9 (compound 17), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.1 for rhLp-PLA2. Lp-PLA2-IN-9 has the potential for neurodegenerative related diseases research .
|
-
- HY-155720
-
|
|
Bacterial
|
Infection
|
|
Mtb-IN-4 (compound 17h) is a nontoxic isoxazole, with anti-Mycobacterium tuberculosis (Mtb) activity (IC50=0.70 μM). Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant .
|
-
- HY-163430
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-71 (Compound 17q) is a potent HDAC inhibitor with IC50 values of 12.6, 14.1, 20, 3, and 72 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC10, respectively. HDAC-IN-71 induces apoptosis and can be used in cancer research .
|
-
- HY-151386
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-13 (Compound 17c) is an orally active, potent and selective Butyrylcholinesterase (BChE) inhibitor with IC50s of 0.22 and 0.016 μM for eqBChE and hBChE, respectively. BChE-IN-13 can improve memory and cognitive impairments, and be used in Alzheimer’s disease (AD) research .
|
-
- HY-146699
-
|
|
Bacterial
Thymidylate Synthase
|
Infection
|
|
MtTMPK-IN-5 (compound 17) is a potent M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 34 μM. MtTMPK-IN-5 combines favorable enzyme inhibitory activity with significant activity against M. tuberculosis (MIC = 12.5 μM). MtTMPK-IN-5 can be used for researching tuberculosis .
|
-
- HY-148315
-
|
|
GLUT
|
Infection
|
|
GLUT1-IN-2 (compound 17) is a GLUT1 inhibitor with an IC50 value of 12 μM. GLUT1-IN-2 shows inhibitory effect to Plasmodium falciparum hexose transporter PfHT with an IC50 value of 13 μM. GLUT1-IN-2 can be used for the research of infection .
|
-
- HY-155739
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-173120
-
|
|
HBV
|
Infection
|
|
HBV-IN-51 (Compound 17e) is a potent HBV capsid assembly modulator. HBV-IN-51 exhibits remarkable anti-HBV activity with an EC50 of 0.033 μM in HepAD38 cells. HBV-IN-51 exhibits robust metabolic stability in plasma, and can be rapidly metabolized in human liver microsomes .
|
-
- HY-118696
-
|
|
GABA Receptor
|
Neurological Disease
|
|
MGAT2-IN-5 (Compound 17b) is a selective inhibitor for mouse GABA transit protection subsidity 2 (mGAT2) with an IC50 of 45 μM. MGAT2-IN-5 exhibits anticonvulsive efficacy in audiogenic seizure (AGS) susceptible frings mouse model with an ED50 of 20.4 mg/kg .
|
-
- HY-176534
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-52 (Compound 17) is a non-nucleoside Protein Arginine Methyltransferase 5 (PRMT5) inhibitor with inhibitory rates of 20.2% at 10 μM. PRMT5-IN-52 has potent antitumor activity, promising for research of cancers, including lung, prostate cancer, and colorectal carcinoma .
|
-
- HY-144309
-
|
|
Cytochrome P450
|
Neurological Disease
|
|
Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier .
|
-
- HY-154972
-
|
|
Glycosidase
Amylases
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-3 (Compound 17) is an α-Amylase/α-Glucosidase dual inhibitor, with IC50s of 0.70 μM and 1.10 μM. α-Amylase/α-Glucosidase-IN-3 can be used for research of type-II diabetes mellitus .
|
-
- HY-147684
-
|
|
FGFR
|
Neurological Disease
|
|
FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research .
|
-
- HY-155742
-
|
|
CFTR
|
Others
|
|
CFTR corrector 12 (compound 17C) is a bithiazole derivative, serving as CFTR corrector. CFTR corrector 12 has the ability to correct some folding defective mutants of the channel responsible for the control of chloride transport across the plasma membrane. CFTR corrector 12 recovers the α-sarcoglycan (α-SG) content in mutant cells .
|
-
- HY-151248
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM . HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively .
|
-
- HY-163339
-
|
|
Beta-lactamase
|
Infection
|
|
Metallo-β-lactamase-IN-14 (Compound 17e) is a Metallo-β-Lactamase inhibitor. Metallo-β-lactamase-IN-14 shows inhibition activity against VIM-1 and VIM-2. Metallo-β-lactamase-IN-14 has antibacterial activity against Gram-negative (GN) bacteria and P. aeruginosa .
|
-
- HY-148129
-
|
TRPC6-IN-3
|
TRP Channel
|
Cardiovascular Disease
|
|
Apecotrep (TRPC6-IN-3) (compound 17) is a potent, orally active transient receptor potential C6 ion channel (TRPC6) inhibitor. Apecotrep modulates not only intracellular calcium concentration, but also membrane potential by modulating the flux of cations including calcium and sodium ions. Apecotrep can be used in research of respiratory system .
|
-
- HY-143326
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 83 (compound 17h) displays potent antibacterial activity against various vancomycin-resistant Enterococcus faecalis (VRE) and methicillin-resistant Staphylococcus aureus (MRSA). Antibacterial agent 83 can significantly reduce the biofilm formation of MRSA and exhibited promising selectivity. Antibacterial agent 83 is metabolically stable in human liver microsomes .
|
-
- HY-150549
-
|
|
HIV Protease
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus .
|
-
- HY-163690
-
|
|
Ser/Thr Protease
|
Inflammation/Immunology
|
|
HTRA1-IN-1 (Compound 17) is a selective inhibitor for serine protease high temperature requirement A serine peptidase 1 (HTRA1), with IC50 of 13 nM. HTRA1-IN-1 is potential for ameliorating HTRA1-related diseases, such as age-related macular degeneration (AMD), osteoarthritis, and rheumatoid arthritis .
|
-
- HY-144096
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activities of EZH2 have been shown by a number of studies in various different cancer types. EZH2-IN-11 has the potential for the research of cancer diseases (extracted from patent WO2019204490A1, compound 17) .
|
-
- HY-147727
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization .
|
-
- HY-145823
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-42 (Compound 17b) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-42 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-42 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-42 has superior anti-cancer activity .
|
-
- HY-157615
-
|
|
17β-HSD
|
Metabolic Disease
|
|
HSD17B13-IN-6(Compound 475) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of 0.01 μM. HSD17B13-IN-6can be used in the research of liver diseases .
|
-
- HY-100864
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM) .
|
-
- HY-175441
-
|
|
Carbonic Anhydrase
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Carbonic anhydrase activator 1 (Compound 17) is an orally active and a BBB-penetrable Carbonic anhydrase (CA) activator with KAs of 7.8, 3.9 and 2.1 μM for hCA I, hCA VA and hCA VII. Carbonic anhydrase activator 1 can be used for cancers, glaucoma, cardiovascular diseases and neurodegenerative disorders like epilepsy research .
|
-
- HY-145824
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-43 (Compound 17c) is a potent inhibitor of EGFR with single-digit nanomolar activity. EGFR-IN-43 connects tamoxifen or endoxifen with the EGFR-inhibitor gefitinib via a covalent linkage. EGFR-IN-43 retains both ER antagonist activity and EGFR inhibition. EGFR-IN-43 has superior anti-cancer activity .
|
-
- HY-158158
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC50= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines .
|
-
- HY-162255
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC50 = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer .
|
-
- HY-163027
-
|
|
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
|
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research .
|
-
- HY-161373
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .
|
-
- HY-142937
-
|
|
ROR
|
Inflammation/Immunology
|
|
RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17) .
|
-
- HY-Q36691
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.33 μM and a Kd of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation .
|
-
- HY-149099
-
|
|
RET
|
Cancer
|
|
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
|
-
- HY-175467
-
|
|
HSP
HDAC
|
Cancer
|
|
HDAC6/HSP90-IN-3 (Compound 17) is an orally active dual histone deacetylase 6 (HDAC6) and heat shock protein 90 (HSP90) inhibitor with IC50 values of 28 nM and 0.88 μM, respectively. HDAC6/HSP90-IN-3 is promising for research of malignant tumors such as prostate cancer .
|
-
- HY-151363
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 μM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis .
|
-
- HY-162032
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-25 (compound 17) is a potent inhibitor of FLT3, with IC50s of 1.2 nM, 1.4 nM and 1.1 nM for FLT3-WT, FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-25 plays an important role in acute myeloid leukemia (AML) .
|
-
- HY-158210
-
|
|
Wnt
β-catenin
MDM-2/p53
|
Cancer
|
|
Wnt/β-catenin-IN-3 (compound 17) is a Wnt/β-catenin inhibitor with low micromolarGI50s against various cancer cells. Wnt/β-catenin-IN-3triggers G2/M cell cycle arrest though activation of p53-p21 pathway as well as intrinsic and extrinsic apoptotic death of colon cancer cells .
|
-
- HY-146239
-
|
|
EGFR
Thymidylate Synthase
|
Cancer
|
|
EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM .
|
-
- HY-146165
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible and competitive broad-spectrum inhibitor of metallo-β-lactamases (MβLs), with IC50s of 1.3 μM, 5.7 μM, 9.8 μM, and 9.9 μM for L1, ImiS, IMP-1 and VIM-2, respectively. Metallo-β-lactamase-IN-8 exhibits antibacterial activity .
|
-
- HY-W181102
-
|
|
Calcineurin
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signalling. Calcineurin is a serine/threonine protein phosphatase regulated by Ca2+ and calmodulin. NFAT Inhibitor-2 has the potential for the research of inflammatory disease, an autoimmune disorder, a cardiovascular disease, a neurodegenerative disease, a disease occurring with uncontrolled cell proliferation and/or differentiation, an angiogenesis-related disease, an allergy, anaphylaxis and alopecia (extracted from patent WO2016207212A1, compound 17) .
|
-
- HY-151337
-
-
- HY-153676
-
|
|
RET
|
Cancer
|
|
RET-IN-23 (compound 17) is a potent and orally active RET inhibitor with IC50 values of 1.32, 2.50, 6.54, 1.03, 1.47 nM for RET-WT, RET-CCDC6, RET-V804L, RET-V804M, RET-M918T, respectively. RET-IN-23 shows anti-tumor activity .
|
-
- HY-144652
-
-
- HY-149431
-
|
|
HSP
Potassium Channel
|
Cancer
|
|
NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
|
-
- HY-163245
-
|
|
17β-HSD
|
Metabolic Disease
|
|
HSD17B13-IN-32(Compound 67) is an inhibitor of hydroxysteroid 17β-dehydrogenase 13 (HSD17B13) with an IC50 value of ≤ 0.1 μM for estradiol. HSD17B13-IN-32can be used for research on liver diseases, metabolic diseases, or cardiovascular diseases, such as NAFLD or NASH, as well as drug-induced liver injury (DILI) .
|
-
- HY-174818
-
-
- HY-161221
-
|
|
17β-HSD
|
Metabolic Disease
|
|
HSD17B13-IN-21 (compound 17) is a ppotent inhibitor of hydroxysteroid 17?-dehydrogenase 13 (HSD17B13), with the IC50 of ＜ 0.1 μM and? ＜ 1 μM estradiol and Leukotriene B3 as substrates, respectively. HSD17B13-IN-21? plays an important role in nonalcoholic fatty liver diseases (NAFLDs) including NASH (nonalcoholic steatohepatitis) .
|
-
- HY-144765
-
|
|
NF-κB
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research .
|
-
- HY-131050
-
|
|
Bacterial
Fungal
|
Infection
|
|
Aspergillus niger-IN-1 (Compound 17), a derivative of thiazolidine-2,4-dione, acts as an antimicrobial agent. Aspergillus niger-IN-1 exhibited antimicrobial activity against various bacterial and fungal strains, including Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumonia, Escherichia coli, Salmonella typhi, Candida albicans and Aspergillus niger, with MIC values of 11.3, 5.65, 11.3, 5.65, 5.65, 5.65, and 5.65 μM/mL, respectively .
|
-
- HY-146098
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Antibacterial agent 105 (Compound 17) is a phenanthrolinic analog of quinolones show antibacterial activity against M. tuberculosis with antibacterial activity (MIC90=2.64 μM). Antibacterial agent 105 exhibits antibacterial activities against different bacterial species with MIC90s of 11.18, 11.18, 0.70, 1.40, 44.70, and 22.35 μM for M. smegmatis, M. aurum, M. marinum, BCG, E. aerogenes and S. aureus, respectively .
|
-
- HY-176860
-
-
- HY-144710
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-170838
-
|
|
PDHK
|
Cancer
|
|
PDHK1-IN-1 (compound 17) is a selective inhibitor of PDHK1 (IC50=1.5 μM) with anticancer activity. PDHK1 negatively regulates the pyruvate dehydrogenase complex (PDC), limiting the tricarboxylic acid (TCA) cycle and oxidative phosphorylation. Overexpression of PDHK1 can shift the metabolism towards an increased glycolysis dependence (Warburg effect). PDHK1-IN-1 can inhibit the phosphorylation of the PDC E1α Ser232 recognition site of PDHK1 and the phosphorylation of Ser293 .
|
-
- HY-163512
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body .
|
-
- HY-163765
-
|
|
PI4K
Potassium Channel
|
Infection
|
|
Antimalarial agent 41 (Compound 17) exhibits antimalarial activity, which inhibits Plasmodium falciparum with an IC50 of 40 nM (NF54 strain) and 76 nM (K1 strain). Antimalarial agent 41 is an inhibitor for P. falciparum phosphatidylinositol-4-kinase β (Pf PI4K) and hERG channel, with an IC50 of 53 nM and 3 μM. Antimalarial agent 41 exhibits cytotoxicity to CHO cells with an IC50 of 34 μM. Antimalarial agent 41 ameliorates the malaria infection and exhibits good pharmacokinetic characters in mouse models .
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- HY-159091
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HIV Integrase
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Infection
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HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
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- HY-172919
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Phosphodiesterase (PDE)
NAMPT
Apoptosis
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Cancer
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PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD +), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer .
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- HY-N1870
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Bacterial
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Others
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1β-Hydroxy-4(15),5E,10(14)-germacratriene (compound 17) is a sesquiterpenoids that can be isolated from Chrysanthemum indicum.1β-Hydroxy-4(15),5E,10(14)-germacratriene significantly reduces PEDV nucleocapsid and spike protein synthesis.1β-Hydroxy-4(15),5E,10(14)-germacratriene shows various biological properties, such as antibacterial, antioxidant, and anti-inflammatory .
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- HY-132138A
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DNA/RNA Synthesis
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Others
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5-Propargylamino-3'-azidomethyl-dCTP (TEA) is a nucleotide molecule that can be used in DNA synthesis and DNA sequencing. For detailed information, refer to compound 17 in patent document WO2004018497A2. 5-Propargylamino-3'-azidomethyl-dCTP (TEA) is a click chemistry reagent containing an azide group, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also react with molecules containing DBCO or BCN groups through strain-promoted alkyne-azide cycloaddition (SPAAC) .
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- HY-146293
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HDAC
HSP
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Cancer
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HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
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- HY-178495
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Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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SDH-IN-36 (Compound 17) is a derivative of alpha-D-tocopherol. SDH-IN-36 increases ROS and induces apoptosis by inhibiting SDHC and blocking electron transfer. SDH-IN-36 can inhibit the proliferation of various tumor cells, such as SSK4 (GI50 = 0.156 µM), SSNU638 (GI50 = 0.659 µM), and SKATOIII (GI50 = 0.490 µM) cells. SDH-IN-36 can significantly inhibit tumor growth. SDH-IN-36 can be used for research on cancers such as gastric cancer .
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- HY-172915
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MDM-2/p53
Apoptosis
Checkpoint Kinase (Chk)
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Cancer
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p53 Stabilizer 2 (Compound 17a16) is a p53 stabilizer. p53 Stabilizer 2 induces S-phase arrest and apoptosis in both p53-proficient and p53-deficient cancer cells. p53 Stabilizer 2 induces mitochondrial stress and activates two checkpoint pathways: NA-PKcs-dependent p53 stabilization and ATR-Chk1 axis activation. p53 Stabilizer 2 inhibits tumor growth in p53-deficient xenograft model .
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- HY-132138
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DNA/RNA Synthesis
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Others
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5-Propargylamino-3'-azidomethyl-dCTP is a nucleoside molecule extracted from patent WO2004018497A2, compound 17. 5-Propargylamino-3'-azidomethyl-dCTP can be used in DNA synthesis and DNA sequencing . 5-Propargylamino-3'-azidomethyl-dCTP is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-172359
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PROTACs
HDAC
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Cancer
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PROTAC HDAC6 degrader 4 (Compound 17c) is the PROTAC degrader for HDAC6 with a DC50 of 14 nM. PROTAC HDAC6 degrader 4 exhibits inhibitory activit against HDAC1, HDAC2, HDAC3 and HDAC6 with IC50s of 2.2, 2.37, 0.61 and 0.295 μM, respectively . (Pink: ligand for target protein HDAC6 ligand-3 (HY-172360); Black: linker (HY-138387); Blue: ligand for cereblon E3 ligase (HY-W093272))
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- HY-150610
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EGFR
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Cancer
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EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC50 values of 4.3, 6.6 and 25.6 nM against EGFR L858R/T790M/C797S, EGFR L858R/T790M, and EGFR 19del/T790M/C797S, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research .
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- HY-150652
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FGFR
Apoptosis
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Cancer
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FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities .
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- HY-168338
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Cannabinoid Receptor
Caspase
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Cancer
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CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoid receptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC50s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87 .
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- HY-162924
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SARS-CoV
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Infection
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SARS-CoV-IN-6 (Compound 17) is an inhibitor of SARS-CoV-1 and SARS-CoV-2 RdRp, with an IC50 value of 7.8 μM against SARS-CoV-2 RdRp. SARS-CoV-IN-6 reduces cytopathic effects in cells infected with SARS-CoV-1 and SARS-CoV-2 replicon-based single-round infectious particles (SRIPs), and inhibits SARS-CoV N protein expression, with EC50 values of 0.12 µM for SARS-CoV-1 replicon-based SRIPs and 1.47 µM for SARS-CoV-2 replicon-based SRIPs .
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- HY-176847
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Orphan Nuclear Receptor
Apoptosis
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Cancer
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HNF4A-IN-1 (Compound 17) is a Hepatocyte nuclear factor 4 alpha (HNF4A) inhibitor. HNF4A-IN-1 has potent anticancer activity against human head and neck squamous cells (SCC131 cells) and with no toxicity to normal cells. HNF4A-IN-1 significantly inhibits SCC131 cells growth with an IC50 of 1.75 μM, and induces apoptosis and G2/M cell cycle arrest. HNF4A-IN-1 promotes tumor regression in SCC131 tumor xenografts mouse models .
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- HY-175041
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Glutathione Peroxidase
Reactive Oxygen Species (ROS)
Cannabinoid Receptor
Ferroptosis
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Cancer
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GPX4-IN-18 (Compound 17) is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4). GPX4-IN-18 is also an inducer of ferroptosis. GPX4-IN-18 can increase the production of ROS and malondialdehyde (MDA) levels in OS-RC-2 clear cell renal cell carcinoma cells. GPX4-IN-18 induces ferroptosis in HT-1080 cells with IC50s of 0.007 μM (absence of ferrostatin-1) and 1.486 μM (presence of ferrostatin-1). GPX4-IN-18 reduces in vivo tumor volume and intratumoral GPX4 levels in OS-RC-2 xenograft murine model .
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- HY-172886
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PI3K
Bcl-2 Family
Apoptosis
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Cancer
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PI3K-IN-58 (Compound 17f) is a PI3Kα inhibitor (IC50: 0.039 μM). PI3K-IN-58 exhibits significant antiproliferative effects on PC-3, 22RV1, MDA-MB-231 and MDA-MB-453 cell lines with IC50s of 3.48 μM, 1.06 μM, 2.21 μM and 0.93 μM, respectively. PI3K-IN-58 induces apoptosis by downregulating the expression levels of anti-apoptotic proteins Bcl-XL and Bcl-2 and upregulating the expression of anti-apoptosis protein BAX. PI3K-IN-58 can be used in PI3K-targeted cancer research .
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- HY-179015
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17β-HSD
PPAR
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Metabolic Disease
Inflammation/Immunology
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HSD17B13/PPAR modulator-1 (Compound 17) is a HSD17B13/PPAR multitarget modulator. HSD17B13/PPAR modulator-1 is an inhibitor of HSD17B13, with its IC50 value being 0.91 μM. HSD17B13/PPAR modulator-1 is a PPAR agonist, with the EC50 values for PPARα, PPARδ, and PPARγ being 1.55, 0.12, and 0.01 μM respectively. HSD17B13/PPAR modulator-1 can significantly improve liver function, regulate lipid metabolism, alleviate fibrosis, and exert antioxidant and anti-inflammatory effects in the model of metabolic dysfunction-related steatohepatitis (MASH). HSD17B13/PPAR modulator-1 can be used for the study of MASH .
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| Cat. No. |
Product Name |
Type |
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- HY-132138
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Gene Sequencing and Synthesis
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5-Propargylamino-3'-azidomethyl-dCTP is a nucleoside molecule extracted from patent WO2004018497A2, compound 17. 5-Propargylamino-3'-azidomethyl-dCTP can be used in DNA synthesis and DNA sequencing . 5-Propargylamino-3'-azidomethyl-dCTP is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
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Classification |
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- HY-132138
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Azide
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5-Propargylamino-3'-azidomethyl-dCTP is a nucleoside molecule extracted from patent WO2004018497A2, compound 17. 5-Propargylamino-3'-azidomethyl-dCTP can be used in DNA synthesis and DNA sequencing . 5-Propargylamino-3'-azidomethyl-dCTP is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-132138A
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Nucleotide Analogs
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5-Propargylamino-3'-azidomethyl-dCTP (TEA) is a nucleotide molecule that can be used in DNA synthesis and DNA sequencing. For detailed information, refer to compound 17 in patent document WO2004018497A2. 5-Propargylamino-3'-azidomethyl-dCTP (TEA) is a click chemistry reagent containing an azide group, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also react with molecules containing DBCO or BCN groups through strain-promoted alkyne-azide cycloaddition (SPAAC) .
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- HY-132138
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Nucleotide Analogs
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5-Propargylamino-3'-azidomethyl-dCTP is a nucleoside molecule extracted from patent WO2004018497A2, compound 17. 5-Propargylamino-3'-azidomethyl-dCTP can be used in DNA synthesis and DNA sequencing . 5-Propargylamino-3'-azidomethyl-dCTP is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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