Search Result
Results for "
5������ reductase Inhibitors
" in MCE Product Catalog:
3390
Inhibitors & Agonists
13
Biochemical Assay Reagents
329
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-152195
-
|
ChoKα inhibitor-5
|
Apoptosis
|
Cancer
|
|
ChoKα inhibitor-5 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-5 can inhibit HChoK α1 with an IC50 value of 0.64 μM. ChoKα inhibitor-5 also can induce apoptosis. ChoKα inhibitor-5 can be used for the research of cancer.
|
-
- HY-152214
-
|
SIRT5 inhibitor 5
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD + -binding pocket and acts as a substrate-competitive inhibitor.
|
-
- HY-146387
-
|
SIRT5 inhibitor 3
|
Sirtuin
|
Cancer
Neurological Disease
|
|
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-151962
-
|
JNK3 inhibitor-5
|
JNK
Apoptosis
GSK-3
p38 MAPK
|
Neurological Disease
|
|
JNK3 inhibitor-5 (Compound 22b) is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. JNK3 inhibitor-5 effectively protects the neuronal cells against amyloid beta-induced apoptosis. JNK3 inhibitor-5 has a high cell permeability and is predicted as BBB permeable.
|
-
- HY-123071
-
|
Box5
|
Wnt
|
Cancer
|
|
Box5 is a potent Wnt5a antagonist. Box5 inhibits Wnt5a signaling and inhibits Wnt5a-mediated Ca 2+ release. Box5 inhibits cell migration. Box5 has the potential for the research of melanoma.
|
-
- HY-149260
-
-
- HY-N2553
-
|
4-Deoxypyridoxine 5'-phosphate
|
LPL Receptor
|
Metabolic Disease
|
|
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase.
|
-
- HY-146386
-
|
SIRT5 inhibitor 2
|
Sirtuin
|
Cancer
Neurological Disease
|
|
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-114996
-
-
- HY-152034
-
|
STING-IN-5
|
STING
|
Inflammation/Immunology
|
|
STING-IN-5 is a potent STING inhibitor, inhibiting LPS-induced NO synthesis in macrophages with an IC50 value of 1.15 μM. STING-IN-5 inhibits the inflammatory response. STING-IN-5 can be used to research anti-inflammatory diseases and sepsis.
|
-
- HY-134883
-
-
- HY-150081
-
-
- HY-124546
-
-
- HY-N7162
-
-
- HY-U00260
-
-
- HY-147726
-
|
Microtubule inhibitor 5
|
Microtubule/Tubulin
|
Cancer
|
|
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.
|
-
- HY-113957
-
|
MPI_5a
|
HDAC
|
Cancer
|
|
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
|
-
- HY-16776A
-
|
(2S,5S)-Censavudine
(2S,5S)-OBP-601; (2S,5S)-BMS-986001
|
HIV
|
Infection
|
|
(2S,5S)-Censavudine ((2S,5S)-OBP-601) is the (2S,5S)-enantiomer of Censavudine. Censavudine, a nucleoside reverse transcriptase inhibitor, is a potent HIV inhibitor.
|
-
- HY-P0081
-
-
- HY-17511
-
|
Potassium oxonate
Potassium azaorotate; Potassium otastat; Oteracil potassium
|
Others
|
Metabolic Disease
|
|
Potassium oxonate is an inhibitor of uricase, inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.
|
-
- HY-143483
-
|
NBTIs-IN-5
|
Bacterial
|
Infection
|
|
NBTIs-IN-5 (Compound 5r) is a NBTI (Novel Bacterial Topoisomerase Inhibitor) DNA gyrase inhibitor with an IC50 of 1.5 μM against Mycobacterium abscessus (Mabs) DNA gyrase. NBTIs-IN-5 inhibits Mabs bamboo bacterial growth with an MIC90 of 0.4 μM.
|
-
- HY-112447
-
|
STAT3-IN-5
|
STAT
|
Cancer
|
|
STAT3-IN-5 is a potent STAT3 inhibitor. STAT3-IN-5 inhibits STAT3-Y705 phosphorylation with an EC50 value of 170 nM. STAT3-IN-5 inhibits cytokine induced JAK activation. STAT3-IN-5 induces apoptosis. STAT3-IN-5 can be used in research of cancer.
|
-
- HY-139022
-
-
- HY-151273
-
|
ALK5-IN-27
|
TGF-β Receptor
|
Cancer
|
|
ALK5-IN-27 (Compound EX-04) is a potent ALK-5 inhibitor with an IC50 ≤10 nM. ALK5-IN-27 also inhibits ALK-2 (selectivity ALK2/ALK5 ≤10).
|
-
- HY-131446
-
|
Chk1-IN-5
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
|
-
- HY-U00156
-
-
- HY-21586B
-
-
- HY-143437
-
|
TNIK-IN-5
|
Wnt
|
Cancer
|
|
TNIK-IN-5 is an efficient TNIK inhibitor with IC50 of 0.05 μM. TNIK-IN-5 efficiently inhibits Wnt signaling in intact cells. TNIK-IN-5 shows excellent in vitro anti-colorectal cancer activity.
|
-
- HY-N0172
-
-
- HY-141875
-
-
- HY-90006
-
-
- HY-151272
-
|
ALK5-IN-26
|
Others
|
Cancer
|
|
ALK5-IN-26 (EX-22) is an ALK (Activin receptor-like kinase) inhibitor. ALK5-IN-26 inhibits ALK5 with an IC50 value ≤10 nM. ALK5-IN-26 can be used for the research of cancer.
|
-
- HY-151281
-
|
ALK5-IN-31
|
TGF-β Receptor
|
Cancer
|
|
ALK5-IN-31 (compound Ex-08) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-31 has the potential to inhibit growth of tumour in vivo. ALK5-IN-31 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-151275
-
|
ALK5-IN-28
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
|
ALK5-IN-28 (compound Ex-05) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit growth of tumour in vivo. ALK5-IN-28 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-151282
-
|
ALK5-IN-32
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
|
ALK5-IN-32 (compound EX-09) is a selective ALK-5 inhibitor (10 nM<IC50<100 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-32 has the potential to inhibit growth of tumour in vivo. ALK5-IN-32 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-101579
-
|
LY 178002
|
COX
Lipoxygenase
Phospholipase
|
Inflammation/Immunology
|
|
LY 178002 is a potent inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2, with IC50 of 0.6 μM for 5-lipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
|
-
- HY-14403
-
|
ERK5-IN-1
|
ERK
|
Cancer
|
|
ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.
|
-
- HY-90006S
-
|
5-Fluorouracil-d1
5-FU-d1
|
Nucleoside Antimetabolite/Analog
HIV
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
5-Fluorouracil-d is the deuterium labeled 5-Fluorouracil. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[1][2]. 5-Fluorouracil also inhibits HIV[3].
|
-
- HY-12056
-
|
BIX02189
|
MEK
ERK
|
Cancer
|
|
BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
|
-
- HY-12886
-
-
- HY-148266
-
|
UBA5-IN-1
|
E1/E2/E3 Enzyme
|
Cancer
|
|
UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5.
|
-
- HY-150606
-
|
ERK5-IN-4
|
ERK
|
Cancer
|
|
ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC50 of 77 nM and 300 nM, respectively.
|
-
- HY-10533
-
|
Eniluracil
5-Ethynyluracil; GW776C85
|
Others
|
Cancer
|
|
Eniluracil (5-Ethynyluracil) is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor. Eniluracil irreversibly inhibits DPD, increases the oral bioavailability of 5-fluorouracil to 100%, and facilitates the uniform absorption and toxicity of 5-fluorouracil. Eniluracil can be used in cancer research of combination with fluoropyrimidines (including 5-fluorouracil).
|
-
- HY-90006S2
-
|
5-Fluorouracil-15N2
|
Nucleoside Antimetabolite/Analog
HIV
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
5-Fluorouracil- 15N2 is the 15N-labeled 5-Fluorouracil. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[1][2]. 5-Fluorouracil also inhibits HIV[3].
|
-
- HY-12055
-
|
BIX02188
|
MEK
ERK
|
Cancer
|
|
BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM.
|
-
- HY-U00217
-
-
- HY-18362
-
-
- HY-U00024
-
-
- HY-147990
-
-
- HY-145685
-
|
RECQL5-IN-1
|
Others
|
Cancer
|
|
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer.
|
-
- HY-101853
-
-
- HY-U00376
-
-
- HY-100148
-
-
- HY-112634
-
-
- HY-10162S
-
-
- HY-10997S
-
|
Ibrutinib-d5
PCI-32765-d5
|
Btk
|
Cancer
|
|
Ibrutinib-d5 is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor[1].
|
-
- HY-10450S
-
-
- HY-151270
-
|
ALK5-IN-25
|
TGF-β Receptor
|
Cancer
|
|
ALK5-IN-25 (compound EX-02) is a potent ALK-5 inhibitor with an IC50 ≤10 nM.ALK5-IN-25 also inhibits ALK-2 (selectivity ALK2/ALK5≤10). ALK5-IN-25 can be used for the research of cancer.
|
-
- HY-112134
-
|
CSN5i-3
|
Others
|
Cancer
|
|
CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.
|
-
- HY-142211
-
-
- HY-15025A
-
-
- HY-112551
-
-
- HY-15881
-
|
TCS JNK 5a
JNK Inhibitor IX
|
JNK
Apoptosis
|
Cancer
|
|
TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
|
-
- HY-152077
-
|
Telomerase-IN-5
|
Apoptosis
|
Cancer
|
|
Telomerase-IN-5 is a potent telomerase inhibitor. Telomerase-IN-5 has antiproliferative activity and induces apoptosis.
|
-
- HY-90006S1
-
|
5-Fluorouracil-13C,15N2
5-FU-13C,15N2
|
Apoptosis
Nucleoside Antimetabolite/Analog
HIV
Endogenous Metabolite
|
Cancer
|
|
5-Fluorouracil- 13C, 15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
|
-
- HY-116217
-
|
5-Fluoro-2'-deoxycytidine
|
DNA Methyltransferase
|
Cancer
|
|
5-Fluoro-2'-deoxycytidine, a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of the potent thymidylate synthase inhibitor 5-fluoro-2′-dUMP.
|
-
- HY-151277
-
|
ALK5-IN-29
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK5-IN-29 is an selective activin receptor-like kinase (ALK) inhibitor. ALK5-IN-29 can inhibit the activity of ALK5 with an IC50 value of ≤10 nM. ALK5-IN-29 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.
|
-
- HY-144774
-
|
Topoisomerase I inhibitor 5
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin.
|
-
- HY-112587
-
-
- HY-150585
-
|
BuChE-IN-5
|
Amyloid-β
Cholinesterase (ChE)
Tau Protein
|
Neurological Disease
|
|
BuChE-IN-5 (compound 25b) is a potent BuChE inhibitor with an IC50 value of 1.94 μM. BuChE-IN-5 efficiently inhibits aggregation Aβ and tau protein in Escherichia coli. BuChE-IN-5 also has free radical scavenging capacity and antioxidant activity. BuChE-IN-5 can be used for researching Alzheimer’s disease.
|
-
- HY-147733
-
-
- HY-135386
-
-
- HY-147520
-
-
- HY-U00438
-
-
- HY-146596
-
-
- HY-139979
-
|
USP5-IN-1
|
Deubiquitinase
|
Cancer
|
|
USP5-IN-1 (compound 64), a potent deubiquitinase USP5 inhibitor, binds to the USP5 ZnF-UBD with a KD of 2.8 μM. USP5-IN-1 is selective over nine proteins containing structurally similar ZnF-UBD domains. USP5-IN-1 inhibits the USP5 catalytic cleavage of a di-ubiquitin substrate.
|
-
- HY-U00347
-
-
- HY-118091B
-
|
LY300503
|
Others
|
Others
|
|
LY300503 is an enantiomer of LY191704. LY191704 is a human type I 5α-reductase inhibitor.
|
-
- HY-101474S
-
|
Zanubrutinib D5
BGB-3111 d5
|
Btk
|
Cancer
|
|
Zanubrutinib-d5 is deuterium labeled Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (Btk) inhibitor[1].
|
-
- HY-A0116S
-
-
- HY-12442
-
|
LY5
|
STAT
Apoptosis
|
Cancer
|
|
LY5 is a STAT3 inhibitor with an IC50 value of 0.5 μM. LY5 induces apoptosis and inhibits STAT3 phosphorylation. LY5 shows antitumor activity in vivo, it can be used for the research of cancer.
|
-
- HY-147904
-
|
HIV-IN-5
|
HIV
|
Infection
|
|
HIV-IN-5 (compound 5r) is a potent HIV-1 inhibitor, with an IC50 of 0.16 μM. HIV-IN-5 shows inhibition of HIV DNA-dependent DNA polymerization activity, with an IC50 of 2.18 μM. HIV-IN-5 can bind to NNIBP (NNRTIs (non-nucleoside reverse transcriptase inhibitors) binding pocket) .
|
-
- HY-147980
-
|
Aβ-IN-5
|
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
Aβ-IN-5 (Compound e12) is an orally active Aβ aggregation inhibitor. Aβ-IN-5 also inhibits AChE and BuChE with IC50 values of 21.29 μM and 1.32 μM, respectively. Aβ-IN-5 shows excellent neuroprotective effects and low neurotoxicity.
|
-
- HY-W009757
-
-
- HY-90006S3
-
|
5-Fluorouracil-13C4,15N2
5-FU-13C4,15N2
|
Apoptosis
Nucleoside Antimetabolite/Analog
HIV
Endogenous Metabolite
|
Cancer
|
|
5-Fluorouracil- 13C4, 15N2 is the 13C and 15N labeled 5-Fluorouracil[1]. 5-Fluorouracil (5-FU) is an analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer[2][3]. 5-Fluorouracil also inhibits HIV[4].
|
-
- HY-151289
-
|
ALK5-IN-34
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
|
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.
|
-
- HY-19969
-
|
YM-90709
|
Interleukin Related
|
Inflammation/Immunology
|
|
YM-90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).YM-90709 potently inhibits the binding of [ 125I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells with IC50 values of 1.0 and 0.57 μM.
|
-
- HY-148151
-
|
(-)-5′-Noraristeromycin
|
HBV
|
Cancer
|
|
(-)-5′-Noraristeromycin is an antiviral agent. (-)-5′-Noraristeromycin also is an enantiomer of 5'-noraristeromycin and can inhibit intracellular HBV replication and virion production. (-)-5′-Noraristeromycin can be used for the research of cancer.
|
-
- HY-N0198
-
-
- HY-15025
-
-
- HY-14164
-
-
- HY-B1664
-
-
- HY-144659
-
|
Metallo-β-lactamase-IN-5
|
Apoptosis
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-5 (compound 5c) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-5 shows inhibitory activity against MBLs NDM-1 and VIM-1. Metallo-β-lactamase-IN-5 inhibits HUVECs with an IC50 of 45 μg/mL. Metallo-β-lactamase-IN-5 plus Imipenem exhibits synergistic antimicrobial activity.
|
-
- HY-111213
-
-
- HY-150727
-
|
SIRT5 inhibitor 4
|
Sirtuin
|
Cancer
|
|
SIRT5 inhibitor 4 (compound 11) is a potent, selective SIRT5 inhibitor with IC50 values of 26.4 and >400μM for SIRT5 and other SIRT subtype, respectively.
|
-
- HY-138684
-
-
- HY-138684A
-
-
- HY-135383A
-
-
- HY-123772
-
|
CDK5 inhibitor 20-223
|
CDK
|
Cancer
|
|
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
|
-
- HY-147054
-
|
WEE1-IN-5
|
Wee1
CDK
|
Cancer
|
|
WEE1-IN-5 is a potent WEE1 inhibitor with an IC50 value of 0.8 nM. WEE1-IN-5 inhibits phospho-CDC2. WEE1-IN-5 abrogates the G2 check point, increasing sensitivity to DNA damaging agents in cancer cells. WEE1-IN-5 can be used for researching anticancer.
|
-
- HY-147691
-
|
MPO-IN-5
|
Glutathione Peroxidase
Potassium Channel
|
Inflammation/Immunology
|
|
MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and hERG binding, with IC50 values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (kinact/Ki) of 23000 M −1s −1.
|
-
- HY-W011336
-
-
- HY-122258
-
|
NSC-370284
|
STAT
TET Protein
|
Cancer
|
|
NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5.
|
-
- HY-145835A
-
|
(S)-PERK-IN-5
|
PERK
|
Cancer
Infection
|
|
(S)-PERK-IN-5 is the S-enantiomer of PERK-IN-5. (S)-PERK-IN-5 (example 39) is a PERK inhibitor, with an IC50 of 0.101-0.250 μM.
|
-
- HY-Y0051
-
|
5-Hydroxymethylfurfural
2-Hydroxymethyl-5-furfural; 2-Formyl-5-hydroxymethylfuran
|
Fungal
|
Others
|
|
5-Hydroxymethylfurfural (2-Hydroxymethyl-5-furfural), derived from Cornus officinalis, inhibits yeast growth and fermentation as stressors.
|
-
- HY-13041
-
-
- HY-13219
-
-
- HY-132937
-
-
- HY-100422
-
-
- HY-145375
-
-
- HY-124663
-
-
- HY-16592
-
|
Brefeldin A
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
Bacterial
|
Cancer
Infection
|
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-111644
-
-
- HY-148767
-
-
- HY-N7757
-
|
Pedunculagin
|
5 alpha Reductase
|
Inflammation/Immunology
|
|
Pedunculagin is a potent 5α-reductase type 1 inhibitor. Pedunculagin inhibits nitric oxide (NO), IL-6, IL-8 production. Pedunculagin decreases the protein expression of 5α-reductase. Pedunculagin shows anti-inflammatory activity.
|
-
- HY-101456
-
-
- HY-B1287
-
|
Citalopram hydrobromide
(±)-Citalopram hydrobromide; Lu 10-171
|
Serotonin Transporter
Autophagy
|
Neurological Disease
Cancer
|
|
Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect.
|
-
- HY-W488004
-
-
- HY-117605
-
-
- HY-13026S
-
|
Idelalisib-d5
CAL-101 d5; GS-1101 d5
|
PI3K
Autophagy
|
Cancer
|
|
Idelalisib-d5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor[1].
|
-
- HY-146218
-
|
MMP-9-IN-5
|
MMP
Akt
Apoptosis
|
Cancer
|
|
MMP-9-IN-5 is a MMP-9 inhibitor (IC50: 4.49 nM) that forms hydrogen bond with MMP-9. MMP-9-IN-5 also inhibits AKT activity (IC50: 1.34 nM). MMP-9-IN-5 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-5 can be used in the research of cancers.
|
-
- HY-148598
-
-
- HY-119671
-
|
BW 755C
|
COX
Lipoxygenase
|
Endocrinology
|
|
BW 755C is a 5-lipoxygenase (5-LO) inhibitor with an IC50 of 5 μM. BW 755C also inhibits cyclooxygenase (COX) with IC50s of 0.65 and 1.2 μg/mL against COX-1 and COX-2, respectively.
|
-
- HY-133669
-
|
DDR1-IN-5
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR1-IN-5 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 7.36 nM. DDR1-IN-5 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 4.1 nM. DDR1-IN-5 has anti-cancer activity.
|
-
- HY-B0346S
-
-
- HY-13419
-
-
- HY-P0222
-
|
PKI(5-24)
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-144437
-
|
ALK5-IN-9
|
TGF-β Receptor
|
Cancer
|
|
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease.
|
-
- HY-133121
-
|
WDR5-IN-1
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
|
-
- HY-101297
-
|
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-144205
-
-
- HY-111482
-
-
- HY-148573
-
-
- HY-139725
-
|
CDK5-IN-1
|
CDK
|
Metabolic Disease
|
|
CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research.
|
-
- HY-148134
-
-
- HY-19527
-
|
IST5-002
N6-Benzyladenosine-5'-phosphate
|
STAT
Apoptosis
|
Cancer
|
|
IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML).
|
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-151980
-
|
Mps1-IN-5
|
Mps1
Apoptosis
|
Cancer
|
|
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage.
|
-
- HY-151409
-
|
CDK1-IN-5
|
CDK
|
Cancer
|
|
CDK1-IN-5 (10h) is a selective CDK1 inhibitor with IC50s of 42.19, 188.71 and 354.15 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN-5 inhibits growth of cancer cells by affecting cell cycle. CDK1-IN-5 can be used for the research of cancer.
|
-
- HY-149922
-
-
- HY-131100S
-
-
- HY-123967
-
|
RNF5 inhibitor inh-02
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research.
|
-
- HY-131710
-
|
PDE5-IN-3
|
Phosphodiesterase (PDE)
EGFR
Wnt
Apoptosis
|
Cancer
|
|
PDE5-IN-3 (compound 11j) is a potent PDE5 inhibitor with an IC50 of 1.57 nM. PDE5-IN-3 shows moderate EGFR inhibition with IC50 of 5.827 µM. PDE5-IN-3 significantly inhibits the Wnt/β-catenin pathway (IC50=1286.96 ng/mL). PDE5-IN-3 induces the intrinsic apoptotic mitochondrial pathway in HepG2 cells. PDE5-IN-3 has strong antitumor activity.
|
-
- HY-115875
-
-
- HY-14164A
-
-
- HY-145374
-
-
- HY-101826
-
-
- HY-15000
-
|
EMD534085
|
Kinesin
|
Cancer
|
|
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
|
-
- HY-144189
-
-
- HY-112165
-
-
- HY-151283
-
-
- 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-151514
-
|
Antituberculosis agent-5
|
Bacterial
|
Infection
|
|
Antituberculosis agent-5 (compound 52) is a nitrofuranylamide derivative, inhibits M. tuberculosis UDP-Gal mutase. Antituberculosis agent-5 inhibits Glf activity with an IC50 value of 99 μM/mL and resists tuberculosis (TB) with a MIC value of 1.6 μg/mL.
|
-
- HY-15198
-
|
KG5
|
Raf
PDGFR
FLT3
c-Kit
|
Cancer
|
|
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
|
-
- HY-151279
-
-
- HY-109963
-
-
- HY-151466
-
|
HIF-1α-IN-5
|
HIF/HIF Prolyl-Hydroxylase
Monoamine Oxidase
|
Cancer
|
|
HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer.
|
-
- HY-P0222A
-
|
PKI(5-24) TFA
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-144043
-
|
ALK5-IN-8
|
TGF-β Receptor
|
Cancer
|
|
ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1).
|
-
- HY-146221
-
|
Dyrk1A-IN-5
|
DYRK
|
Neurological Disease
|
|
Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research.
|
-
- HY-130606
-
|
Nampt-IN-5
|
NAMPT
Cytochrome P450
|
Cancer
|
|
Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.
|
-
- HY-135383
-
-
- HY-146671
-
|
ITK inhibitor 5
|
Itk
|
Cancer
|
|
ITK inhibitor 5 (compound 27) is a potent and selective ITK inhibitor with IC50s of 5.6, 25 nM for ITK, BTK, respectively.
|
-
- HY-151410
-
|
Chitin synthase inhibitor 5
|
Fungal
|
Infection
|
|
Chitin synthase inhibitor 5 (compound 9a) is an inhibitor of chitin synthase with an IC50 value of 0.14 mM. Chitin synthase inhibitor 5 shows broad-spectrum antifungal activity in vitro and shows good inhibition to C. albicans, A. flavus, A. fumigatus and C. neoformans. Chitin synthase inhibitor 5 can be used for the research of fungal.
|
-
- 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 agent resistance.
|
-
- HY-U00308
-
-
- HY-112134A
-
|
(R)-CSN5i-3
|
Others
|
Cancer
|
|
(R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5.
|
-
- HY-146584
-
|
Cathepsin C-IN-5
|
Cathepsin
|
Inflammation/Immunology
|
|
Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity.
|
-
- HY-150566
-
|
BCR-ABL-IN-5
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl WT and Bcr-Abl T3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells.
|
-
- HY-102048
-
|
STAT5-IN-2
|
STAT
Apoptosis
|
Cancer
|
|
STAT5-IN-2 is a STAT5 inhibitor, extracted from reference 1, example 17f. STAT5-IN-2 has potent antileukemic effect.
|
-
- HY-N0551
-
|
Wedelolactone
|
Caspase
Lipoxygenase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC50 of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer.
|
-
- HY-W011235
-
|
Norfluoxetine hydrochloride
|
5-HT Receptor
Calcium Channel
Drug Metabolite
|
Neurological Disease
|
|
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity.
|
-
- HY-107856
-
-
- HY-15665
-
|
XMD17-109
|
ERK
|
Cancer
|
|
XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.
|
-
- HY-100025A
-
-
- HY-101496
-
|
MT-DADMe-ImmA
MTDIA; Methylthio-DADMe-Immucillin A
|
Others
|
Cancer
|
|
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
|
-
- HY-139821
-
-
- HY-100240
-
-
- HY-111926
-
-
- HY-101172
-
|
RS 23597-190
EP-A-501322
|
5-HT Receptor
|
Cardiovascular Disease
|
|
RS 23597-190 (EP-A-501322) is a high affinity and selective 5-HT4 receptor antagonist. RS 23597-190 inhibits 5-HT-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose.
|
-
- HY-B0279S
-
-
- HY-141876
-
-
- HY-147647
-
-
- HY-P1111A
-
|
Lyn peptide inhibitor TFA
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-135710
-
|
ADAMTS-5-IN-2
|
Others
|
Inflammation/Immunology
|
|
ADAMTS-5-IN-2 (compound 25) is a potent ADAMTS-5 inhibitor with an IC50 value of 0.71 µM. ADAMTS-5-IN-2 has the potential for the research of modifying osteoarthritis.
|
-
- HY-145150
-
|
TRPC5-IN-1
|
TRP Channel
|
Metabolic Disease
|
|
TRPC5-IN-1 (Compound 6j) is a selective TRPC5 inhibitor with 50.5 % Inhibition for TRPC5 at 3 μM. TRPC5-IN-1 can be used for the research of chronic kidney disease (CKD).
|
-
- HY-100846
-
|
JQEZ5
|
Histone Methyltransferase
|
Cancer
|
|
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
|
-
- 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-151975
-
-
- HY-103464
-
|
5'-Fluoroindirubinoxime
5'-FIO
|
FLT3
|
Cancer
|
|
5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
|
-
- HY-143423
-
|
MALT1-IN-5
|
MALT1
|
Cancer
|
|
MALT1-IN-5 (compound 1) is a potent MALT1 protease inhibitor. MALT1-IN-5 can be used for cancer research.
|
-
- HY-146348
-
|
Tuberculosis inhibitor 5
|
Bacterial
|
Infection
|
|
Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue without noticeable cytotoxicity. Tuberculosis inhibitor 5 is an anti-tuberculosis agent.
|
-
- HY-50714
-
|
Quiflapon sodium
MK-591 sodium
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
|
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
|
-
- HY-13327
-
|
Evacetrapib
LY2484595
|
CETP
|
Cardiovascular Disease
|
|
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
|
-
- HY-100562
-
-
- HY-112915
-
-
- HY-101587
-
-
- HY-N2513
-
|
β-Boswellic acid
|
Lipoxygenase
DNA/RNA Synthesis
|
Cancer
|
|
β-Boswellic acid is isolated from the gum resin of Boswellia serrata.
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-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. ddGTP acts as an inhibitor or a substrate for DNA polymerase α.
|
-
- HY-135780
-
-
- HY-147621
-
-
- HY-B0307A
-
|
Idoxuridine hydrate
5-Iodo-2′-deoxyuridine hydrate; 5-IUdR hydrate; IdUrd hydrate
|
Phosphatase
|
Infection
|
|
Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) hydrate is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM.
|
-
- HY-150654
-
|
WDR5-IN-5
|
Histone Methyltransferase
|
Cancer
|
|
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM.
|
-
- HY-151448
-
|
ZIKV-IN-5
|
Virus Protease
|
Infection
|
|
ZIKV-IN-5 (compound 5c) is a low-cytotoxicity and acid-stable anti-ZIKV agent (EC50=0.71 μM). ZIKV-IN-5 effectively inhibits the activity of ZIKV NS5 MTase.
|
-
- 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-113846
-
|
CMP-5 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|
-
- HY-148037
-
-
- HY-15414
-
-
- HY-W004924S
-
|
5-Hydroxymethyluracil-d3
|
Endogenous Metabolite
|
Others
|
|
5-Hydroxymethyluracil-d3 is the deuterium labeled 5-Hydroxymethyluracil[1]. 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[2][3].
|
-
- HY-144208
-
-
- HY-100231
-
|
Cathepsin inhibitor 1
|
Cathepsin
|
Cancer
|
|
Cathepsin inhibitor 1 (compound 25) is a potent and selective inhibitor of Cathepsin, with pIC50s of 7.9, 6.7, 6.0, 5.5 and 5.2 for CatL, CatL2, CatS, CatK, and CatB, respectively.
|
-
- HY-19417A
-
-
- HY-100693
-
-
- HY-110399
-
-
- HY-B0331AS
-
-
- HY-17357S
-
|
Nepafenac-d5
AHR-9434-d5; AL-6515-d5
|
COX
|
Others
|
|
Nepafenac-d5 is the deuterium labeled Nepafenac, which is a selective COX-2 inhibitor.
|
-
- HY-153160
-
-
- HY-12392
-
-
- HY-100996
-
-
- HY-150095
-
|
YE6144
|
Others
|
Inflammation/Immunology
|
|
YE6144 is a prototypical interferon regulatory factor 5 (IRF5) inhibitor. YE6144 selectively suppresses IRF5 activity through inhibition of IRF5 phosphorylation.
|
-
- HY-152239
-
|
RdRP-IN-5
|
Influenza Virus
|
Infection
|
|
RdRP-IN-5 (compound 20) is a potent influenza virus RNA-dependent RNA polymerase (RdRP) inhibitor. RdRP-IN-5 can be used in research of influenza virus.
|
-
- HY-119611A
-
-
- HY-135089
-
-
- HY-106689
-
-
- HY-W011044
-
|
CID 5951923
|
KLF
|
Cancer
|
|
CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro.
|
-
- HY-13227
-
|
SD-208
|
TGF-β Receptor
|
Cancer
|
|
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
|
-
- HY-143468
-
|
MEK-IN-5
|
Apoptosis
MEK
|
Cancer
|
|
MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells.
|
-
- HY-147080
-
|
Avacincaptad pegol sodium
ARC1905
|
Complement System
|
Others
|
|
Avacincaptad pegol (ARC1905) is is an anti-C5 RNA aptamer that inhibits the cleavage of complement factor 5 (C5) into C5a and C5b. Avacincaptad pegol is being used for the study of age-related macular degeneration (AMD).
|
-
- HY-P9914
-
|
Eculizumab
Anti-Human C5, Humanized Antibody
|
Complement System
|
Cardiovascular Disease
|
|
Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5. Eculizumab inhibits the cleavage of C5 into C5a and C5b and hence inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab has the potential for haemolysis research.
|
-
- HY-131140
-
|
BD750
|
JAK
STAT
|
Cancer
Inflammation/Immunology
|
|
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
|
-
- HY-151552
-
|
Mtb-cyt-bd oxidase-IN-5
|
Bacterial
|
Infection
|
|
Mtb-cyt-bd oxidase-IN-5 (compound 1k) is a Mycobacterium tuberculosis (Mtb) cytochrome bd (cyt-bd) oxidase (MtbCyt-bd Oxidase) inhibitor with an IC50 value of 0.37 μM. Mtb-cyt-bd oxidase-IN-5 can effectively inhibit the growth of Mtb (MIC= 256 μM). Mtb-cyt-bd oxidase-IN-5 can be used in the study of tuberculosis.
|
-
- HY-15424
-
|
5-Iodotubercidin
NSC 113939; 5-ITu
|
Adenosine Kinase
|
Cancer
|
|
5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin.
|
-
- HY-146540
-
|
GEM-5
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
MDM-2/p53
|
Cancer
|
|
GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.
|
-
- HY-15339
-
|
CVT-313
Cdk2 Inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
|
-
- HY-N5011
-
|
5,7-Dimethoxyflavone
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
|
-
- HY-12220
-
|
MM-102
HMTase Inhibitor IX
|
Histone Methyltransferase
|
Cancer
|
|
MM-102 (HMTase Inhibitor IX) is a potent WDR5/MLL interaction inhibitor, achieves IC50= 2.4 nM with an estimated Ki< 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
|
-
- HY-144420
-
|
Neuraminidase-IN-5
|
Influenza Virus
|
Infection
|
|
Neuraminidase-IN-5 (Compound 5b) is a potent inhibitor of neuraminidase with an IC50 of 0.02 μM. Neuraminidase (NA) is a promising target for development of anti-influenza agents. Neuraminidase-IN-5 is a dihydrofurocoumarin derivative compound.
|
-
- HY-147750
-
-
- HY-151619
-
|
sEH inhibitor-12
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-12 (compound 34) is a sEH inhibitor with an IC50 value of 0.7 μM. sEH inhibitor-12 inhibits the 5-lipoxygenase-activating protein (FLAP)-mediated leukotriene (LT) biosynthesis with an IC50 value of 2.9 μM. sEH inhibitor-12 can be used for the research of inflammation.
|
-
- HY-143747
-
|
Cap-dependent endonuclease-IN-5
|
Influenza Virus
|
Infection
|
|
Cap-dependent endonuclease-IN-5 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-5 inhibits influenza virus well, and/or has lower cytotoxicity, better in vivo pharmacokinetic properties and in vivo pharmacodynamic properties (extracted from patent WO2020078401A1, compound 13-1).
|
-
- HY-119098
-
|
GSK983
|
EBV
HPV
|
Infection
|
|
GSK983 is a broad-spectrum antiviral agent. GSK983 inhibits the replication of adenovirus-5 (Ad-5) and polyoma virus SV40. GSK983 inhibits the growth of cell lines immortalized by
EBV, HTLV1, HPV. GSK983 induces the expression of interferon-stimulated genes.
|
-
- HY-134103A
-
|
ddGTP trisodium
2′,3′-Dideoxyguanosine 5′-triphosphate trisodium
|
DNA/RNA Synthesis
|
Others
|
|
ddGTP (2′,3′-Dideoxyguanosine 5′-triphosphate) trisodium is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing. ddGTP trisodium acts as an inhibitor or a substrate for DNA polymerase α.
|
-
- HY-135780A
-
-
- HY-143459
-
|
Tyrosinase-IN-5
|
Tyrosinase
|
Cancer
|
|
Tyrosinase-IN-5 (compound 16c) is a potent inhibitor of tyrosinase with an IC50 of 0.02 μM. Tyrosinase-IN-5 efficiently suppresses the melanogenesis without significant toxicity on cells.
|
-
- HY-143465
-
-
- HY-139986
-
|
CDK7-IN-5
|
CDK
|
Cancer
|
|
CDK7-IN-5 is a CDK7 inhibitor with an IC50 value <100 nM. CDK7-IN-5 has anticancer effects. (WO2015154022A1 (Compound 104)).
|
-
- HY-10586
-
-
- 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-111643
-
-
- HY-123210
-
-
- HY-B0346
-
|
Propylthiouracil
6-n-Propylthiouracil; 6-Propyl-2-thiouracil; PTU
|
Others
|
Endocrinology
|
|
Propylthiouracil(6-Propyl-2-thiouracil) is a thyroperoxidase and 5'-deiodinase inhibitor.
|
-
- HY-W039722
-
-
- HY-111471
-
-
- HY-107615
-
|
TC LPA5 4
|
LPL Receptor
|
Cancer
|
|
TC LPA5 4 is a LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 displays selectivity for LPA5 over 80 other screened agent targets. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells.
|
-
- HY-120137
-
|
CMP-5
|
Histone Methyltransferase
|
Cancer
|
|
CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|
-
- HY-149005
-
|
PRMT5-IN-19
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research.
|
-
- HY-147607
-
-
- HY-146341
-
|
FAAH-IN-5
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH-IN-5 (Compound 7) is a relative selective, irreversible fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 10.5 nM. FAAH-IN-5 shows low PAMPA (Parallel Artificial Membrane Permeability Assay) permeability.
|
-
- HY-15414A
-
-
- HY-123538
-
-
- HY-14165
-
-
- HY-12429
-
|
Beclabuvir
BMS-791325
|
HCV
|
Infection
|
|
Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.
|
-
- HY-B0032S
-
-
- HY-15027S
-
-
- HY-152239B
-
|
trans-RdRP-IN-5
|
Influenza Virus
|
Infection
|
|
trans-RdRP-IN-5 (compound 18) is a potent influenza virus RNA-dependent RNA polymerase (RdRP) inhibitor. trans-RdRP-IN-5 can be used in research of influenza virus.
|
-
- HY-119611
-
-
- HY-152239A
-
|
cis-RdRP-IN-5
|
Influenza Virus
|
Infection
|
|
cis-RdRP-IN-5 (compound 19) is a potent influenza virus RNA-dependent RNA polymerase (RdRP) inhibitor. cis-RdRP-IN-5 can be used in research of influenza virus.
|
-
- HY-153007
-
|
DHFR-IN-5
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity.
|
-
- HY-101945
-
|
A-69412
|
Lipoxygenase
|
Inflammation/Immunology
|
|
A-69412 is a reversible, specific inhibitor of the 5-lipoxygenase (5-LO). A-69412 has the potential to treat asthma and ulcerative colitis, and possibly other inflammatory and allergic conditions.
|
-
- HY-111852
-
-
- HY-147991
-
-
- HY-112698
-
|
CA-5f
|
Autophagy
Apoptosis
|
Cancer
|
|
CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
|
-
- HY-145835
-
|
PERK-IN-5
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.
|
-
- HY-142059
-
-
- HY-100437
-
|
HA15
|
HSP
Autophagy
Apoptosis
|
Cancer
|
|
HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
|
-
- HY-B0882S
-
|
Edrophonium-d5 chloride
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-12220A
-
|
MM-102 TFA
HMTase Inhibitor IX TFA
|
Histone Methyltransferase
|
Cancer
|
|
MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
|
-
- HY-W010918
-
|
Adenosine 5'-diphosphate
Adenosine diphosphate; ADP
|
Endogenous Metabolite
|
Others
|
|
Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
|
-
- HY-146016
-
|
PI3K/mTOR Inhibitor-5
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-5 (compound 19a) is a potent and dual PI3K and mTOR inhibitor, with IC50 values of 86.9 nM and 14.6 nM, respectively.
|
-
- HY-147994
-
|
EGFR/HER2-IN-5
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research.
|
-
- HY-144038
-
|
DNA-PK-IN-5
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021204111A1, compound 2).
|
-
- HY-151441
-
|
LRRK2-IN-5
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-5 (compound 25) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 1.2 and 16 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-5 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-5 can cross the blood-brain barrier.
|
-
- HY-D0843S
-
|
N-Ethylmaleimide-d5
NEM-d5
|
Cathepsin
Deubiquitinase
|
Others
|
|
N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
|
-
- 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-115986
-
-
- HY-107777
-
|
LLY-283
|
Histone Methyltransferase
|
Cancer
|
|
LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
|
-
- HY-135358
-
-
- HY-152669
-
|
Urease-IN-5
|
Bacterial
|
Infection
|
|
Urease-IN-5 is an inhibitor of urease with an IC50 value of 1.473 µM. Urease-IN-5 has low cytotoxicity and inhibitory activity on P. vulgaris with an IC50 value of 17.78 µg/mL.
|
-
- HY-145415
-
|
W13
|
Bacterial
|
Infection
|
|
W13 is a potent MsbA inhibitor. W13 is an ATPase stimulator with an EC50 of 5.5 µM.
|
-
- HY-139657
-
-
- HY-13032
-
-
- HY-111471A
-
-
- HY-115876
-
-
- HY-14775
-
|
Nesbuvir
HCV-796
|
HCV
|
Infection
|
|
Nesbuvir is a nonnucleoside inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B) polymerase.
|
-
- HY-139684
-
-
- HY-137243
-
-
- HY-15825
-
|
IWP L6
Porcn Inhibitor III
|
Porcupine
|
Cancer
|
|
IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
|
-
- HY-112269
-
-
- HY-N9194
-
|
5-Methoxycanthin-6-one
|
Parasite
|
Infection
|
|
5-Methoxycanthin-6-one is an orally active inhibitor of Leishmania strains. 5-Methoxycanthin-6-one shows cytotoxicity with an IC50 of 5.44 μg/mL against Ailanthus altissima cells.
|
-
- HY-131704
-
|
FGFR4-IN-5
|
FGFR
|
Cancer
|
|
FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC50 of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research.
|
-
- HY-P3821
-
|
PRMT5-IN-22
|
Histone Methyltransferase
|
Cancer
|
PRMT5-IN-22 (compound 53) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
|
-
- HY-P3822
-
|
PRMT5-IN-23
|
Histone Methyltransferase
|
Cancer
|
PRMT5-IN-23 (compound 50) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
|
-
- HY-150605
-
|
ERK5-IN-3
|
ERK
|
Cancer
|
|
ERK5-IN-3 (compound 33j) is a potent and selective ERK5 (extracellular signal-related kinase 5) inhibitor, with an IC50 of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC50 of 31 nM.
|
-
- HY-13406
-
|
TAK-779
Takeda 779
|
CCR
HIV
CXCR
|
Infection
Inflammation/Immunology
Endocrinology
|
|
TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
|
-
- HY-147803
-
|
TrxR-IN-5
|
Reactive Oxygen Species
|
Cancer
|
|
TrxR-IN-5 (compound 4f) is a potent TrxR (thioredoxin reductase) inhibitor, with an IC50 of 0.16 μM. TrxR-IN-5 increases the levels of ROS, thus leading to potent antiproliferative effects. TrxR-IN-5 exhibits prominent anticacer and anti-metastasis effects.
|
-
- HY-101423
-
-
- HY-19776
-
-
- HY-B0307
-
|
Idoxuridine
5-Iodo-2′-deoxyuridine; 5-IUdR; IdUrd
|
Phosphatase
Orthopoxvirus
|
Infection
Cancer
|
|
Idoxuridine (5-Iodo-2′-deoxyuridine, 5-IUdR, IdUrd) is an iodinated thymidine analogue that competitively inhibits phosphorylases. Idoxuridine can inhibit viral activity, particularly viral eye infections, including herpes simplex keratitis, by inhibiting DNA polymerase and affecting viral replication. Idoxuridine against feline herpesvirus has the IC50 value of 4.3 μM. Idoxuridine shows anti-orthopoxvirus activity.
|
-
- HY-141882
-
|
DC-LC3in-D5
|
Autophagy
|
Cancer
Infection
Inflammation/Immunology
|
|
DC-LC3in-D5 acts as an autophagy inhibitor by attenuating LC3B lipidation. DC-LC3in-D5 binds with LC3B. DC-LC3in-D5 disrupts the LC3B-LBP2 interaction with an IC50 of 200 nM. DC-LC3in-D5 may contribute to anti-HCV or combination researchs in cancer through inhibiting autophagy.
|
-
- HY-133019
-
-
- HY-105024
-
|
FPL 62064
|
Lipoxygenase
COX
|
Inflammation/Immunology
|
|
FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC50 values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity.
|
-
- HY-150021
-
-
- HY-12983
-
|
ALS-8112
|
RSV
|
Infection
|
|
ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.
|
-
- HY-12632
-
|
GNE 2861
|
PAK
|
Cancer
|
|
GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.
|
-
- HY-N8188
-
|
Dehydrojuncusol
|
HCV
HCV Protease
|
Infection
|
|
Dehydrojuncusol, a potent HCV inhibitor, targets HCV NS5A and is able to inhibit RNA replication of replicons harboring resistance mutations to anti-NS5A direct-acting antivirals. Dehydrojuncusol significantly inhibits HCV infection when added after virus inoculation of HCV genotype 2a (EC50=1.35 µM).
|
-
- HY-147718
-
-
- HY-153011
-
-
- HY-116947
-
|
COX-2-IN-5
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-5 (compound 11a) is a potent COX-2 inhibitor with an IC50 value of 0.65 µM. COX-2-IN-5 has the potential for the research of inflammation.
|
-
- HY-144188
-
|
PRMT5-IN-17
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
|
-
- HY-144187
-
|
PRMT5-IN-16
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification.
|
-
- HY-145950
-
-
- HY-15315S
-
|
Baricitinib-d5
LY3009104-d5; INCB028050-d5
|
JAK
|
Inflammation/Immunology
|
|
Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-145613
-
-
- HY-108630
-
|
U-73343
|
Phospholipase
|
Others
|
|
U-73343, works as a protonophore, is an inactive analog of U-73122 and can be used as a negative control. U-73343 dose-dependently inhibits acid secretion irrespective of the stimulant. U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 µM for PLC.
|
-
- HY-137042
-
|
Cyanine5 alkyne
Alkyne-Cy5
|
Mitochondrial Metabolism
|
Cancer
|
|
Cyanine5 alkyne (Alkyne-Cy5) is a fluorescent dye used to label azide proteins and can be used to analyse post-translational modifications of proteins, glycosylation etc. Cyanine5 alkyne can also be used as a mitochondrial OXPHOS inhibitor to inhibit the growth of cancer stem cells (CSC). Storage: protect from light.
|
-
- HY-13012
-
|
RepSox
E-616452; SJN 2511
|
TGF-β Receptor
|
Metabolic Disease
|
|
RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.
|
-
- HY-143274
-
|
DENV-IN-5
|
HIV
DNA/RNA Synthesis
|
Infection
|
|
DENV-IN-5 (Compound 4b) is a dengue virus (DENV) inhibitor with EC50s of 1.47, 9.23, 7.08 and 8.91 μM against DENV-I ∼ IV replication, respectively. DENV-IN-5 also inhibits HIV-1IIIB strain with an EC50 of 0.1512 μM.
|
-
- HY-B0352S
-
|
Mirtazapine D3
Org3770 d3; 6-Azamianserin d3
|
5-HT Receptor
|
Neurological Disease
|
|
Mirtazapine-d3 is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors[1].
|
-
- HY-136144
-
|
FIDAS-5
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities.
|
-
- HY-129910
-
|
FABP5-IN-1
|
FABP
|
Inflammation/Immunology
|
|
FABP5-IN-1 is a selective and high affinity fatty acid binding protein 5 (FABP5) inhibitor with a Ki value of 1.7 μM, and does not bind to both FABP3 and FABP7. FABP5-IN-1 shows potent antinociceptive effects.
|
-
- HY-119383
-
|
iCRT-5
|
β-catenin
|
Cancer
|
|
iCRT-5 is a β-catenin-regulated transcription (CRT) inhibitor. iCRT-5 can block Wnt/β-catenin reporter activity and down regulate β-catenin expression. iCRT-5 can be used for the research of multiple myeloma.
|
-
- HY-105090
-
-
- HY-136561
-
-
- HY-119397
-
|
KDM5-C49
KDOAM-20
|
Histone Demethylase
|
Cancer
|
|
KDM5-C49 (KDOAM-20) is a potent and selective inhibitor of KDM5 demethylases, with IC50s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 can be used for the research of cancer.
|
-
- HY-119397A
-
|
KDM5-C49 hydrochloride
KDOAM-20 hydrochloride
|
Histone Demethylase
|
Cancer
|
|
KDM5-C49 (KDOAM-20) hydrochloride is a potent and selective inhibitor of KDM5 demethylases, with IC50s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 hydrochloride can be used for the research of cancer.
|
-
- HY-142283AS
-
|
Dosimertinib mesylate
|
EGFR
|
Cancer
|
|
Dosimertinib-d5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1].
|
-
- HY-146670
-
|
KDM5B-IN-3
|
Histone Demethylase
|
Cancer
|
|
KDM5B-IN-3 (Compound 5) is a histone lysine specific demethylase 5B (KDM5B/JARID1B) inhibitor with an IC50 of 9.32 μM. KDM5B-IN-3 can be used for the research of gastric cancer.
|
-
- HY-145693
-
|
CDK5-IN-2
|
CDK
|
Others
|
|
CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively.
|
-
- HY-70005
-
-
- HY-14261
-
-
- HY-145334
-
|
CD73-IN-5
|
CD73
|
Cancer
|
|
CD73-IN-5 is a potent and selective non-nucleotide small molecule inhibitor of CD73 (IC50 = 19 nM).
|
-
- HY-B0231AS
-
-
- HY-108321S
-
-
- HY-U00022
-
-
- HY-U00028
-
-
- HY-B0141A
-
-
- HY-B0231BS
-
-
- HY-15025AS
-
-
- HY-108348
-
|
BML-259
|
CDK
|
Neurological Disease
|
|
BML-259 is a potent cyclin-dependent kinase 5 (Cdk5) inhibitor, with IC50s of 64 and 98 nM for Cdk5 and Cdk2, respectively.
|
-
- HY-112390A
-
|
Syk Inhibitor II
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-112390
-
|
Syk Inhibitor II dihydrochloride
|
5-HT Receptor
Syk
|
Inflammation/Immunology
|
|
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-U00439
-
-
- HY-106406
-
|
Benzylacyclouridine
BAU; 5-Benzylacyclouridine
|
Others
|
Cancer
|
|
Benzylacyclouridine (BAU) is a potent and specific inhibitor of uridine phosphorylase, the first enzyme in the catabolism of uridine. Benzylacyclouridine can modulate the cytotoxic side effects of 5-fluorouracil (5-FU) and its derivatives.
|
-
- HY-132297
-
|
PARP1-IN-5
|
PARP
|
Cancer
|
|
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer.
|
-
- HY-132297A
-
|
PARP1-IN-5 dihydrochloride
|
PARP
|
Cancer
|
|
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.
|
-
- HY-139611
-
-
- HY-148949
-
|
Kallikrein 5-IN-2
|
Others
|
Others
|
|
Kallikrein 5-IN-2 (compound 21) is a selective Kallikrein KLK5 inhibitor (pIC50=7.1). KLK5 inhibition may normalise epidermal shedding and reduce the associated inflammation and itching.
|
-
- HY-139611C
-
-
- HY-100714A
-
|
D-AP5
D-APV; D-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
|
|
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors.
|
-
- HY-N11675
-
-
- HY-W009538
-
-
- HY-139691
-
|
SR15006
|
KLF
|
Cancer
|
|
SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells).
|
-
- HY-117853
-
|
Atreleuton
ABT-761; VIA-2291
|
Lipoxygenase
|
Cardiovascular Disease
|
|
Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation.
|
-
- HY-137655
-
|
BMS-P5
|
Protein Arginine Deiminase
|
Cancer
|
|
BMS-P5 is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model.
|
-
- HY-139779
-
|
β-Lactamase-IN-5
|
Bacterial
|
Infection
|
|
β-Lactamase-IN-5 is a β-lactamase inhibitor extracted from patent WO2013149121A1, compound 720. β-Lactamase-IN-5 can be used for the research of bacterial infections.
|
-
- HY-N2020
-
-
- HY-18253
-
|
Udenafil
DA8159
|
Phosphodiesterase (PDE)
|
Endocrinology
Others
|
|
Udenafil (DA8159) is a potent, selective and orally active phosphodiesterase type 5 (PDE5) inhibitor. Udenafil also inhibits cGMP hydrolysis and can be used for erectile dysfunction research.
|
-
- HY-146699
-
|
MtTMPK-IN-5
|
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-111753
-
|
WDR5-IN-4
|
Histone Methyltransferase
|
Cancer
|
|
WDR5-IN-4 is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
|
-
- HY-11018
-
-
- HY-111745
-
|
Tyk2-IN-5
|
JAK
|
Inflammation/Immunology
|
|
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.
|
-
- HY-14434
-
|
Asunaprevir
BMS-650032
|
HCV
HCV Protease
SARS-CoV
|
Infection
|
|
Asunaprevir (BMS-650032) is a potent and orally bioavailable hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM. Asunaprevir inhibits SARS-CoV-2 3CL pro activity.
|
-
- HY-136220A
-
|
AHR antagonist 5 hemimaleate
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).
|
-
- HY-16938
-
|
5'-Methylthioadenosine
5'-(Methylthio)-5'-deoxyadenosine; 5'-Deoxy-5'-(methylthio)adenosine; 5'-S-Methyl-5'-thioadenosine
|
Endogenous Metabolite
Apoptosis
Parasite
|
Cancer
Metabolic Disease
|
|
5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis.
|
-
- HY-12953
-
-
- HY-W006566
-
|
5-AIQ
5-Aminoisoquinolin-1-one
|
PARP
|
Cancer
|
|
5-AIQ (5-Aminoisoquinolin-1-one) is a water-soluble PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver.
|
-
- HY-103089
-
|
LY393558
|
5-HT Receptor
|
Neurological Disease
|
|
LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression.
|
-
- HY-130244
-
|
BACE1-IN-5
|
Beta-secretase
|
Neurological Disease
|
|
BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux.
|
-
- HY-147527
-
|
CDK8-IN-5
|
CDK
|
Inflammation/Immunology
|
|
CDK8-IN-5 is a potent CDK8 inhibitor with an IC50 of 72 nM. CDK8-IN-5 shows anti-inflammatory activities with 43% IL-10 enhancement rate. CDK8-IN-5 has the potential for the research of inflammatory bowel disease.
|
-
- HY-131493
-
|
PF-06939999
PRMT5-IN-3
|
Histone Methyltransferase
|
Cancer
|
|
PF-06939999 (PRMT5-IN-3) is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents.
|
-
- HY-100650
-
|
Carbodenafil
|
Phosphodiesterase (PDE)
|
Others
|
|
Carbodenafil is a Sildenafil (UK-92480) related compound found in health foods. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.
|
-
- HY-15025S
-
-
- HY-136774
-
|
BCL6-IN-5
|
Bcl-2 Family
|
Cancer
|
|
BCL6-IN-5 is a potent BCL6 inhibitor exacted from patent WO2018215801A1, example 1n, has a pIC50 of 5.82.
|
-
- HY-111931
-
-
- HY-145420
-
|
IRE1α kinase-IN-5
|
IRE1
|
Others
|
|
IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α.
|
-
- HY-152094
-
|
SRD5A1-IN-1
|
Others
|
Endocrinology
|
|
SRD5A1-IN-1 (Compound 4) is a competitive and covalent steroid 5α-reductase type 1 (SRD5A1) inhibitor with an IC50 of 1.44 µM. SRD5A1-IN-1 modulates SRD5A1 function, leading to a lower level of dihydrotestosterone (DHT) production and SRD5A1 protein suppression.
|
-
- HY-15414S
-
-
- HY-100235
-
-
- HY-118835
-
-
- HY-148040
-
-
- HY-100130
-
-
- HY-18625
-
-
- HY-18625A
-
-
- HY-13032B
-
-
- HY-19956
-
|
GI254023X
GI4023; SRI028594
|
MMP
|
Cancer
|
|
GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.
|
-
- HY-131284
-
|
(S)-Dehydro Venlafaxine
|
Drug Metabolite
|
Others
|
|
(S)-Dehydro Venlafaxine is an inactive S-enantiomer of Dehydro Venlafaxine. Dehydro Venlafaxine is an impurity of Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is a potent serotonin (5-HT) / norepinephrine (NE) reuptake dual inhibitor.
|
-
- HY-112390B
-
|
Syk Inhibitor II dihydrochloride dihydrate
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-136220
-
|
AHR antagonist 5
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
|
-
- HY-150565
-
|
P-gp inhibitor 5
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 5 is a potent P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-In TM-293 and KBvin cells by restoring their sensitivity to Vincristine (HY-N0488A) and Paclitaxel (HY-B0015).
|
-
- HY-16938S
-
|
5'-Methylthioadenosine-13C6
-(Methylthio)-5'-deoxyadenosine-13C6; 5'-Deoxy-5'-(methylthio)adenosine-13C6; 5'-S-Methyl-5'-thioadenosine-13C6
|
Endogenous Metabolite
Apoptosis
|
Cancer
Metabolic Disease
|
|
5'-Methylthioadenosine- 13C6 is the 13C-labeled 5'-Methylthioadenosine. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis[1]. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2].
|
-
- HY-16938S1
-
|
5'-Methylthioadenosine-d3
5'-(Methylthio)-5'-deoxyadenosine-d3; 5'-Deoxy-5'-(methylthio)adenosine-d3; 5'-S-Methyl-5'-thioadenosine-d3
|
Apoptosis
Parasite
Endogenous Metabolite
|
|
|
5'-Methylthioadenosine-d3 is the deuterium labeled 5'-Methylthioadenosine[1]. 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis[2][3][4].
|
-
- HY-15027S1
-
-
- HY-117082
-
|
UTL-5g
GBL-5g
|
TNF Receptor
|
Inflammation/Immunology
|
|
UTL-5g (GBL-5g), an anti-inflammatory TNF-α inhibitor, has chemoprotective and liver radioprotective effects. UTL-5g lowers hepatotoxicity, nephrotoxicity, and myelotoxicity induced by Cisplatin through TNF-α inhibition among other factors.
|
-
- HY-151576
-
|
PRMT5:MEP50 PPI
|
Others
|
Cancer
|
|
PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells.
|
-
- HY-N2008
-
-
- HY-111753A
-
|
WDR5-IN-4 TFA
|
Histone Methyltransferase
|
Cancer
|
|
WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
|
-
- HY-144429
-
|
TRPC5-IN-4
|
TRP Channel
|
Metabolic Disease
|
|
TRPC5-IN-4 is potent and safe TRPC inhibitor with IC50 value of 14.07 nM and 65 nM for TRPC5 and TRPC4, respectively. TRPC5-IN-4 shows no damage on the cellular component of liver and kidney. TRPC5-IN-4 can be used for the research of chronic kidney disease (CKD).
|
-
- HY-143207
-
-
- HY-10351A
-
|
Robalzotan hydrochloride
NAD-299 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Robalzotan hydrochloride (NAD-299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system.
|
-
- HY-W014316
-
|
5-Bromo-5-nitro-1,3-dioxane
|
Bacterial
Fungal
|
Infection
|
|
5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol.
|
-
- HY-11018A
-
-
- 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-N9179
-
|
3′,4′,5′,5,6,7-Hexamethoxyflavone
|
Parasite
|
Infection
|
|
3′,4′,5′,5,6,7-Hexamethoxyflavone is a flavonoid with antiprotozoal activity. 3′,4′,5′,5,6,7-Hexamethoxyflavone inhibits trypanosoma bruceirhodesiense with IC50 of 21.3 μM (8.58 g/mL).
|
-
- HY-151470
-
|
Chitinase-IN-5
|
Parasite
|
Others
|
|
Chitinase-IN-5 (8i) is a potent chitinase OfChi-h inhibitor with an IC50 value of 0.051 μM. Chitinase-IN-5 shows good insecticidal activity, it can be used for the research of green pest control and management.
|
-
- HY-132309
-
|
BRD0639
|
Histone Methyltransferase
|
Cancer
|
|
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.
|
-
- HY-145078
-
-
- HY-15025S1
-
-
- HY-B0215
-
-
- HY-B0442S
-
|
Vardenafil-d5
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Endocrinology
|
|
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
|
-
- HY-12364
-
|
C75
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator.
|
-
- HY-146261
-
|
HI5
|
Microtubule/Tubulin
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
|
Cancer
|
|
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer.
|
-
- HY-138767
-
|
AKT-IN-5
|
Akt
|
Cancer
|
|
AKT-IN-5 (Example 8) is a Akt inhibitor with IC50 values of 450 nM and 400 nM for Akt1 and Akt2, respectively.
|
-
- HY-117374
-
|
HDAC3-IN-1
|
HDAC
|
Cancer
|
|
HDAC3-IN-1 (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM.
|
-
- HY-18305
-
|
BMS-5
LIMKi 3
|
LIM Kinase (LIMK)
|
Cancer
|
|
BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.
|
-
- HY-139650
-
|
HDAC1/2-IN-3
|
HDAC
|
Cancer
|
|
HDAC1/2-IN-3 is a HDAC1 and HDAC2 inhibitor with IC50 values 0-5 and 5-10 nM, respectively.
|
-
- HY-30236
-
|
5-Bromoindole
|
Others
|
Cancer
|
|
5-Bromoindole is a chemical intermediate that can be used for the synthesis of GSK-3 inhibitors and anti-cancer agents.
|
-
- HY-128569
-
-
- HY-B1847S1
-
-
- HY-150961
-
-
- HY-150975
-
-
- HY-B0588S
-
|
Brinzolamide-d5
AL-4862-d5
|
Carbonic Anhydrase
|
Others
|
|
Brinzolamide-d5 is the deuterium labeled Brinzolamide. Brinzolamide (AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.
|
-
- HY-B0444S
-
-
- HY-100261
-
-
- HY-17390
-
-
- HY-17390B
-
-
- HY-136352
-
|
Adenosine 5'-succinate
|
Others
|
Others
|
|
Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
|
-
- HY-13631AS
-
|
Exatecan-d5 mesylate
DX8951f-d5; Exatecan-d5 (mesylate); Deuterated labeled Exatecan (mesylate)
|
Topoisomerase
|
Cancer
|
|
Exatecan-d5 (mesylate) is deuterium labeled Exatecan mesylate. Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL[1].
|
-
- HY-101157
-
|
Propargyl-PEG5-acid
|
ADC Linker
PROTAC Linkers
|
Cancer
|
|
Propargyl-PEG5-acid is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-acid can used to synthesize ADC inhibitors of Galectin-3. Propargyl-PEG5-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-145694
-
|
CDK5-IN-3
|
CDK
|
Metabolic Disease
|
|
CDK5-IN-3 (compound 11) is a potent and selective CDK5 inhibitor, with IC50s of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. CDK5-IN-3 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD).
|
-
- HY-118283
-
|
5-Hydroxylansoprazole
AG1908
|
Proton Pump
|
Metabolic Disease
|
|
5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole in plasma. Lansoprazole is metabolized by CYP2C19 forming 5-Hydroxylansoprazole. Lansoprazole is a gastric proton-pump inhibitor and is effective in the treatment of various peptic diseases.
|
-
- HY-146359
-
-
- HY-144798
-
|
FWM-5
|
SARS-CoV
|
Infection
|
|
FWM-5 is a potent NSP13 helicase inhibitor. SARS-COV-2 NSP13 helicase enzyme plays crucial role in the virus life cycle. FWM-5 has the potential for the research of infection diseases.
|
-
- HY-108372
-
|
Boc-C5-O-C5-O-C6-Cl
PROTAC Linker 2
|
PROTAC Linkers
|
Cancer
|
|
Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
|
-
- HY-144299
-
-
- HY-147988
-
-
- HY-P0095
-
|
Acetyl tetrapeptide-5
|
Angiotensin-converting Enzyme (ACE)
|
Others
|
|
Acetyl tetrapeptide-5 inhibits glycosylation and ACE-1 activity. Acetyl tetrapeptide-5 reduces edema and relieves vascular pressure by improving the vascular system and strengthening the skin under the eyes. Acetyl tetrapeptide-5 can be used in the research of Antioxidant, anti-aging skin care.
|
-
- HY-15027S2
-
|
5-Aminosalicylic acid-13C6
Mesalamine-13C6; 5-ASA-13C6; Mesalazine-13C6
|
PPAR
PAK
NF-κB
Endogenous Metabolite
|
|
|
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
|
-
- HY-152187
-
|
Topoisomerase IIα-IN-5
|
Topoisomerase
Apoptosis
|
Others
|
|
Topoisomerase IIα-IN-5 is a topoisomerase II (topo II) α catalytic inhibitor. Topoisomerase IIα-IN-5 intercalates into DNA and binds to the DNA minor groove. Topoisomerase IIα-IN-5 exhibits better efficacy and less genotoxicity than Etoposide (HY-13629).
|
-
- HY-126256
-
|
PRMT5-IN-1
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
|
-
- HY-146390
-
|
Antiproliferative agent-5
|
Autophagy
Reactive Oxygen Species
|
Cancer
|
|
Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer.
|
-
- HY-101755
-
-
- HY-128342
-
|
Complement C5-IN-1
|
Complement System
|
Inflammation/Immunology
|
|
Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM.
|
-
- HY-147186
-
|
5,5'-Difluoro BAPTA
|
Others
|
Others
|
|
5,5'-Difluoro BAPTA is a difluoro-derivative of BAPTA (HY-100168). 5,5'-Difluoro BAPTA is the most widely used probe for studying cytosolic free Ca 2+ by 19F NMR. 5,5'-Difluoro BAPTA has high selectivity for Ca 2+. 5,5'-Difluoro BAPTA can inhibit the growth of pollen tube.
|
-
- HY-100869
-
|
MM-589
|
Histone Methyltransferase
|
Cancer
|
|
MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
|
-
- HY-148001
-
-
- HY-13746
-
|
Sardomozide
CGP 48664; SAM-486A
|
Others
|
Cancer
|
|
Sardomozide is an S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM.
|
-
- HY-19944
-
-
- HY-13746B
-
-
- HY-11018B
-
-
- HY-133248
-
-
- HY-N8399
-
-
- HY-133247
-
-
- HY-18708
-
|
Erdafitinib
JNJ-42756493
|
FGFR
Apoptosis
|
Cancer
|
|
Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
|
-
- HY-128171
-
|
Diflapolin
|
FLAP
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s of 30 and 170 nM, respectively, and suppressed the activity of isolated sEH (IC50=20 nM).
|
-
- HY-129101
-
|
(-)-Eseroline fumarate
Eseroline fumarate
|
5-HT Receptor
|
Neurological Disease
|
|
(-)-Eseroline fumarate is a metabolic of Physostigmine (HY-N6608), an AChE inhibitor. (-)-Eseroline fumarate elicits a leakage of lactic acid dehydrogenase (LDH) from cancer cells. (-)-Eseroline fumarate also induces the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, thus induce cell death. (-)-Eseroline fumarate inhibits the electrically evoked twitches of the mouse vas deferens and of the guinea-pig ileum.
|
-
- HY-P99520
-
|
Vilobelimab
CaCP-29, IFX-1
|
Complement System
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Vilobelimab (CaCP-29, IFX-1) is a monoclonal anti-C5a antibody to the allergen C5a, a pro-inflammatory complement division product that plays a central role in mediating organ dysfunction. Vilobelimab acts as a C5a inhibitor, inhibiting neutrophil activation, chemotaxis, and reducing inflammatory signalling, and may be used in studies related to sepsis, COVID-19, etc.
|
-
- HY-100552
-
|
VUF10166
|
5-HT Receptor
|
Neurological Disease
|
|
VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM.
|
-
- HY-146665
-
-
- HY-Y1093S2
-
|
Ethyl acetoacetate-d5
Ethyl acetylacetate-d5
|
Bacterial
|
Others
|
|
Ethyl acetoacetate-d5 is the deuterium labeled Ethyl acetoacetate[1]. Ethyl acetoacetate (Ethyl acetylacetate) is an ester widely used as an intermediate in the synthesis of many varieties of compounds[2][3][4]. Ethyl acetoacetate is an inhibitor of bacterial biofilm[5].
|
-
- 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 agent.
|
-
- HY-148779
-
|
FGFR3-IN-5
|
FGFR
|
Cancer
|
|
FGFR3-IN-5 is a potent and selective FGFR3 inhibitor with IC50 values of 3, 44, and 289 nM for FGFR3, FGFR2, and FGFR1, respectively. FGFR3-IN-5 can be used in research of cancer.
|
-
- HY-137655A
-
|
BMS-P5 free base
|
Protein Arginine Deiminase
|
Cancer
|
|
BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model.
|
-
- HY-150022
-
-
- HY-146675
-
|
COX/5-LOX-IN-1
|
COX
|
Inflammation/Immunology
|
|
COX/5-LOX-IN-1 (compound 6b) is a potent and dual inhibitor of COX/5-LOX with IC50s of 1.07, 0.55, and 0.28 μM for COX-1, COX-2, and 5-LOX enzyme, respectively. COX/5-LOX-IN-1 has the potential for the research of inflammation diseases.
|
-
- HY-120400
-
|
KDM5-C70
|
Histone Demethylase
|
Cancer
|
|
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.
|
-
- HY-15414AS
-
-
- HY-148000
-
-
- HY-114189
-
|
GW284543
UNC10225170
|
MEK
|
Cancer
|
|
GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein.
|
-
- HY-114189A
-
|
GW284543 hydrochloride
UNC10225170 hydrochloride
|
MEK
|
Cancer
|
|
GW284543 (UNC10225170) hydrochloride is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein.
|
-
- HY-14113
-
-
- HY-B0196A
-
-
- HY-13927
-
-
- HY-B0196
-
-
- HY-B1272
-
-
- HY-144176
-
-
- HY-134851
-
|
HIV-1 inhibitor-6
|
HIV
|
Infection
|
|
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM.
|
-
- HY-115981
-
|
NS5A-IN-2
|
HCV Protease
|
Infection
|
|
NS5A-IN-2 (Compound 33) is a potent inhibitor of NS5A. NS5A-IN-2 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability.
|
-
- HY-111861
-
|
SNIPER(ABL)-024
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM.
|
-
- HY-146147
-
-
- HY-112125
-
-
- HY-147080A
-
|
Non-PEGylated/naked ARC1905
|
Complement System
|
Others
|
|
Non-PEGylated/naked ARC1905 is is an anti-C5 RNA aptamer without PEG conjugation. Non-PEGylated/naked ARC1905 inhibits the cleavage of complement factor 5 (C5) into C5a and C5b. Non-PEGylated/naked ARC1905 is being used for the study of age-related macular degeneration (AMD).
|
-
- HY-145061
-
|
ADAMTS-5-IN-3
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
ADAMTS-5-IN-3 (Example 37-2) is a potent inhibitor of ADAMTS-5 and ADAMTS-4 with IC50s of 8 and 12 nM, respectively. ADAMTS-5-IN-3 can be used for the research of diseases involving degradation of cartilage or disruption of cartilage homeostasis, in particular osteoarthrosis and/or rheumatoid arthritis.
|
-
- HY-147585
-
|
C5aR-IN-1
|
Complement System
|
Inflammation/Immunology
|
|
C5aR-IN-1 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-1 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 47).
|
-
- HY-147587
-
|
C5aR-IN-3
|
Complement System
|
Inflammation/Immunology
|
|
C5aR-IN-3 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-3 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 89).
|
-
- HY-126256A
-
|
PRMT5-IN-1 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
|
-
- HY-147586
-
|
C5aR-IN-2
|
Complement System
|
Inflammation/Immunology
|
|
C5aR-IN-2 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-2 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 49).
|
-
- HY-110216
-
|
5J-4
|
CRAC Channel
|
Inflammation/Immunology
|
|
5J-4 is a potent CRAC inhibitor. 5J-4 decreases the numbers of infiltrated mononuclear cell into the CNS, and significantly decreases the population of infiltrated CD4+ population. 5J-4 reduces the symptoms and delayed the onset of EAE (experimental autoimmune encephalomyelitis) in mouse model of inflammation.
|
-
- HY-10439
-
|
HPGDS inhibitor 1
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
|
-
- HY-144381
-
|
Glutamate-5-kinase-IN-1
|
Bacterial
|
Infection
|
|
Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents.
|
-
- HY-144382
-
|
Glutamate-5-kinase-IN-2
|
Bacterial
|
Infection
|
|
Glutamate-5-kinase-IN-2 (compound 54) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.2 µM. Glutamate-5-kinase-IN-2 shows G5K inhibition by promotes conformational changes at the L-glutamate binding site. Glutamate-5-kinase-IN-2 has the potential for the research of anti-TB agents.
|
-
- HY-N1942
-
|
5-O-Demethylnobiletin
5-Demethylnobiletin
|
Lipoxygenase
Leukotriene Receptor
|
Inflammation/Immunology
Neurological Disease
Cancer
|
|
5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
|
-
- HY-131999
-
-
- HY-151798
-
|
TDI-11861
|
Adenylate Cyclase
|
Others
|
|
TDI-11861 is second-generation soluble Adenylyl Cyclase (sAC, ADCY10) inhibitor with slow dissociation rates. TDI-11861 inhibits sAC cellular with an IC50 value of 5.5 nM.
|
-
- HY-19696S
-
|
Tauroursodeoxycholate-d5
|
ERK
Caspase
Endogenous Metabolite
Apoptosis
|
Cancer
|
|
Tauroursodeoxycholate-d5 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
|
-
- HY-12357S
-
-
- HY-112809
-
|
GSK2646264
|
Syk
Src
LRRK2
GSK-3
JAK
VEGFR
Aurora Kinase
|
Inflammation/Immunology
|
|
GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.
|
-
- HY-111640
-
|
3'-Azido-3'-deoxy-5-methylcytidine
|
HIV
Reverse Transcriptase
|
Infection
|
|
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells.
|
-
- HY-N7514
-
|
Strictosidinic acid
|
5-HT Receptor
|
Neurological Disease
|
|
Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice.
|
-
- HY-143736
-
|
RAD51-IN-5
|
RAD51
|
Cancer
|
|
RAD51-IN-5 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-5 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2021164746A1, compound 3).
|
-
- HY-104039
-
-
- HY-10679A
-
|
PF-03049423
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
PF-03049423 (Compound PF-5) is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 can be used for the research of acute ischaemic stroke.
|
-
- HY-B0144AS1
-
|
Pitavastatin-d5 sodium
NK-104-d5 (sodium)
|
Mitophagy
HMG-CoA Reductase (HMGCR)
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
|
|
Pitavastatin-d5 (sodium) is the deuterium labeled Pitavastatin sodium. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
|
-
- HY-100869A
-
|
MM-589 TFA
|
Histone Methyltransferase
|
Cancer
|
|
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
|
-
- HY-123981
-
|
5MPN
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines.
|
-
- HY-143423A
-
|
(S)-MALT1-IN-5
|
MALT1
|
Cancer
Inflammation/Immunology
|
|
(S)-MALT1-IN-5 is a potent inhibitor of MALT1 protease. (S)-MALT1-IN-5 inhibits the activity of MALT1 is expected to be able to correct the enhancement of MALT1 activity due to abnormality of T cell receptor signal or B cell receptor signal, and cancer or inflammatory disease caused by MALT1 activity is expected. (S)-MALT1-IN-5 has the potential for the research of MALT1-related diseases (extracted from patent WO2020111087A1, compound 1).
|
-
- HY-15971A
-
|
AMD 3465
GENZ-644494
|
CXCR
HIV
|
Infection
Endocrinology
|
|
AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
|
-
- HY-110232
-
-
- HY-139894
-
-
- HY-119938
-
-
- HY-143281
-
-
- HY-13060
-
-
- HY-D1640
-
|
5',5-Difluoro BAPTA tetrapotassium
|
Biochemical Assay Reagents
|
Others
|
|
5,5'-Difluoro BAPTA tetrapotassium is a difluoro-derivative of BAPTA (HY-100168). 5,5'-Difluoro BAPTA tetrapotassium shows large 19F NMR chemical shifts upon chelating divalent cations. 5,5'-Difluoro BAPTA tetrapotassium has high selectivity for Ca 2+. 5,5'-Difluoro BAPTA tetrapotassium can inhibit the growth of pollen tube.
|
-
- HY-115567
-
|
5-NIdR
1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole
|
Apoptosis
|
Cancer
|
|
5-NIdR (1-(β-D-2-Deoxyribofuranosyl)-5-nitroindole), an artificial nucleoside, exhibits the ability to inhibit the replication of DNA lesions generated by Temozolomide (HY-17364). 5-NIdR induces cancer cells apoptosis and arrests cell cycle at G0 phase. 5-NIdR enhances Temozolomide anti-tumor efficacy in murine glioblastoma model.
|
-
- HY-15738
-
|
GNF-5
|
Bcr-Abl
|
Cancer
|
|
GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer.
|
-
- HY-103156
-
|
NAS-181 dimesylate
|
5-HT Receptor
|
Neurological Disease
|
|
NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors.
|
-
- HY-147786
-
|
TGFβRI-IN-5
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-5 (Compound 4b) is a potent inhibitor of TGFβRI with an IC50 of 0.08 μM. TGFβRI-IN-5 displays amazing anticancer activity 5–7 times that of reference agent against all the tested cell lines. TGFβRI-IN-5 enhances apoptosis and arrested G2/M phase of cell cycle.
|
-
- HY-N0652
-
|
2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside
2,3,4',5-Tetrahydroxystilbene 2-O-D-glucoside
|
Others
|
Others
|
|
2,3,4',5-tetrahydroxystilbene 2-O-D-glucoside isolats from the roots of Polygonaceae species, inhibits the formation of 5-HETE, HHT and thromboxane B2, although less strongly.
|
-
- HY-10544
-
|
Tegobuvir
GS 333126; GS-9190
|
HCV
|
Infection
|
|
Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
|
-
- HY-103350
-
-
- HY-19735
-
-
- HY-B0170
-
-
- HY-17016S
-
|
Oseltamivir-d5 phosphate
GS 4104-d5
|
Influenza Virus
|
Infection
|
|
Oseltamivir-d5 (phosphate) is the deuterium labeled Oseltamivir phosphate. Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B[1][2].
|
-
- HY-145363
-
-
- HY-12495
-
-
- HY-19205A
-
-
- HY-101563
-
-
- 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-B1122
-
-
- HY-19548A
-
-
- HY-101474BS
-
-
- HY-14164S
-
-
- HY-15504A
-
|
RGB-286638 free base
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-15504
-
|
RGB-286638
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-W010791
-
|
Adenosine 5'-diphosphate sodium salt
|
Endogenous Metabolite
|
Others
|
|
Adenosine 5'-diphosphate (ADP) sodium salt is a nucleoside diphosphate, which is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate sodium salt induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
|
-
- HY-144265
-
-
- HY-113492
-
-
- HY-101298
-
|
Paprotrain
|
Kinesin
|
Neurological Disease
|
|
Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.
|
-
- HY-121162
-
-
- HY-N7683
-
|
Prunetin 5-O-β-D-glucopyranoside
|
Glucosidase
|
Metabolic Disease
|
|
Prunetin 5-O-β-D-glucopyranoside is an isoflavone isolated from extracts of Potentilla astracanica. Prunetin 5-O-β-D-glucopyranoside is a potent and uncompetitive inhibitor of α-glucosidase, with an IC50 of 56.05 μg/mL. Prunetin 5-O-β-D-glucopyranoside can be used for the research of type-2 diabetes.
|
-
- HY-144284
-
|
MsbA-IN-5
|
Bacterial
|
Infection
|
|
MsbA-IN-5 (compound 40) is a potent and highly selective MsbA inhibitor with an IC50 value of 2 nM. MsbA-IN-5 has inhibitory activity against Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae with MICs of 12 μM, 12 μM and 25 μM, respectively. MsbA-IN-5 can be used for researching anti-Gram-negative bacteria.
|
-
- HY-146543
-
|
KRAS inhibitor-13
|
Ras
|
Cancer
|
|
KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers.
|
-
- HY-143306
-
|
IDH1 Inhibitor 5
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor. IDH1 Inhibitor 5 inhibits MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC50s of 64.4 and 34.9 nM, respectively.
|
-
- HY-121638
-
|
CU-3
|
Apoptosis
DGK
|
Cancer
Inflammation/Immunology
|
|
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
|
-
- HY-145048
-
|
SOS1-IN-5
|
Ras
|
Cancer
|
|
SOS1-IN-5 is a potent inhibitor of SOS1. SOS1-IN-5 is a pyrimidobicyclic derivative. SOS1-IN-5 blocks the activation of KRAS by interfering with RAS-SOS1 interaction, and achieves the purpose of broad-spectrum inhibition of KRAS activity. SOS1-IN-5 has the potential for the research of cancer diseases (extracted from patent WO2021203768A1, compound 4).
|
-
- HY-129983
-
|
5-Hydroxymethyl-2'-deoxyuridine
|
HSV
|
Cancer
Infection
|
|
5-Hydroxymethyl-2'-deoxyuridine is a nucleoside analog. 5-Hydroxymethyl-2'-deoxyuridine inhibits the replication of multiple human leukemia cell lines with IC50 values of 1.7-5.8 μM. 5-Hydroxymethyl-2'-deoxyuridine prolongs the survival of mice carrying L1210 leukemia. 5-Hydroxymethyl-2'-deoxyuridine can be used for the research of cell replication and leukemia.
|
-
- HY-128341
-
|
ERK5-IN-2
|
ERK
|
Cancer
Cardiovascular Disease
|
|
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
|
-
- HY-15971
-
|
AMD 3465 hexahydrobromide
GENZ-644494 hexahydrobromide
|
CXCR
HIV
|
Infection
Endocrinology
|
|
AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
|
-
- HY-152100
-
|
CUR5g
|
Autophagy
|
Cancer
|
|
CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo.
|
-
- HY-19807
-
|
Indirubin-3'-monoxime
Indirubin-3'-oxime
|
GSK-3
CDK
Lipoxygenase
|
Cancer
|
|
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
|
-
- HY-124591
-
|
TC-2153
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and 5-HT1A receptors mRNA level in midbrain. TC-2153 also inhibits 5-HT2A receptor-mediated signaling.
|
-
- HY-17385S
-
-
- HY-129138
-
-
- HY-147620
-
|
FGFR-IN-5
|
FGFR
|
Cancer
|
|
FGFR-IN-5 is a potent inhibitor of FGFR. Fibroblast growth factor receptor (FGFR) is a tyrosine kinase receptor that binds to fibroblast growth factor ligands. FGFR-IN-5 has the potential for the research of cancer diseases (extracted from patent WO2022042612A1, compound 3).
|
-
- HY-154019
-
-
- HY-115581
-
|
Thymidine 3',5'-disphosphate
Deoxythymidine 3′,5′-diphosphate; pdTp
|
Apoptosis
|
Cancer
|
|
Thymidine 3',5'-disphosphate (Deoxythymidine 3′,5′-diphosphate; pdTp) is a selective small molecule inhibitor of staphylococcal nuclease and tudor domain containing 1 (SND1, the miRNA regulatory complex RISC subunit) and inhibits SND1 activity. Thymidine 3',5'-disphosphate exhibits anti-tumor efficacy in vivo.
|
-
- HY-10572S
-
|
Efavirenz-d5
|
Reverse Transcriptase
HIV
Autophagy
|
Infection
Cancer
|
|
Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
|
-
- HY-135194
-
|
Risperidone E-oxime
|
Drug Metabolite
|
Others
|
|
Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
|
-
- HY-117605S
-
-
- HY-15427
-
|
GDC-0834
|
Btk
|
Inflammation/Immunology
|
|
GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.
|
-
- HY-150039
-
-
- HY-13685
-
|
Miltefosine
HePC; Hexadecyl phosphocholine
|
Akt
HIV
Parasite
|
Infection
Cancer
|
|
Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).
|
-
- HY-15284S
-
-
- HY-N10402
-
|
Norbatzelladine L
|
Fungal
Bacterial
Parasite
|
Cancer
Infection
|
|
Norbatzelladine L (Compound 2) is an inhibitor of the catalytic and functional activity of Pdr5p transporter. Norbatzelladine L inhibits Pdr5p ATPase activity with an IC50 of 3.8 µM. Norbatzelladine L shows antifungal, antiparasitic, antiviral, antibacterial and antitumoral activities.
|
-
- HY-12814A
-
-
- HY-12814
-
|
TH588
|
DNA/RNA Synthesis
|
Cancer
|
|
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
|
-
- HY-18928
-
|
FAK inhibitor 5
|
FAK
|
Cancer
|
|
FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
|
-
- HY-111408
-
-
- HY-143733
-
|
HER2-IN-5
|
EGFR
|
Cancer
|
|
HER2-IN-5 is a potent and orally active HER-2 inhibitor, example 10, extracted from patent WO2021164697.
|
-
- HY-112553
-
|
HZ52
|
Lipoxygenase
|
Inflammation/Immunology
|
|
HZ52 is a potent, reversible 5-lipoxygenase inhibitor, blocking leukotriene synthesis with an IC50 of 0.7 μM in intact human polymorphonuclear leukocytes.
|
-
- HY-112502C
-
|
MethADP triammonium
Adenosine 5'-(α,β-methylene)diphosphate triammonium
|
CD73
|
Cancer
|
|
MethADP (Adenosine 5'-(α,β-methylene)diphosphate) triammonium is a CD73 inhibitor. MethADP can be used for the research of ATP-adenosine pathway.
|
-
- HY-W002008
-
-
- HY-15315
-
|
Baricitinib
LY3009104; INCB028050
|
JAK
|
Inflammation/Immunology
|
|
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-B0393
-
-
- HY-14550A
-
-
- HY-151596
-
-
- HY-139150
-
|
EZH2-IN-4
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.
|
-
- HY-N10623
-
|
5-epi-Arvestonate A
|
Tyrosinase
|
Cancer
|
|
5-epi-Arvestonate A is a sesquiterpenoid isolated from the whole plants of Seriphidium transiliense. 5-epi-Arvestonate A promotes melanogenic production by activating the transcription of microphthalmia-associated transcription factor (MITF) and tyrosinase family genes. 5-epi-Arvestonate A inhibits the expression of IFN-γ-chemokine through the JAK/STAT signaling pathway in immortalized human keratinocyte (HaCaT) cells.
|
-
- HY-117048
-
|
PF-4191834
PF-04191834
|
Lipoxygenase
|
Inflammation/Immunology
|
|
PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain.
|
-
- HY-18302
-
|
c-Kit-IN-5-1
|
c-Kit
|
Inflammation/Immunology
|
|
c-Kit-IN-5 is potent inhibitor of c-Kit, with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties.
|
-
- HY-121638A
-
|
(5Z,2E)-CU-3
|
Apoptosis
DGK
|
Cancer
|
|
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
|
-
- HY-103440
-
|
EGFR/ErbB-2/ErbB-4 inhibitor-3
|
EGFR
|
Cancer
|
|
EGFR/ErbB-2/ErbB-4 inhibitor-3 (compound 29) is a potent tyrosine kinase inhibitor with IC50s of 0.3, 1.1, 0.5, 2.5, 24 nM for erbB1, erbB2, erbB4, EGF, HER, respectively.
|
-
- HY-B0182
-
|
Carmofur
HCFU
|
Nucleoside Antimetabolite/Analog
SARS-CoV
Virus Protease
|
Cancer
|
|
Carmofur (HCFU), a derivative of 5-Fluorouracil, is an antineoplastic agent. Carmofur is an inhibitor of acid ceramidase with an IC50 of 79 nM for the rat enzyme. Carmofur inhibits the SARS-CoV-2 main protease (Mpro). Carmofur Inhibits SARS-CoV-2 in Vero E6 cell with an EC50 of 24.3 μM.
|
-
- HY-15982
-
-
- HY-100754B
-
-
- HY-147650
-
|
HIV-1 protease-IN-5
|
HIV Protease
|
Infection
|
|
HIV-1 protease-IN-5 (Compound 13c) is a HIV-1 protease inhibitor with an IC50 of 1.64 nM. HIV-1 protease-IN-5 shows remarkable activity against wild-type and DRV-resistant HIV-1 variants.
|
-
- HY-N1957
-
|
Gamma-Mangostin
γ-Mangostin
|
5-HT Receptor
|
Metabolic Disease
|
|
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3 H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 µM) .
|
-
- HY-128343
-
|
KDM4-IN-2
|
Histone Demethylase
|
Cancer
|
|
KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.
|
-
- HY-139888
-
-
- HY-13817
-
-
- HY-101846
-
-
- HY-115717
-
|
UZH2
|
Others
|
Cancer
|
|
UZH2 is a potent and selective METTL3 inhibitor with an IC50 value of 5 nM.
|
-
- HY-15984
-
-
- HY-B0170A
-
-
- HY-145335
-
-
- HY-N10156
-
-
- HY-147951
-
|
COX-2/5-LOX-IN-3
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
COX-2/5-LOX-IN-3 (compound 5b) is a potent and dual COX-2/5-LOX inhibitor with IC50 values of 45.73, 5.45 and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. COX-2/5-LOX-IN-3 has the potential for the research of inflammation diseases.
|
-
- HY-16992A
-
|
W-54011
|
Complement System
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca 2+ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC50s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively.
|
-
- HY-B0215S
-
|
Acetylcysteine-d3
N-Acetylcysteine-d3; N-Acetyl-L-cysteine-d3; NAC-d3
|
Reactive Oxygen Species
Endogenous Metabolite
Apoptosis
Ferroptosis
Influenza Virus
|
Infection
Neurological Disease
|
|
Acetylcysteine-d3 is the deuterium labeled Acetylcysteine. Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor[1]. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases[5]. Acetylcysteine induces cell apoptosis[2][3]. Acetylcysteine also has anti-influenza virus activities[7].
|
-
- HY-101873S
-
-
- HY-144641
-
-
- HY-15391
-
|
Lucitanib
E-3810
|
VEGFR
FGFR
|
Cancer
|
|
Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
|
-
- HY-12334
-
|
HTH-01-015
|
AMPK
|
Cancer
|
|
HTH-01-015 is a selective NUAK1/ARK5 inhibitor (IC50 is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).
|
-
- HY-18253S
-
|
Udenafil-d7
|
Phosphodiesterase (PDE)
|
Endocrinology
Others
|
|
Udenafil-d7 is the deuterium labeled Udenafil. Udenafil (DA8159) is a potent, selective and orally active phosphodiesterase type 5 (PDE5) inhibitor. Udenafil also inhibits cGMP hydrolysis and can be used for erectile dysfunction research[1][2].
|
-
- HY-18684
-
|
SIBA
5'-Isobutylthioadenosine; 5'-Deoxy-5'-isobutylthioadenosine
|
Nucleoside Antimetabolite/Analog
HSV
Parasite
|
Cancer
Infection
Metabolic Disease
|
|
SIBA (5'-Isobutylthioadenosine) is a transmethylation inhibitor (SAH (HY-19528) analogue), with potent anti-proliferative activity. SIBA reversibly inhibits the production of HSV-1 by blocking methylation, specifically by blocking the 5' end-capping of viral mRNA. SIBA also inhibits the growth of tumour cells in vitro and metastatic spread in vivo. SIBA can be used in cancer, HSV-1 infection and anti-malaria studies.
|
-
- HY-10118
-
|
Filibuvir
|
HCV
DNA/RNA Synthesis
|
Infection
|
|
Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively. Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation.
|
-
- HY-13203
-
-
- HY-112704
-
|
PDE5-IN-2
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity.
|
-
- HY-115452
-
|
G5-7
|
JAK
Apoptosis
|
Cancer
|
|
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
|
-
- 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-100859
-
|
LSD1-IN-5
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
|
-
- HY-10679
-
-
- HY-134039
-
|
5-Hydroxy-8-methoxypsoralen
5-Hydroxyxanthotoxin
|
Others
|
Inflammation/Immunology
|
|
5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a metabolite of Xanthotoxin. Xanthotoxin is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight.
|
-
- HY-W083062
-
|
hMAO-B-IN-5
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-5(B15) is a potent, selective and reversible inhibitor of human monoamine oxidase hMAO-B with IC50 of 0.12 μM. hMAO-B-IN-5 can pass through the blood-brain barrier and can be used in the research of neurodegenerative diseases.
|
-
- HY-125990
-
|
SLC13A5-IN-1
|
Sodium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
|
-
- HY-B1033
-
|
Metergoline
|
5-HT Receptor
Dopamine Receptor
Sodium Channel
|
Neurological Disease
|
|
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
|
-
- HY-100014
-
|
KDM5A-IN-1
|
Histone Demethylase
|
Cancer
|
|
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
|
-
- HY-109151
-
|
Milategrast
E6007
|
Others
|
Inflammation/Immunology
|
|
Milategrast is useful as cell adhesion inhibitor or cell infiltration inhibitor. Milategrast in vitro inhibites the adhesion of Jurkat cells to human fibronectin with an IC50 of ＜5 μM.
|
-
- HY-122908
-
|
Atuliflapon
AZD5718
|
FLAP
|
Cardiovascular Disease
|
|
Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
|
-
- HY-15315A
-
|
Baricitinib phosphate
LY3009104 phosphate; INCB028050 phosphate
|
JAK
|
Inflammation/Immunology
|
|
Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-N0473S14
-
|
L-Tyrosine-d5
|
Endogenous Metabolite
|
|
|
L-Tyrosine-d5 is the deuterium labeled L-Tyrosine. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex.
|
-
- HY-112649
-
|
Pomstafib-2
|
STAT
Apoptosis
|
Cancer
|
|
Pomstafib-2 is a potent and selective STAT5b inhibitor. Pomstafib-2 decreases the expression of pSTAT5b and induces Apoptosis.
|
-
- HY-15027
-
-
- HY-150695
-
|
hCAIX/XII-IN-5
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
|
hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis.
|
-
- HY-13635A
-
|
Finasteride acetate
MK-906 acetate
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
|
-
- HY-150054
-
|
G12Si-5
|
Ras
|
Cancer
|
|
G12Si-5 is a covalent inhibitor of the G12S mutant of K-Ras (Ki: 26 μM). G12Si-5 binds with the S-IIP domain and suppresses oncogenic signaling. G12Si-5 reduces phospho-ERK level in KRAS G12S mutated cells.
|
-
- HY-144456
-
|
Xanthine oxidase-IN-5
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model.
|
-
- HY-13635
-
|
Finasteride
MK-906
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
|
-
- HY-15766A
-
|
GNE-617 hydrochloride
|
NAMPT
|
Cancer
|
|
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-15766
-
|
GNE-617
|
NAMPT
|
Metabolic Disease
Cancer
|
|
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-W042648
-
-
- HY-115956
-
|
Tubulin inhibitor 18
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 18 (compound 5j) is a potent inhibitor of tubulin. Tubulin inhibitor 18 is a chalcone compound. Tubulin inhibitor 18 has the potential for the research of cancer diseases.
|
-
- HY-W380450
-
|
Viloxazine
Viloxazin; Emovit
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Viloxazine (Viloxazin) is a norepinephrine reuptake inhibitor, also a potent 5-HT2C agonist and 5-HT2B antagonist with an EC50 of 32 μM and an IC50 of 27 μM for 5-HT2C and 5-HT2B, respectively. The mechanism of action of Viloxazine predominantly involves serotonergic and noradrenergic pathways. Viloxazine can be used for researching depression.
|
-
- HY-146677
-
-
- HY-112648
-
|
Stafib-2
|
STAT
|
Others
|
|
Stafib-2 is a potent and selctive inhibitor of the transcription factor STAT5b, with an IC50 of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively. Stafib-2 exhibits poor cell permeability.
|
-
- HY-115982
-
|
NS5A-IN-3
|
HCV Protease
|
Infection
|
|
NS5A-IN-3 (Compound 15) is a potent inhibitor of NS5A. NS5A-IN-3 has extremely high potency against HCV genotype 1b, improved activity against genotype 3a (GT 3a) and good metabolic stability. NS5A-IN-3 exhibits a higher resistance barrier than daclatasvir against genotype 1b.
|
-
- HY-108470
-
|
Ro5-3335
|
Others
|
Cancer
|
|
Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.
|
-
- HY-17399S
-
|
Racecadotril-d5
Acetorphan-d5
|
Neprilysin
|
Metabolic Disease
|
|
Racecadotril-d5 is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent[1].
|
-
- HY-17468S
-
|
Bumetanide-d5
|
NKCC
|
Cardiovascular Disease
|
|
Bumetanide-d5 is a deuterium labeled Bumetanide. Bumetanide is a selective Na+-K+-Cl- (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively[1].
|
-
- HY-12085S
-
-
- HY-10579
-
|
Pluripotin
SC1
|
Ribosomal S6 Kinase (RSK)
ERK
|
Cancer
|
|
Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 µM, respectively.
|
-
- HY-144829
-
|
PI3Kα-IN-5
|
PI3K
mTOR
|
Cancer
|
|
PI3Kα-IN-5 (Compound 6ab) is a potent PI3Kα inhibitor with an IC50 of 0.7 nM. PI3Kα-IN-5 shows antitumor activity with good metabolic stabilities and safety profiles.
|
-
- HY-P99697
-
|
Leronlimab
PRO 140
|
CCR
HIV
|
Cancer
Infection
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer.
|
-
- HY-N2666
-
|
5α-Hydroxycostic acid
|
VEGFR
|
Cancer
|
|
5α-Hydroxycostic acid, a eudesmane-type sesquiterpene, is isolated from the herb Laggera alata. 5α-Hydroxycostic acid inhibits angiogenesis and suppresses breast cancer cell migration through regulating VEGF/VEGFR2 and Ang2/Tie2 pathways.
|
-
- HY-152978
-
|
2'-Deoxy-5'-O-DMT-N4-Fmoc-5-methylcytidine
|
Others
|
Others
|
|
2'-Deoxy-5'-O-DMT-N4-Fmoc-5-methylcytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities.
|
-
- HY-B0589C
-
|
(3S,5S)-Atorvastatin
|
Cytochrome P450
|
Metabolic Disease
|
|
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-106200
-
|
CJ-13,610
|
Lipoxygenase
|
Inflammation/Immunology
|
|
CJ-13,610, a nonredox-type 5-LO inhibitor, dose dependently suppresses 5-LO product formation in ionophore A23187-stimulated PMNL in the absence of exogenous AA with an IC50 of about 70 nM. PMNL: polymorphonuclear leukocytes; AA: arachidonic acid
|
-
- HY-144452
-
|
Immunoproteasome inhibitor 1
|
Proteasome
|
Cancer
|
|
Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the research of certain neoplastic diseases.
|
-
- HY-18252
-
|
Avanafil
TA1790
|
Phosphodiesterase (PDE)
NO Synthase
Endogenous Metabolite
|
Endocrinology
Cardiovascular Disease
|
|
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis.
|
-
- HY-147705
-
|
PPARγ phosphorylation inhibitor 1
|
PPAR
|
Metabolic Disease
|
|
PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects.
|
-
- HY-13905
-
|
Flumatinib mesylate
HHGV678 mesylate
|
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
|
Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model.
|
-
- HY-18758
-
|
IN-1130
|
TGF-β Receptor
|
Cancer
Inflammation/Immunology
|
|
IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.
|
-
- HY-103046
-
|
UbcH5c-IN-1
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
|
-
- HY-N7656
-
|
5,7,8-Trimethoxyflavone
Norwogonin 5,7,8-trimethyl ether
|
NO Synthase
|
Inflammation/Immunology
|
|
5,7,8-Trimethoxyflavone (Norwogonin 5,7,8-trimethyl ether), isolated from Andrographis echioides, inhibits NO with an IC50 of 39.1 μM. 5,7,8-Trimethoxyflavone has anti-inflammatory activity.
|
-
- HY-152155
-
-
- HY-100959
-
|
3,5-Dinitrocatechol
OR-486; 3,5-Dinitropyrocatechol
|
Others
|
Neurological Disease
|
|
3,5-Dinitrocatechol (OR-486) is a potent catechol-O-methyltransferase inhibitor, with an IC50 of 12 nM. 3,5-Dinitrocatechol can be used in the preparation of the molybdenum (VI)- 3,5-Dinitrocatechol complex.
|
-
- HY-150054A
-
|
G12Si-5 formic
|
Ras
|
Cancer
|
|
G12Si-5 formic is a covalent inhibitor of the G12S mutant of K-Ras (Ki: 26 μM). G12Si-5 formic binds with the S-IIP domain and suppresses oncogenic signaling. G12Si-5 formic reduces phospho-ERK level in KRAS G12S mutated cells.
|
-
- HY-W097792
-
|
5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine
5'-O-DMT-dU
|
DNA/RNA Synthesis
|
Others
|
|
5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks.
|
-
- HY-145294
-
|
ROCK2-IN-5
|
ROCK
|
Neurological Disease
|
|
ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation.
|
-
- HY-123349
-
|
5α-Hydroxy-6-keto cholesterol
|
Drug Metabolite
|
Cardiovascular Disease
|
|
5α-Hydroxy-6-keto cholesterol is major metabolite of β-epoxide (5α,6β-epoxycholesterol) during direct exposure of intact cultured human bronchial epithelial cells (16-HBE) to ozone. 5α-Hydroxy-6-keto cholesterol inhibits cholesterol synthesis with an IC50 of 350 nM.
|
-
- HY-131069A
-
|
MBX2329
|
Influenza Virus
|
Infection
|
|
MBX2329, a potent influenza virus inhibitor, specifically inhibits hemagglutinin (HA)-mediated viral entry with HIV/HA(H5) displaying IC90 of 8.6 μM. MBX2329 inhibits a wide spectrum of influenza A viruses, which includes the 2009 pandemic influenza virus A/H1N1/2009, highly pathogenic avian influenza (HPAI) virus A/H5N1, and oseltamivir-resistant A/H1N1 strains.
|
-
- HY-128067
-
|
5-(N,N-Hexamethylene)-amiloride
Hexamethylene amiloride; HMA
|
Sodium Channel
HIV
Apoptosis
|
Cancer
Infection
|
|
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
|
-
- HY-135128
-
-
- HY-117411A
-
|
Coblopasvir dihydrochloride
KW-136 dihydrochloride
|
HCV
HCV Protease
|
Infection
|
|
Coblopasvir (KW-136) dihydrochloride is a pangenotypic non-structural protein 5A (NS5A) inhibitor. Coblopasvir dihydrochloride can be used for research of chronic hepatitis C virus infection.
|
-
- HY-145809
-
-
- 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 agent, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
|
-
- HY-14841
-
-
- HY-108045
-
-
- HY-B0196B
-
|
(S)-Venlafaxine
|
Serotonin Transporter
|
Cancer
|
|
(S)-Venlafaxine is the (S)-configuration of Venlafaxine. Venlafaxine is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant agent.
|
-
- HY-100696
-
|
PNZ5
|
Epigenetic Reader Domain
|
Cancer
|
|
PNZ5 is a potent and isoxazole-based pan-BET inhibitor with high selectivity and potency similar to the well-established (+)-JQ1, with a KD of 5.43 nM for BRD4(1).
|
-
- HY-147358A
-
|
Yimitasvir
Emitasvir; DAG-181
|
HCV
|
Infection
|
|
Yimitasvir (Emitasvir) is an orally active hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor. Yimitasvir can be used for research of chronic HCV infection.
|
-
- HY-N3558
-
|
Ceanothic acid
Emmolic acid
|
Others
|
Cancer
|
|
Ceanothic acid (Emmolic acid) is a ring-A homologue of betulinic acid. Ceanothic acid inhibits OVCAR-3, HeLa, and FS-5 cells with the cell survival of 68%, 65%, and 81%, respectively.
|
-
- HY-14261S
-
-
- HY-111534
-
-
- HY-B0555BS
-
|
Nafcillin-d5 sodium
|
Antibiotic
|
Infection
|
|
Nafcillin-d5 (sodium) is the deuterium labeled Nafcillin sodium. Nafcillin sodium, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium can be used for the research of staphylococcal infections[1][2].
|
-
- HY-117411
-
-
- HY-12318
-
-
- HY-18206S
-
-
- HY-18630A
-
-
- HY-139645
-
-
- HY-101836
-
-
- HY-111472
-
-
- HY-13465
-
-
- HY-W001179
-
-
- HY-101966
-
-
- HY-B0279
-
-
- HY-90009A
-
-
- HY-12727
-
-
- HY-18630
-
-
- HY-147387
-
|
DSS30
|
CDK
Amyloid-β
|
Inflammation/Immunology
|
|
DSS30 is a P25/CDK5 inhibitor that reduces β-amyloid (Aβ) secretion by inhibiting amyloid precursor protein lyase 1 (BACEl) phosphorylation. DSS30 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
|
-
- HY-10981S1
-
|
Lenvatinib-d5
E7080-d5
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
|
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
|
-
- HY-14768
-
|
Favipiravir
T-705
|
DNA/RNA Synthesis
Influenza Virus
SARS-CoV
Bacterial
|
Infection
|
|
Favipiravir (T-705) is a potent viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with an IC50 of 341 nM.
|
-
- HY-13012G
-
|
RepSox
E-616452; SJN 2511
|
TGF-β Receptor
|
Metabolic Disease
|
|
RepSox (E-616452) (GMP) is a RepSox (HY-13012) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RepSox is a potent and selective TGF-β-RI/ALK5 inhibitor.
|
-
- HY-18763S
-
|
Indobufen-d5
Ibustrin-d5
|
COX
|
Cardiovascular Disease
|
|
Indobufen-d5 is deuterium labeled Indobufen. Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes[1].
|
-
- HY-N10401
-
|
Batzelladine D
|
Fungal
Bacterial
Parasite
|
Cancer
Infection
|
|
Batzelladine D (Compound 1) is an inhibitor of the catalytic and functional activity of Pdr5p transporter. Batzelladine D inhibits Pdr5p ATPase activity with an IC50 of 7.1 µM. Batzelladine D shows antifungal, antiparasitic, antiviral, antibacterial and antitumoral activities.
|
-
- HY-P3785
-
|
PKI(5-22)amide
|
PKA
|
Neurological Disease
|
|
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors.
|
-
- HY-143458
-
|
FAK PROTAC B5
|
FAK
PROTACs
|
Cancer
|
|
FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion.
|
-
- HY-12057S
-
|
Vemurafenib-d5
|
Raf
Autophagy
|
Cancer
|
|
Vemurafenib-d5 is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
|
-
- HY-112732
-
|
Sparfosic acid
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Sparfosic acid, a DNA antimetabolite agent, is a potent inhibitor of aspartate transcarbamoyl transferase, the enzyme catalyzing the second step of de novo pyrimidine biosynthesis. Sparfosic acid synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines.
|
-
- HY-101911
-
|
5-BDBD
|
P2X Receptor
|
Neurological Disease
|
|
5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).
|
-
- HY-111540B
-
|
(S)-IDO1-IN-5
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
(S)-IDO1-IN-5 (Example 1B) is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL with an IC50 value less than 1.5 µΜ. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
|
-
- HY-B0215S1
-
|
Acetylcysteine-15N
N-Acetylcysteine-15N; N-Acetyl-L-cysteine-15N; NAC-15N
|
Reactive Oxygen Species
Endogenous Metabolite
Apoptosis
Ferroptosis
Influenza Virus
|
Infection
Neurological Disease
|
|
Acetylcysteine- 15N (N-Acetylcysteine- 15N) is the 15N-labeled Acetylcysteine. Acetylcysteine (N-Acetylcysteine) is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor[1]. Acetylcysteine is a cysteine precursor, prevents hemin-induced ferroptosis by neutralizing toxic lipids generated by arachidonate-dependent activity of 5-lipoxygenases[5]. Acetylcysteine induces cell apoptosis[2][3]. Acetylcysteine also has anti-influenza virus activities[7].
|
-
- HY-154397
-
-
- HY-N6256
-
-
- HY-146372
-
|
CXCR4 antagonist 5
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately.
|
-
- HY-102047
-
|
KDOAM-25
|
Histone Demethylase
|
Cancer
|
|
KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
|
-
- HY-102047A
-
|
KDOAM-25 trihydrochloride
|
Histone Demethylase
|
Cancer
|
|
KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
|
-
- HY-111540A
-
|
(Rac)-IDO1-IN-5
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
(Rac)-IDO1-IN-5 (Example 1) is a racemate of IDO1-IN-5. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
|
-
- HY-150015
-
|
4,5'-Dimethylangelicin-NHS
|
DNA/RNA Synthesis
|
Cancer
|
|
4,5'-Dimethylangelicin-NHS is a modified 4,5'-Dimethylangelicin containing an NHS. 4,5'-Dimethylangelicin is an angular furocoumarin with photochemical and photosensitizing properties. 4,5'-Dimethylangelicin can inhibit the DNA and RNA syntheses in Ehrlich ascites tumor cells alter irradiation at 365 nm. 4,5'-Dimethylangelicin has potential as a photochemotherapy agent.
|
-
- HY-146126
-
|
NS5A-IN-4
|
HCV Protease
|
Infection
|
|
NS5A-IN-4 (Compound 1.12) is an orally active pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with IC50 values of 1.2, 2296, 4.6, 362, 10.3 and 693 pM against gT1b, gT1a, gT2a, gT3a, gT4a and gT5a.
|
-
- HY-101840
-
-
- HY-101840A
-
|
EIPA hydrochloride
L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride
|
TRP Channel
Autophagy
COX
Prostaglandin Receptor
Na+/H+ Exchanger (NHE)
|
Cancer
Inflammation/Immunology
|
|
EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.
|
-
- HY-102071
-
|
KIN59
5'-O-Tritylinosine; 5'-O-Trityl-inosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
KIN59 (5’-O-Tritylinosine) is a potent thymidine phosphorylase allosteric inhibitor. KIN59 inhibits FGF2-stimulated cell growth. KIN59 inhibits the expression of p-FGFR1, P-Akt in FGF2 (10 ng/mL) stimulated cells. KIN59 shows anti-tumor activity.
|
-
- HY-105336
-
|
3-Deazauridine
NSC 126849
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
|
Cancer
|
|
3-Deazauridine (NSC 126849) is a uridine analogue. 3-Deazauridine competitively inhibits cytidine triphosphate synthase to inhibit the biosynthesis of cytidine-5'-triphosphate. 3-Deazauridine acts synergistically with several antineoplastic agents, acting as a biological response modifier.
|
-
- HY-122243
-
|
IU1-47
|
Deubiquitinase
|
Neurological Disease
|
|
IU1-47 is a potent and specific USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 inhibits IsoT/USP5 with an IC50 of 20 μM. IU1-47 induces tau elimination in cultured neurons.
|
-
- HY-W011834
-
|
2'-O-Methylcytidine
|
HCV
|
Infection
|
|
2'-O-Methylcytidine is a 2'-substituted nucleoside as a inhibitor of HCV replication. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate.
|
-
- HY-B0592S
-
-
- HY-147662
-
|
hCAIX-IN-5
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-5 (compound 6b) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 130.7, 829.1 nM for hCAI, hCAII, hCAIV, hCAIX, respectively.
|
-
- HY-128593
-
-
- HY-146256
-
|
hCAXII-IN-5
|
Carbonic Anhydrase
|
Cancer
|
|
hCAXII-IN-5 (compound 6o) is a potent and selective hCAXII inhibitor with Ki values of >10000, >10000, 286.1, 1.0 nM for hCAI, hCAII, hCAIX and hCAXII, respectively.
|
-
- HY-117109
-
|
Amino Tadalafil
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Amino Tadalafil is an analog of Tadalafil. Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
|
-
- HY-108619
-
-
- HY-100747
-
|
PSB-12379
|
CD73
|
Cancer
|
|
PSB-12379, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).
|
-
- HY-10882S
-
-
- HY-18252A
-
|
Avanafil dibenzenesulfonate
TA1790 dibenzenesulfonate
|
Phosphodiesterase (PDE)
NO Synthase
Endogenous Metabolite
|
Endocrinology
Cardiovascular Disease
|
|
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.
|
-
- HY-101507
-
|
Pico145
HC-608
|
TRP Channel
|
Cancer
|
|
Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
|
-
- HY-107139
-
|
JNJ-10229570
|
Melanocortin Receptor
|
Endocrinology
|
|
JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
|
-
- HY-152031
-
-
- HY-10327
-
-
- HY-18931A
-
|
(Rac)-NSC305787 hydrochloride
|
Others
|
Cancer
|
|
NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
|
-
- HY-15679
-
-
- HY-18931
-
|
(Rac)-NSC305787
|
Others
|
Cancer
|
|
NSC305787 is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
|
-
- HY-112128
-
-
- HY-112164
-
-
- HY-109619
-
|
D4-abiraterone
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-146306
-
|
Neuraminidase-IN-9
|
Influenza Virus
|
Infection
|
|
Neuraminidase-IN-9 (Compound 6l) is a potent influenza neuraminidase inhibitor with IC50 values of 0.12, 0.049 and 0.16 µM against H5N1, H5N2 and H5N6, respectively.
|
-
- HY-114303
-
|
CM-675
|
Phosphodiesterase (PDE)
HDAC
|
Neurological Disease
|
|
CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease.
|
-
- HY-N9975
-
-
- HY-144295
-
|
PI3Ka-IN-5
|
PI3K
mTOR
|
Cancer
|
|
PI3Ka-IN-5 (compound 6 ab) is a potent PI3Kα/mTOR inhibitor, with an IC50 of 0.7 nM and 3.3 nM, respectively. PI3Ka-IN-5 can be used for the research of colorectal cancer.
|
-
- HY-121778
-
|
Melitracen
Melitracene; N 7001; Trausabun
|
Others
|
Neurological Disease
|
|
Melitracen (Melitracene) is an orally active tricyclic antidepressant and it is also a bipolar thymoleptic with activating properties. Melitracen inhibits 3H-5-HT and 14H-5-HT with IC50s of 670 nM and 5500 nM, respectively. Melitracen can be used for the research of depression and anxiety.
|
-
- HY-146155
-
-
- HY-152182
-
|
ML-SA5
|
TRP Channel
|
Cancer
|
ML-SA5 is a potent TRPML1 cation channel agonist that activates the entire endosomal TRPML1 (ML1) current in DMD myocytes with an EC50 of 285 nM and is more potent than ML-SA1. ML-SA5 has anticancer activity and can inhibit tumour growth.
|
-
- HY-146301
-
|
Mt KARI-IN-5
|
Bacterial
|
Infection
|
|
Mt KARI-IN-5 (compound 6c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 4.72 μM. Mt KARI-IN-5 has inhibitory activity against Mtb H37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)
|
-
- HY-100851A
-
|
LY-272015 hydrochloride
|
5-HT Receptor
|
Cardiovascular Disease
|
|
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats.
|
-
- HY-111930
-
|
5-Iodo-indirubin-3'-monoxime
|
GSK-3
CDK
|
Cancer
|
|
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
|
-
- HY-118091
-
|
LY191704
|
5 alpha Reductase
|
Endocrinology
|
|
LY191704, as a benzoquinolinone, is a potent, nonsteroidal, noncompetitive and selective human type I 5α-reductase inhibitor. LY191704 is a racemic mixture of the compounds LY300502 and LY300503. LY191704 may be useful in the research of human endocrine disorders associated with overproduction of dihydrotestosterone (DHT) by 5α-reductase type 1.
|
-
- HY-B0975AS
-
|
Penicillin V-d5
|
Bacterial
Antibiotic
|
Infection
|
|
Penicillin V-d5 (Phenoxymethylpenicillin-d5) is the deuterium labeled Penicillin V. Penicillin V (Phenoxymethylpenicillin) is an orally active antibiotic. Penicillin V inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis[1][2][3][4].
|
-
- HY-146554
-
|
PDHK-IN-5
|
PDHK
|
Cancer
|
|
PDHK-IN-5 (Compound 19) is a potent inhibitor of PDHK with IC50s of 0.006 and 0.0329 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating agent targets for numerous diseases, including diabetes and cancers. PDHK-IN-5 has the potential for the research of cancer diseases.
|
-
- HY-142671
-
|
ATR-IN-5
|
ATM/ATR
|
Cancer
|
|
ATR-IN-5 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-5 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent CN112047938A, compound D24).
|
-
- HY-152979
-
-
- HY-A0060
-
|
Malotilate
NKK 105
|
Lipoxygenase
|
Cancer
|
|
Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) (IC50=4.7 μM). Malotilate prevents the development of hepatocytic injury in alcohol-pyrazole hepatitis by decreasing hepatic acetaldehyde levels and preventing the retention of transferrin in the hepatocytes.
|
-
- HY-139865
-
-
- HY-145345
-
-
- HY-A0006
-
-
- HY-142933
-
-
- HY-101934
-
-
- HY-12069
-
-
- HY-141859
-
|
PPO-IN-1
|
Others
|
Others
|
|
PPO-IN-1 is a potent protoporphyrinogen IX oxidase (PPO) inhibitor with a Ki value of 2.5 nM.
|
-
- HY-15683
-
-
- HY-13989
-
-
- HY-17367S3
-
-
- HY-D0145S
-
|
7-Ethoxyresorufin-d5
Resorufin ethyl ether-d5
|
Cytochrome P450
NO Synthase
|
Others
|
|
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
|
-
- HY-12071A
-
|
LDN193189 Tetrahydrochloride
|
TGF-β Receptor
|
Cancer
|
|
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
|
-
- HY-132233A
-
|
DDO-2093 dihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
DDO-2093 dihydrochloride is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 dihydrochloride selectively inhibits the catalytic activity of MLL complex.
|
-
- HY-148304
-
-
- HY-132233
-
|
DDO-2093
|
Histone Methyltransferase
|
Cancer
|
|
DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex.
|
-
- HY-146580
-
|
Cathepsin C-IN-3
|
Cathepsin
|
Inflammation/Immunology
|
|
Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC50 values of 101.5 and 86.5 nM, respectively.
|
-
- HY-148304A
-
-
- HY-100943
-
|
Cinanserin hydrochloride
SQ 10643
|
5-HT Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
|
-
- HY-146678
-
|
HDAC6-IN-5
|
HDAC
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity.
|
-
- HY-144181
-
|
MAT2A-IN-5
|
Others
|
Cancer
|
|
MAT2A-IN-5 is a potent inhibitor of MAT2A. The expression level of MAT2A is abnormally elevated in several types of tumors, including gastric, colon, liver and pancreatic cancers. MAT2A-IN-5 reduces the proliferative activity of MTAP-deficient cancer cells. MAT2A-IN-5 has the potential for the potential for the research of cancer diseases (extracted from patent WO2021254529A1, compound 1).
|
-
- HY-13635S
-
|
Finasteride-d9
MK-906-d9
|
5 alpha Reductase
|
Cancer
|
|
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
|
-
- HY-14664C
-
|
(3S,5R)-Fluvastatin sodium
(3S,5R)-XU 62-320
|
HMG-CoA Reductase (HMGCR)
|
Cancer
Cardiovascular Disease
|
|
(3S,5R)-Fluvastatin sodium ((3S,5R)-XU 62-320) is the (3S,5R)-enantiomer of Fluvastatin. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway.
|
-
- HY-102047B
-
|
KDOAM-25 citrate
|
Histone Demethylase
|
Cancer
|
|
KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
|
-
- HY-146339
-
|
HIV-1 inhibitor-27
|
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-27 (compound 5) is a potent HIV-1 inhibitor with IC50s of 16 μM, 0.5 μM and 0.39 μM for HIV-1 YU2, NL4-3 and 89.6 strain, respectively. HIV-1 inhibitor-27 has low cytotoxicity with a CC50 of 128 μM in TZM-bl cells. HIV-1 inhibitor-27 can be used for researching AIDS.
|
-
- HY-147358
-
|
Yimitasvir diphosphate
Emitasvir diphosphate; DAG-181 diphosphate
|
HCV
|
Infection
|
|
Yimitasvir (Emitasvir) diphosphate is an orally active hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor and can be used for research of chronic hepatitis C virus infection.
|
-
- HY-B0862S
-
|
Pendimethalin-d5
|
Isotope-Labeled Compounds
|
Others
|
|
Pendimethalin-d5 is the deuterium labeled Pendimethalin[1]. Pendimethalin is an herbicide that controls annual grasses and certain broadleaf weeds. Pendimethalin inhibits cell division and cell elongation[2].
|
-
- HY-Y0586
-
-
- HY-100747A
-
|
PSB-12379 disodium
|
CD73
|
Cancer
|
|
PSB-12379 disodium, a nucleotide analogue, is a potent Ecto-5'-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human).
|
-
- HY-141566
-
-
- HY-116808
-
-
- HY-125974
-
|
HM03
|
HSP
|
Cancer
|
|
HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity.
|
-
- HY-125974A
-
|
HM03 trihydrochloride
|
HSP
|
Cancer
|
|
HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity.
|
-
- HY-B1744S
-
-
- HY-N1200
-
-
- HY-18976
-
|
UF010
|
HDAC
|
Cancer
|
|
UF010 is a potent and selective HDAC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively.
|
-
- HY-P3383
-
|
Peceleganan
PL-5
|
Bacterial
|
Infection
|
|
Peceleganan (PL-5) is an artificial antimicrobial cecropin A (1-10) × melittin B (3-18) hybrid (10+16)-peptide analogue. Peceleganan inhibits wound infection.
|
-
- HY-111854
-
|
SNIPER(ABL)-015
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5 μM .
|
-
- HY-P3383A
-
|
Peceleganan acetate
PL-5 acetate
|
Bacterial
|
Infection
|
|
Peceleganan (PL-5) acetate is an artificial antimicrobial cecropin A (1-10) × melittin B (3-18) hybrid (10+16)-peptide analogue. Peceleganan acetate inhibits wound infection.
|
-
- HY-N0737
-
-
- HY-15463
-
|
Imatinib
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-108357
-
|
6-Diazo-5-oxo-L-nor-Leucine
L-6-Diazo-5-oxonorleucine; DON
|
Glutaminase
Bacterial
Influenza Virus
Antibiotic
|
Cancer
Infection
|
|
6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) is a glutamine antagonist that irreversibly inhibits the catabolic effect of glutamine. 6-Diazo-5-oxo-L-nor-Leucine shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 6-Diazo-5-oxo-L-nor-Leucine also possesses antibacterial and antiviral activity.
|
-
- HY-151153
-
|
HDAC1-IN-5
|
HDAC
Microtubule/Tubulin
Caspase
Apoptosis
|
Cancer
|
|
HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice.
|
-
- HY-143243
-
|
Antioxidant agent-5
|
Apoptosis
NF-κB
Keap1-Nrf2
Reactive Oxygen Species
|
Cardiovascular Disease
|
|
Antioxidant agent-5 (compound D-6) is a potent antioxidant agent. Antioxidant agent-5 can inhibit oxLDL (oxidized low-density lipoprotein)-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Antioxidant agent-5 suppresses oxLDL-induced increase of ROS level and nuclear translocation of NF-κB. Antioxidant agent-5 protects against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway.
|
-
- HY-10432A
-
|
A 83-01 sodium
|
TGF-β Receptor
|
Cancer
|
|
A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-113038B
-
|
α-Hydroxyglutaric acid
2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases.
|
-
- HY-151104
-
|
Neuraminidase-IN-11
|
Influenza Virus
|
Infection
|
Neuraminidase-IN-11 (15e) is a potent and selective neuraminidase (NA) inhibitor with the IC50 values of 4.7 nM, 8.46 nM and 1.5 nM against H1N1, H5N1 and H5N8 NAs respectively.
|
-
- HY-151485
-
|
Anti-infective agent 5
|
Parasite
|
Infection
|
|
Anti-infective agent 5 (compound 74) is an orally active inhibitor of Trypanosoma cruzi with an IC50 value of 0.10 μM. Anti-infective agent 5 effectively reduces parasite burden in vivo. Anti-infective agent 5 can be used for the research of infection.
|
-
- HY-139188
-
|
CC260
|
Others
|
Cancer
Metabolic Disease
|
|
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research.
|
-
- HY-14654
-
-
- HY-151446
-
|
ZIKV-IN-3
|
DNA Methyltransferase
Virus Protease
|
Infection
|
|
ZIKV-IN-3 (compound 5a), an andrographolide derivatives, is a potent ZIKV NS5 methyl transferase (MTase) inhibitor with an IC50 value of 18.34 μM. ZIKV-IN-3 inhibits ZIKV replication and infection. ZIKV-IN-3 can be used in research of Zika virus (ZIKV).
|
-
- HY-17390A
-
|
Loxapine succinate
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
|
|
Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages.
|
-
- HY-100348
-
|
EPI-001
|
Androgen Receptor
PPAR
Apoptosis
|
Cancer
|
|
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer.
|
-
- HY-B0006S2
-
|
Carvedilol-d5
BM 14190-d5
|
Adrenergic Receptor
Autophagy
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
|
-
- HY-112712
-
|
Cyclophilin inhibitor 1
|
HCV
|
Infection
|
|
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a.
|
-
- HY-111357
-
|
Antifungal agent 2
|
Fungal
|
Infection
|
|
Antifungal agent 2 is a broad-spectrum fungal inhibitor which inhibits growth of pertinent species of Candida, Cryptococcus, and Aspergillus at a concentration as low as 0.5 μg/mL.
|
-
- HY-W018931
-
-
- HY-10129
-
|
Veliparib
ABT-888
|
PARP
Autophagy
|
Cancer
|
|
Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
|
-
- HY-13067
-
-
- HY-133246
-
-
- HY-151483
-
|
TK-129
|
Histone Demethylase
|
Cardiovascular Disease
|
|
TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease.
|
-
- HY-115412
-
|
Vorinostat-d5
SAHA-d5; Suberoylanilide hydroxamic acid-d5
|
HDAC
Autophagy
Mitophagy
Filovirus
Apoptosis
HPV
|
Cancer
Infection
|
|
Vorinostat-d5 (SAHA-d5) is the deuterium labeled Vorinostat. 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-110208
-
|
BRD9876
|
Kinesin
Microtubule/Tubulin
|
Cancer
|
|
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research.
|
-
- HY-16716
-
|
Basmisanil
RG1662; RO5186582
|
GABA Receptor
|
Neurological Disease
|
|
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders.
|
-
- HY-B1452
-
|
Licofelone
ML-3000
|
COX
Lipoxygenase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
|
-
- HY-135881
-
|
OMDM-5
|
TRP Channel
Endogenous Metabolite
|
Neurological Disease
|
|
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM).
|
-
- HY-154450
-
-
- HY-147698
-
|
ZLHQ-5f
|
CDK
Topoisomerase
Apoptosis
|
Cancer
|
|
ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.
|
-
- HY-47573
-
-
- HY-112732B
-
|
Sparfosic acid trisodium
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Sparfosic acid trisodium is a DNA antimetabolite agent and a potent inhibitor of aspartate transcarbamoyl transferase. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis. Sparfosic acid trisodium synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines.
|
-
- HY-12304
-
|
IOX1
|
Histone Demethylase
|
Cancer
|
|
IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.
|
-
- HY-W510159
-
-
- HY-Y0079S
-
|
D-Phenylalanine-d5
|
Endogenous Metabolite
|
Others
|
|
D-Phenylalanine-d5 is the deuterium labeled D-Phenylalanine. D-Phenylalanine is the synthetic dextro isomer of phenylalanine. D-Phenylalanine inhibits biofilm development of Pseudoalteromonas sp. SC2014[1].
|
-
- HY-116934
-
|
5-Pentadecylresorcinol
Adipostatin A
|
Others
|
Cancer
Infection
|
|
5-Pentadecylresorcinol (Adipostatin A) is a glycerol-3-phosphate dehydrogenase (GPDH) inhibitor with an IC50 of 4.1 µM. Adipostatin A shows good larvicidal activity against Aedes aegypti.
|
-
- HY-W400159
-
-
- HY-152694
-
|
5-Vinylcytidine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
5-Vinylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities.
|
-
- HY-122593
-
|
PI3Kδ-IN-5
|
PI3K
|
Cancer
|
|
PI3Kδ-IN-5 (compound 7n) is a highly potent and selective inhibitor of PI3Kδ with an IC50 of 0.9 nM.
|
-
- HY-N4289
-
|
3-Epiursolic Acid
|
Cathepsin
|
Cancer
|
|
3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B.
|
-
- HY-146318
-
-
- HY-B0196S
-
-
- HY-13613
-
|
Dutasteride
GG 745; GI 198745
|
5 alpha Reductase
Apoptosis
|
Cancer
|
|
Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
|
-
- HY-152658
-
|
5-Phenylcytidine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
5-Phenylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities.
|
-
- HY-W555551
-
-
- HY-145023
-
|
RET-IN-5
|
RET
|
Cancer
|
|
RET-IN-5 is a potent RET (rearranged during transfection) inhibitor with an IC50s of 0.4 nM and 135.1 nM for RET and VEGFR2, respectively (WO2021213476A1, compound 18).
|
-
- HY-B0196AS1
-
|
Venlafaxine-d6 hydrochloride
Wy 45030-d6 (hydrochloride)
|
Serotonin Transporter
|
Neurological Disease
|
|
Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].
|
-
- HY-134622
-
|
GSK-3/CDK5/CDK2-IN-1
|
CDK
GSK-3
|
Cancer
Neurological Disease
|
|
GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases.
|
-
- HY-N0693
-
-
- HY-100285
-
|
RD3-0028
|
RSV
|
Infection
|
|
RD3-0028 is a potent and selective inhibitor of RSV replication with an EC50 of 4.5 μM.
|
-
- HY-119885A
-
-
- HY-17605
-
-
- HY-N8726
-
-
- HY-16902
-
-
- HY-100519
-
|
NVS-PAK1-1
|
PAK
|
Cancer
|
|
NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
|
-
- HY-14846A
-
|
Litronesib Racemate
LY2523355 Racemate
|
Kinesin
|
Others
|
|
Litronesib Racemate (LY2523355 Racemate) is the racemate of litronesib. Litronesib is a selective, allosteric inhibitor of kinesin Eg5.
|
-
- HY-101071A
-
|
Monastrol
(±)-Monastrol
|
Kinesin
Apoptosis
|
Cancer
|
|
Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
|
-
- HY-10818
-
|
LY309887
|
Antifolate
|
Cancer
|
|
LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
|
-
- HY-15333
-
-
- HY-19966
-
-
- HY-148430
-
-
- HY-N0401A
-
|
(Z)-Ligustilide
|
Bacterial
|
Infection
Metabolic Disease
|
|
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6.
(Z)-Ligustilide inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) .
|
-
- HY-127026S
-
|
Quinaprilat-d5
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Quinaprilat-d5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance[1].
|
-
- HY-145843
-
|
c-Myc inhibitor 5
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 5 (DA3) is a fluorescent, long chain-bridged bispurine that selectively targets the c-MYC G-quadruplex (KD of 16 μM). c-Myc inhibitor 5 shows inhibition on c-MYC expression rather than other G4-driven oncogenes.
|
-
- HY-17447SA
-
|
Tranylcypromine-d5 hydrochloride
SKF 385-d5 (hydrochloride)
|
Monoamine Oxidase
Histone Demethylase
|
Neurological Disease
|
|
Tranylcypromine-d5 (hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis[1][2].
|
-
- HY-131064
-
|
RIPK3-IN-1
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM.
|
-
- HY-107613A
-
|
R 59-022 hydrochloride
DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride
|
PKC
5-HT Receptor
|
Cancer
Infection
Inflammation/Immunology
|
|
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
|
-
- HY-W062835
-
|
CGP77675
|
Src
|
Cancer
|
|
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity.
|
-
- HY-107613
-
|
R 59-022
DKGI-I; Diacylglycerol kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
|
R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
|
-
- HY-75800
-
|
Lomibuvir
VX-222
|
DNA/RNA Synthesis
HCV
|
Infection
|
|
Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis.
|
-
- HY-66005S4
-
|
Acetaminophen-13C2,15N
Paracetamol-13C2,15N; 4-Acetamidophenol-13C2,15N; 4'-Hydroxyacetanilide-13C2,15N
|
COX
Bacterial
Histone Acetyltransferase
Parasite
Endogenous Metabolite
|
|
|
Acetaminophen- 13C2, 15N is the 13C and 15N labeled Acetaminophen[1]. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent[2][3][4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[5].
|
-
- HY-117427
-
|
D5D-IN-326
|
Others
|
Metabolic Disease
|
|
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice.
|
-
- HY-151535
-
|
SARS-CoV-2 3CLpro-IN-5
|
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-2 3CLpro-IN-5 has inhibitory activity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19).
|
-
- HY-103149
-
|
SB-216641A
SB-216641 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A inhibits the function of SKF-99101H.
|
-
- HY-106100A
-
|
Roxindole hydrochloride
EMD 38362
|
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities.
|
-
- HY-32329
-
|
Setiptiline
Org-8282
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-151901
-
|
SARS-CoV-2 Mpro-IN-5
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 Mpro-IN-5 is a dual Inhibitor of Main Protease (M Pro) and Cathepsin L (CatL), with IC50s of 1800 nM and 145 nM respectively. SARS-CoV-2 Mpro-IN-5 has antiviral activity against SARS-CoV2. SARS-CoV-2 Mpro-IN-5 blocks SARS-CoV2 replication in hACE2 expressing A549 cells with IC50 value of 14.7 nM.
|
-
- HY-117025A
-
|
Manzamine A hydrochloride
Keramamine A hydrochloride
|
GSK-3
CDK
Parasite
Proton Pump
HSV
Autophagy
|
Cancer
Infection
Neurological Disease
|
|
Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1.
|
-
- HY-117025
-
|
Manzamine A
Keramamine A
|
GSK-3
CDK
Parasite
Proton Pump
HSV
Autophagy
|
Cancer
Infection
Neurological Disease
|
|
Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1.
|
-
- HY-115885
-
|
XP5
|
HDAC
|
Cancer
Inflammation/Immunology
|
|
XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma.
|
-
- HY-10580
-
|
GSK 3 Inhibitor IX
6-Bromoindirubin-3'-oxime; BIO; MLS 2052
|
GSK-3
CDK
Apoptosis
|
Cancer
|
|
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
|
-
- HY-17624
-
|
Framycetin
Neomycin B; Fradiomycin B
|
Bacterial
Antibiotic
|
Infection
|
|
Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
|
-
- HY-128579
-
|
DW14800
|
Histone Methyltransferase
|
Cancer
|
|
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
|
-
- HY-151103
-
|
Neuraminidase-IN-10
|
Influenza Virus
|
Infection
|
|
Neuraminidase-IN-10 is a potent neuraminidase (NA) inhibitor with anti-influenza activity. Neuraminidase-IN-10 is against H1N1, H5N1, and H5N8 with IC50 values of 2.6 nM, 5.1 nM, and 1.65 nM, respectively.
|
-
- HY-16767
-
|
Doravirine
MK-1439
|
HIV
Reverse Transcriptase
|
Infection
|
|
Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.
|
-
- HY-113038A
-
|
α-Hydroxyglutaric acid disodium
2-Hydroxyglutarate disodium; 2-Hydroxyglutaric acid disodium; 2-Hydroxypentanedioic acid disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases.
|
-
- HY-111419A
-
-
- HY-111419
-
-
- HY-15769A
-
-
- HY-70035
-
|
Otamixaban
FXV673
|
Factor Xa
|
Cardiovascular Disease
|
|
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
|
-
- HY-114168
-
-
- HY-15769
-
|
WHI-P180
Janex 3
|
RET
VEGFR
EGFR
|
Cancer
|
|
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
|
-
- HY-139880
-
-
- HY-U00439A
-
-
- HY-150731
-
-
- HY-10165
-
|
PSI-6130
R 1656
|
HCV
|
Infection
|
|
PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM.
|
-
- HY-120494
-
-
- HY-145359
-
|
eIF4A3-IN-5
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-5 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), such as eIF4AI and eIF4AII. eIF4A3-IN-5 has the potential for the research of eIF4A dependent diseases, including the research of cancer (extracted from patent US20170145026A1).
|
-
- HY-B0174A
-
|
Olsalazine
|
Leukotriene Receptor
Antibiotic
|
Inflammation/Immunology
|
|
Olsalazine is a potent inhibitor of macrophages chemotaxis to LTB4 with an IC50 value of 0.39 mM, also reduces the synthesis of 5-hydroxyeicosatetraenoic acid (5-HETE), 11-HETE, 12-HETE, and 15-HETE in polymorphonuclear leukocyte (PMNL) and mononuclear cells (MNL). Olsalazine can be used for researching ulcerative colitis. Anti-inflammatory activity.
|
-
- HY-150626
-
|
SARS-CoV-2 nsp13-IN-5
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 nsp13-IN-5 (compound C6) is a potent SARS-CoV-2 nsp13 inhibitor with IC50 values of 50 and 55 μM for ssDNA + ATPase and ssDNA - ATPase. SARS-CoV-2 nsp13-IN-5 can be used for researching anti-COVID-19.
|
-
- HY-P3502
-
|
Zilucoplan
RA101495
|
Complement System
|
Inflammation/Immunology
|
|
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM).
|
-
- HY-B0141AS
-
-
- HY-B0132S
-
|
Norfloxacin-d5
|
Bacterial
Antibiotic
|
Infection
|
|
Norfloxacin-d5 is the deuterium labeled Norfloxacin. Norfloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase[1][2].
|
-
- HY-14829F
-
|
L-Afegostat
5-epi-Isofagomine
|
Glucosidase
|
Metabolic Disease
|
|
L-Afegostat (5-epi-Isofagomine) is a glycosidase inhibitor. L-Afegostat is an iminosugar that can be used for the synthesis of carbohydrates. L-Afegostat shows enzyme inhibition to β-Glucosidase with an Ki of 30 μM.
|
-
- HY-N3270
-
|
Methyl orsellinate
|
Fungal
Lipoxygenase
|
Infection
|
|
Methyl orsellinate is a phytotoxic compound with antifungal activities. Methyl orsellinate is a 5-lipoxygenase inhibitor with an IC50 value of 59.6 μM. Methyl orsellinate can be used for fungal infection research.
|
-
- HY-B0196S1
-
-
- HY-112468
-
|
PNU112455A hydrochloride
|
CDK
|
Cancer
|
|
PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
|
-
- HY-135407S
-
-
- HY-139611B
-
-
- HY-18770
-
-
- HY-B0196AS
-
-
- HY-13997
-
|
Ombitasvir
ABT-267
|
HCV
|
Infection
|
|
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
|
-
- HY-15789
-
|
Elbasvir
MK-8742
|
HCV
|
Infection
|
|
Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.
|
-
- HY-109592S
-
-
- HY-W031727S1
-
-
- HY-100933
-
-
- HY-13521
-
|
SB-505124
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-P3930
-
|
PKI (5-24),amide
IP20-amide
|
PKA
|
Neurological Disease
|
|
PKI (5-24),amide (IP20-amide) is a 20-residue peptide that corresponds to the active portion of the heat-stable inhibitor protein of cAMP-dependent protein kinase. PKI (5-24),amide is a potent cAMP-dependent protein kinase (PKA) (PKA) inhibitor with a Ki of 2.3 nM.
|
-
- HY-10864
-
|
URB-597
KDS-4103
|
FAAH
Autophagy
Mitophagy
|
Neurological Disease
|
|
URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity.
|
-
- HY-B0589S1
-
-
- HY-139065
-
|
AMPC
|
Others
|
Cancer
|
|
AMPC is a potent and effective TFF3 inhibitor. AMPC inhibits cell proliferation, survival, oncogenicity, and CSC-like behaviour in TFF3-positive CMS4 CRC cells. AMPC acts as a potential anti-cancer agent alone or in combination with 5-FU, and can be used for cancer research.
|
-
- HY-13521A
-
|
SB-505124 hydrochloride
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-129079A
-
|
TFMB-(S)-2-HG
|
DNA Methyltransferase
|
Cancer
|
|
TFMB-(S)-2-HG is a potent inhibitor of the 5'-methylcytosine hydroxylase TET2. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML).
|
-
- HY-15945
-
|
DBeQ
JRF 12
|
p97
Autophagy
Apoptosis
|
Cancer
|
|
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
|
-
- HY-145858
-
|
Chalcones A-N-5
|
Ferroptosis
|
Cancer
|
|
Chalcones A-N-5 is a trihydroxy chalcone derivative compound. Chalcones A-N-5 doesn’t show cytotoxicity at the concentration lower than 100 µM (with IC50 > 1 mM), but has a significant effect on promoting cell proliferation. Chalcones A-N-5 potentially promotes neuronal cell growth in the damaged brain tissue. Chalcones A-N-5 also inhibits ferroptosis induced by RSL or erastin and reduces the lipid peroxidation levels induced by Aβ1-42 protein aggregation. Chalcones A-N-5 is a promising molecular skeleton candidate for further development of lead compound for in vivo test to research AD.
|
-
- HY-128679
-
|
TBK1/IKKε-IN-5
|
IKK
|
Cancer
|
|
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity.
|
-
- HY-17459
-
|
Clopidogrel hydrogen sulfate
(S)-(+)-Clopidogrel bisulfate; (S)-(+)-Clopidogrel hydrogen sulfate
|
Cytochrome P450
P2Y Receptor
|
Cardiovascular Disease
Cancer
|
|
Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor.
|
-
- HY-131275
-
|
Imatinib Impurity E
|
Drug Metabolite
|
Others
|
|
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-122203
-
|
PCS1055 dihydrochloride
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively.
|
-
- HY-100975
-
-
- HY-N0196
-
-
- HY-14846
-
|
Litronesib
LY2523355
|
Kinesin
|
Cancer
|
|
Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.
|
-
- HY-10992
-
-
- HY-10997A
-
|
Ibrutinib Racemate
PCI-32765 Racemate
|
Btk
|
Cancer
|
|
Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
|
-
- HY-145000
-
-
- HY-128561
-
-
- HY-10993
-
|
Adavosertib
AZD1775; MK-1775
|
Wee1
|
Cancer
|
|
Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.
|
-
- HY-10550A
-
-
- HY-102035
-
-
- HY-112463
-
-
- HY-145651
-
-
- HY-16691
-
-
- HY-16937
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- HY-12082A
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- HY-10992A
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- HY-145050
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HBV-IN-7
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HBV
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Infection
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HBV-IN-7 is a potent HBV inhibitor with an EC50 of 7 nM (WO2021213445A1, compound 5).
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- HY-N1201
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- HY-19994
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ML264
|
KLF
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Cancer
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ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
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- HY-101465
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- HY-135385
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- HY-121291
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Aureothin
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HIV
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Infection
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Aureothin, is a natural polyketide, is a HIV inhibitor with an IC50 of 5.3 nM. Aureothin is a microbial biolarvicide.
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- HY-101774
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- HY-10997
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- HY-B0165A
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- HY-12302
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Kenpaullone
9-Bromopaullone; NSC-664704
|
CDK
GSK-3
|
Cancer
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Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
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- HY-105349
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T-0156
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Phosphodiesterase (PDE)
|
Neurological Disease
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T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway.
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- HY-14654A
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- HY-108938
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