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Results for "

Alpha Inhibitors

" in MCE Product Catalog:

1227

Inhibitors & Agonists

2

Screening Libraries

1

Fluorescent Dye

3

Biochemical Assay Reagents

42

Peptides

15

Inhibitory Antibodies

201

Natural
Products

67

Isotope-Labeled Compounds

Targets Recommended:
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-152191
    ChoKα inhibitor-3

    		Apoptosis Cancer
    ChoKα inhibitor-3 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-3 can inhibit HChoK α1 with an IC50 value of 0.66 μM. ChoKα inhibitor-3 also can induce apoptosis. ChoKα inhibitor-3 can be used for the research of cancer.
  • HY-144178
    HIF-2α-IN-6

    		HIF/HIF Prolyl-Hydroxylase Others
    HIF-2α-IN-6 (117) is a HIF-2α inhibitor.
  • HY-147644
    α-Synuclein inhibitor 3

    		Others Neurological Disease
    α-Synuclein inhibitor 3 (Compound 7g) is a α-synuclein (α -Syn) aggregation inhibitor. α-Synuclein inhibitor 3 can be used for Parkinson’s disease research.
  • HY-119593
    α-Homonojirimycin

    Homonojirimycin

    		 Glucosidase Metabolic Disease
    α-Homonojirimycin is a potent α-glucosidase inhibitor.
  • HY-113960
    ERRα antagonist-1

    		Estrogen Receptor/ERR Cancer
    ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
  • HY-152552
    α-Synuclein inhibitor 8

    		α-synuclein Neurological Disease
    α-Synuclein inhibitor 8 is an active inhibitor of α-Synuclein with an IC50 value of 2.5 µM. α-Synuclein inhibitor 8 has highly inhibition on the aggregation and disaggregation of α-Synuclein fibers. α-Synuclein inhibitor 8 reduces the formation of inclusions in neurons that can repairs damage neurons and improves Parkinson’s disease (PD)-like symptoms. α-Synuclein inhibitor 8 has high antioxidant activity and low cytotoxicity.
  • HY-113038
    D-α-Hydroxyglutaric acid

    (R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid

    		 Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-19949
    HIF-2α-IN-1

    		HIF/HIF Prolyl-Hydroxylase Metabolic Disease
    HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay.
  • HY-129434A
    4aα,7α,7aα-Nepetalactone

    		Bacterial Infection
    4aα,7α,7aα-Nepetalactone exhibits antibacterial activity, and inhibits Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterococcus faecalis.
  • HY-101491
    SR-18292

    		PGC-1α Autophagy Metabolic Disease
    SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
  • HY-151341
    HIF-1/2α-IN-1

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) .
  • HY-15438
    SB 415286

    		GSK-3 Apoptosis Metabolic Disease
    SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
  • HY-148863
    Cavα2δ1&NET-IN-2

    		Calcium Channel Monoamine Transporter Inflammation/Immunology
    Cavα2δ1&NET-IN-2 (Compound 45CS) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-2 inhibits Cavα2δ-1 with a Ki of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a Ki of 59 nM and IC50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain.
  • HY-148862
    Cavα2δ1&NET-IN-1

    		Calcium Channel Monoamine Transporter Inflammation/Immunology
    Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain.
  • HY-111507
    PDGFRα kinase inhibitor 1

    		PDGFR Cancer
    PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
  • HY-110266
    GN44028

    		HIF/HIF Prolyl-Hydroxylase Cancer
    GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.
  • HY-14571
    E7820

    ER68203-00

    		 Molecular Glues Integrin Cancer
    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
  • HY-136735
    IRE1α kinase-IN-1

    		IRE1 Cancer Neurological Disease
    IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM).
  • HY-114423
    p38α inhibitor 1

    		p38 MAPK Autophagy Inflammation/Immunology
    p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
  • HY-70073
    Zaurategrast

    CT7758

    		 Integrin Inflammation/Immunology
    Zaurategrast (CT7758) is a potent and oral-effective α4-integrin inhibitor.
  • HY-148264
    HIF-2α-IN-7

    		HIF/HIF Prolyl-Hydroxylase Cancer Infection Metabolic Disease Inflammation/Immunology
    HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC50 value of 6 nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders.
  • HY-18509
    IRE1α kinase-IN-2

    		IRE1 Cancer
    IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines.
  • HY-13671
    LW6

    HIF-1α inhibitor; LW8

    		 HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
  • HY-145419
    IRE1α kinase-IN-4

    		IRE1 Others
    IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α.
  • 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-145418
    IRE1α kinase-IN-3

    		IRE1 Others
    IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α.
  • HY-100542
    D-α-Hydroxyglutaric acid disodium

    Disodium (R)-2-hydroxyglutarate

    		 Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite Cancer Inflammation/Immunology Neurological Disease
    D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling.
  • HY-111387
    IDF-11774

    		HIF/HIF Prolyl-Hydroxylase Cancer
    IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.
  • HY-144176
    HIF-2α-IN-5

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of < 50 nM.
  • HY-152193
    ChoKα inhibitor-4

    		Others Cancer
    ChoKα inhibitor-4 is a bioisosteric inhibitor of HChoK α1 (IC50=0.66 μM), with inhibitory and antiproliferative effect on cancer cells. ChoKα inhibitor-4 induces apoptosis via mitochondrial pathway, and reduces anti-apoptotic proteins expression.
  • HY-142618
    TNF-α-IN-6

    		TNF Receptor Inflammation/Immunology
    TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα (KD = 6.8 nM).
  • HY-18874
    p38-α MAPK-IN-1

    		p38 MAPK Autophagy Others
    p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
  • HY-146225
    α-Amylase/α-Glucosidase-IN-2

    		Glucosidase Metabolic Disease
    α-Amylase/α-Glucosidase-IN-2 (compound 5) is a potent α-amylase and α-glucosidase dual inhibitor with IC50 values of 13.02, 13.09 µM for α-amylase and α-glucosidase, respectively. α-Amylase/α-Glucosidase-IN-2 has the potential for the research of diabetic complications.
  • HY-147711
    α-Amylase/α-Glucosidase-IN-1

    		Glucosidase Metabolic Disease
    α-Amylase/α-Glucosidase-IN-1 (compound 33) is a potent α-amylase/α-glucosidase inhibitor with IC50s of 2.01, 2.09 µM for α-amylase and α-glucosidase, respectively. Kinetic studies predict that α-Amylase/α-Glucosidase-IN-1 has the potential of anti hyperglycemia.
  • HY-153002
    p38α inhibitor 3

    		p38 MAPK Inflammation/Immunology
    p38α inhibitor 3 (Comp G7) is a p38α inhibitor that blocks the effectiveness of myoblast differentiation.
  • HY-14929A
    Migalastat hydrochloride

    GR181413A

    		 Others Others
    Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
  • HY-U00459
    GSK2850163

    		IRE1 Cancer
    GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
  • HY-U00459B
    GSK2850163 hydrochloride

    		IRE1 Cancer
    GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
  • HY-B0141AS
    Alpha-Estradiol-d3

    Alfatradiol-d3; Epiestradiol-d3; Epiestrol-d3

    		 Endogenous Metabolite 5 alpha Reductase Inflammation/Immunology
    Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
  • HY-112535
    α-2,3-sialyltransferase-IN-1

    Lith-O-Asp analog

    		 Others Cancer Inflammation/Immunology
    α-2,3-sialyltransferase-IN-1 (Lith-O-Asp analog) is a noncompetitive α-2,3-sialyltransferase inhibitor with an IC50 of 6 μM.
  • HY-18371
    TC-S 7009

    		HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
  • HY-18370
    HIF-2α-IN-3

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent.
  • HY-100735
    C 87

    		TNF Receptor Inflammation/Immunology
    C 87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
  • HY-125840
    Belzutifan

    PT2977; MK-6482

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC).
  • HY-12836
    IFN alpha-IFNAR-IN-1

    		IFNAR Inflammation/Immunology
    IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).
  • HY-147668
    α-Synuclein inhibitor 6

    		Others Neurological Disease
    α-Synuclein inhibitor 6 (compound 3ge) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.70 μM and inhibition ratio at 30 μM of 94.4%.
  • HY-147666
    α-Synuclein inhibitor 4

    		Others Neurological Disease
    α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2%.
  • HY-147669
    α-Synuclein inhibitor 7

    		Others Neurological Disease
    α-Synuclein inhibitor 7 (compound 3gf) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.95 μM and inhibition ratio at 30 μM of 85.8%.
  • HY-147667
    α-Synuclein inhibitor 5

    		Others Neurological Disease
    α-Synuclein inhibitor 5 (compound 4aa) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.22 μM and inhibition ratio at 30 μM of 94.3%.
  • 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-15672
    FM19G11

    		HIF/HIF Prolyl-Hydroxylase Cancer Neurological Disease
    FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.
  • HY-N3002
    α-Arbutin

    4-Hydroxyphenyl α-D-glucopyranoside

    		 Tyrosinase Metabolic Disease
    α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.
  • HY-B0141AS1
    Alpha-Estradiol-d2

    Alfatradiol-d2; Epiestradiol-d2; Epiestrol-d2

    		 5 alpha Reductase Endogenous Metabolite Metabolic Disease Cardiovascular Disease
    Alpha-Estradiol-d2 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia[1].
  • HY-107532
    N-Nonyldeoxynojirimycin

    NN-DNJ; Nonyl-DNJ

    		 Glucosidase Metabolic Disease
    N-Nonyldeoxynojirimycin (NN-DNJ) is a potent inhibitor of alpha-glucosidase and alpha-1,6-glucosidase (IC50s, 0.42, 8.4 μM, respectively), inhibits glycogen breakdown.
  • HY-W019838
    D-Erythro-dihydrosphingosine

    		Endogenous Metabolite Phospholipase Cancer
    D-Erythro-dihydrosphingosin directly inhibits cytosolic phospholipase A2α (cPLA2α) activity.
  • HY-152473
    Topoisomerase IIα-IN-6

    		Topoisomerase Cancer
    Topoisomerase IIα-IN-6 (Compound 47d) is an inhibitor of DNA topoisomerase IIα/β. Topoisomerase IIα-IN-6 inhibits human topoisomerase IIα and human topoisomerase IIβ with IC50 values of 0.67 µM and 0.55 µM, respectively. Topoisomerase IIα-IN-6 has stable metabolism.
  • HY-142659
    IRE1α kinase-IN-6

    		IRE1 Cancer
    IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.
  • HY-U00376
    5α-reductase-IN-1

    		5 alpha Reductase Metabolic Disease
    5α-reductase-IN-1 is an inhibitor of 5α-reductase, used for the research of patterned alopecia in combination with minoxidil.
  • HY-123076
    Pifithrin-α, p-Nitro, Cyclic

    PFN-α

    		 MDM-2/p53 Neurological Disease
    Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
  • HY-148860
    HIF-2α-IN-8

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity.
  • HY-P3976
    Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine

    		Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is a blood pressure lowering peptide containing 4 amino acids. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is an angiotensin-converting Enzyme (ACE) inhibitor. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine can be used in research of high blood pressure.
  • HY-151344
    HIF-1/2α-IN-2

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2).
  • HY-136748
    HIF-2α-IN-4

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.
  • HY-146032
    p38-α MAPK-IN-4

    		p38 MAPK Inflammation/Immunology Neurological Disease
    p38-α MAPK-IN-4 (Compound 69) is a selective p38α MAPK inhibitor with an IC50 of 1.5 µM. p38-α MAPK-IN-4 rapidly and strongly prevents the development of mechanical allodynia (MA) in vivo.
  • HY-146268
    CaMKIIα-IN-1

    		CaMK Neurological Disease
    CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability.
  • HY-N0242
    Fraxinellone

    		PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Cancer Inflammation/Immunology
    Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1.
  • HY-145580
    Minzasolmin

    		α-synuclein Neurological Disease
    Minzasolmin is an alpha-synuclein oligomerization inhibitor.
  • HY-N8120
    Bisabolone oxide A

    		Glucosidase Metabolic Disease
    Bisabolone oxide A is an α-glucosidase inhibitor.
  • HY-146752
    α-Amylase-IN-1

    		Others Others
    α-Amylase-IN-1 is a potent α-amylase inhibitor with an IC50 of 4.46 μM.
  • HY-P99148
    Anti-Mouse TNF alpha Antibody

    		TNF Receptor Inflammation/Immunology
    Anti-Mouse TNF alpha Antibody is an anti-mouse TNF alpha IgG antibody inhibitor derived from host Rat.
  • HY-B0141A
    Alpha-Estradiol

    Alfatradiol; Epiestradiol; Epiestrol

    		 5 alpha Reductase Endogenous Metabolite Bacterial Inflammation/Immunology
    Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
  • HY-146424
    OBHS

    		Estrogen Receptor/ERR Cancer Neurological Disease
    OBHS is an estrogen receptor α (ERα) inhibitor. OBHS can also be used as a blowing agent.
  • HY-134471
    TNF-α-IN-2

    		TNF Receptor Inflammation/Immunology
    TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.
  • HY-14929
    Migalastat

    GR181413A free base

    		 Others Others
    Migalastat (GR181413A free base) is an orally active and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
  • HY-115978
    α-Glucosidase-IN-2

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-2 (compound 5d) is a potent α-Glucosidase inhibitor with an IC50 of 9.48 µM. α-Glucosidase-IN-2 is an antidiabetic agent.
  • HY-113212
    Ursocholic acid

    		Endogenous Metabolite Metabolic Disease
    Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.
  • HY-147813
    HIF-1α-IN-3

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-3 (Compound (S)-3f) is a hypoxia-selective HIF-1α inhibitor. HIF-1α-IN-3 shows strong antiestrogenic potency.
  • HY-17537
    APY29

    		IRE1 Cancer
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
  • HY-107371
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde

    NSC95682

    		 IRE1 Cancer
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5.
  • HY-146156
    α-Glucosidase-IN-7

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-7 is a noncompetitive α-glucosidase inhibitor with an IC50 value of 18.9 µM.
  • HY-12710
    Rauwolscine

    α-Yohimbine; Corynanthidine; Isoyohimbine

    		 Adrenergic Receptor Cancer
    Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis.
  • HY-B0194A
    Tizanidine hydrochloride

    		Adrenergic Receptor Cancer Neurological Disease Endocrinology
    Tizanidine hydrochloride is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-145940
    BAY-204

    BRD3727

    		 Others Cancer
    BAY-204 is an inhibitor of Casein kinase 1 alpha and delta (CSNK1α and δ) useful for the treatment of proliferative disorders.
  • HY-150960
    α-Glucosidase-IN-13

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-13 (Compound 8) is a α-glucosidase inhibitor with an IC50 of 5.69 μM.
  • HY-B0194
    Tizanidine

    		Adrenergic Receptor Neurological Disease Endocrinology Cancer
    Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-P99782
    Opinercept

    		TNF Receptor Inflammation/Immunology
    Opinercept is a tumor necrosis factor-alpha (TNF-alpha) inhibitor. Opinercept can be used for the research of rheumatoid arthritis (RA).
  • HY-12867
    PT-2385

    		HIF/HIF Prolyl-Hydroxylase Cancer
    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.
  • HY-112910
    Grp94 Inhibitor-1

    		HSP Cancer Inflammation/Immunology
    Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
  • HY-N1064
    Xanthoplanine

    		nAChR Neurological Disease
    Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
  • HY-153017
    HIF-1 inhibitor-4

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level.
  • 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-147823
    α-Glucosidase-IN-6

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-6 (compound 18) is a competitive α-glucosidase inhibitor with an IC50 of 5.69 µM. α-Glucosidase-IN-6 has anti-diabetic potential.
  • HY-113038AS
    α-Hydroxyglutaric acid-13C5 sodium

    2-Hydroxyglutarate-13C5 sodium; 2-Hydroxyglutaric acid-13C5 sodium; 2-Hydroxypentanedioic acid-13C5 sodium

    		 Histone Demethylase Endogenous Metabolite Cancer
    α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
  • HY-120675
    SSTC3

    		Casein Kinase Wnt Cancer
    SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
  • HY-112275
    TNF-α-IN-1

    		TNF Receptor Cancer Inflammation/Immunology
    TNF-α-IN-1 is a TNF-α inhibitor extracted from patent US20030096841A1, compound example I-7.
  • HY-150959
    α-Glucosidase-IN-12

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-12 (compound 14) is a potent α-glucosidase inhibitor, with an IC50 of 10.20 μM.
  • HY-150961
    α-Glucosidase-IN-14

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-14 (compound 5) is a potent α-glucosidase inhibitor, with an IC50 of 5.22 μM.
  • HY-B0942
    Benzethonium chloride

    		nAChR Bacterial Neurological Disease
    Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
  • HY-P99153
    Farletuzumab

    MORAb-003

    		 Antibiotic Cancer
    Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a therapeutic humanized monoclonal antibody with high affinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer.
  • HY-P3653
    α-Conotoxin M I

    		mAChR nAChR Neurological Disease
    α-Conotoxin M I is a potent and selective inhibitor of mAChR and α1β1γδ nAChR, but has no effect on nicotine-stimulated dopamine release. α-Conotoxins are small, disulfide-rich peptides that competitively inhibit muscle and neuronal nicotinic AChRs.
  • HY-150560
    α-Glucosidase-IN-11

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels.
  • HY-147718
    α-Glucosidase-IN-5

    		Glutaminase Metabolic Disease
    α-Glucosidase-IN-5 (compound 8) is a potent α-glucosidase inhibitor with an IC50 of 57.9 µM. α-Glucosidase-IN-5 has the potential for the research of diabetes mellitus.
  • HY-151142
    α-Glucosidase-IN-18

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-18 (7B) is an orally active α-glucosidase inhibitor with an IC50 value of 3.96 μM. α-Glucosidase-IN-18 has antidiabetic activity.
  • 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-147100
    α1A-AR Degrader 9c

    		PROTACs Adrenergic Receptor Cancer
    α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research.
  • HY-115903
    HIF-1α-IN-2

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.
  • HY-113038AS1
    α-Hydroxyglutaric acid-d4 disodium

    2-Hydroxyglutarate-d4 disodium; 2-Hydroxyglutaric acid-d4 disodium; 2-Hydroxypentanedioic acid-d4 disodium

    		 Histone Demethylase Endogenous Metabolite Cancer
    α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. 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[2].
  • HY-149000
    PI3Kα-IN-7

    		PI3K Apoptosis Cancer
    PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor. PI3Kα-IN-7 also inhibits PI3Kβ. PI3Kα-IN-7 decreases cancer cells mitochondrial membrane potential and induces apoptosis.
  • HY-118694
    TAPI-0

    		TNF Receptor MMP Bacterial Cancer Infection
    TAPI-0 is a TACE (TNF-α converting enzyme; ADAM17) inhibitor with an IC50 of 100 nM. TAPI-0 is a MMP inhibitor and also attenuates TNF-α processing.
  • HY-N10564
    8α,9α-Epoxycoleon-U-quinone

    		P-glycoprotein Cancer
    8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX.
  • HY-19763
    BEBT-908

    PI3Kα inhibitor 1

    		 PI3K Cancer
    BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
  • HY-N4155
    2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid

    		HIV Protease HSV Cancer Infection
    2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitory activity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells.
  • HY-115746
    Dimethyl-bisphenol A

    DMBPA

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    Dimethyl-bisphenol A (DMBPA) is a potent HIF-1α inhibitor. Dimethyl-bisphenol A can decrease Vegfa mRNA expression.
  • HY-132179
    Fucoidan

    		Glucosidase Cancer Metabolic Disease Cardiovascular Disease
    Fucoidan, a biologically active polysaccharide, is an efficient inhibitor of α-amylase and α-glucosidase. Anticoagulant, antitumor, antioxidant and antisteatotic activities.
  • HY-111376
    Pyrrophenone

    		Phospholipase Inflammation/Immunology Cardiovascular Disease
    Pyrrophenone is a potent and specific cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 4.2 nM.
  • HY-50855B
    Silmitasertib sodium salt

    CX-4945 sodium salt

    		 Casein Kinase Autophagy Cancer
    Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
  • HY-147879
    α-Glucosidase-IN-8

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-8 (Compound 4k) is a competitive α-glucosidase inhibitor with an IC50 of 0.18 µg/mL.
  • HY-11087
    SD 0006

    SD-06

    		 p38 MAPK Autophagy Inflammation/Immunology
    SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α.
  • HY-147964
    α-Glucosidase-IN-9

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-9 (compound 7) is a potent α-glucosidase inhibitor, with an IC50 of 55.6 μM. α-Glucosidase-IN-9 can be used for type II diabetes research.
  • HY-151135
    α-Glucosidase-IN-15

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-15 (Compound 14B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.34 μM. α-Glucosidase-IN-15 shows antidiabetic activity.
  • HY-18510
    IRE1α kinase-IN-7

    		IRE1 Others
    IRE1α kinase-IN-7 (compound 4) is an IRE1α kinase inhibitor. IRE1α kinase-IN-7 can be used for research of endoplasmic reticulum stress-related diseases.
  • HY-147965
    α-Glucosidase-IN-10

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-10 (compound 13) is a potent α-glucosidase inhibitor, with an IC50 of 92.7 μM. α-Glucosidase-IN-10 can be used for type II diabetes research.
  • HY-151141
    α-Glucosidase-IN-17

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-17 (Compound 12B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.79 μM. α-Glucosidase-IN-17 shows antidiabetic activity.
  • HY-148575
    α-Glucosidase-IN-23

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-23 is an orally active α-Glucosidase inhibitor. α-Glucosidase-IN-23 decreases blood glucose by a-glucosidase inhibition with an IC50 value of 4.48 μM. α-Glucosidase-IN-23 can be used for the research of diabetes.
  • HY-U00313
    Tropodifene

    Tropaphen

    		 Adrenergic Receptor Cardiovascular Disease Endocrinology
    Tropodifene (Tropaphen) is an α-Adrenergic receptor inhibitor.
  • HY-12753A
    Debutyldronedarone hydrochloride

    SR35021 hydrochloride

    		 Thyroid Hormone Receptor Cardiovascular Disease
    Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic.
  • HY-147518
    p38-α MAPK-IN-5

    		p38 MAPK Inflammation/Immunology
    p38-α MAPK-IN-5 (compound 4e) is a potent p38α inhibitor with IC50s of 0.1 nM, 0.2 nM, 944 nM, 4100 nM for p38α, p38 β, p38γ, p38δ, respectively. p38-α MAPK-IN-5 has anti-inflammatory effect. p38-α MAPK-IN-5 has the potential for asthma and chronic obstructive pulmonary disease (COPD) research.
  • HY-106954
    Upidosin

    Rec 15/2739; Recordati 15/2739; SB 216469

    		 Adrenergic Receptor Inflammation/Immunology
    Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction.
  • HY-129453
    BOP sodium

    		Integrin Inflammation/Immunology
    BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.
  • HY-12836A
    IFN alpha-IFNAR-IN-1 hydrochloride

    		IFNAR Inflammation/Immunology
    IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR. IFN alpha-IFNAR-IN-1 hydrochloride inhibits modified Vaccinia virus ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3- L-differentiated pDC cultures (BM-pDCs) (IC50=2-8 μM).
  • 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-151143
    α-Glucosidase-IN-19

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-19 (Compound 6B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.63 μM. α-Glucosidase-IN-19 shows anti-diabetic activity.
  • HY-151145
    α-Glucosidase-IN-21

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-21 (Compound 2B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 2.62 μM. α-Glucosidase-IN-21 shows anti-diabetic activity.
  • HY-151144
    α-Glucosidase-IN-20

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-20 (Compound 3B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.01 μM. α-Glucosidase-IN-20 shows anti-diabetic activity.
  • HY-W089785
    Methyl α-D-galactopyranoside monohydrate

    		Others Others
    Methyl α-D-galactopyranoside monohydrate is an alpha-D-galactoside having a methyl substituent at the anomeric position. Methyl α-D-galactopyranoside inhibits debaryomyces hansenii UFV-1 extracellular and intracellular α-galactosidases with Ki values of 0.82 and 1.12 mM, respectively.
  • HY-P99721
    Lutikizumab

    ABT-981

    		 Interleukin Related Inflammation/Immunology
    Lutikizumab (ABT-981) is an anti-IL-1α and IL-1β dual variable domain immunoglobulin. Lutikizumab binds and inhibits IL-1α and IL-1β. Lutikizumab can be used for the research of osteoarthritis.
  • HY-153122A
    YCT529

    		RAR/RXR Endocrinology
    YCT529 is a potent, selective and orally active RAR-α inhibitor.
  • HY-121172
    1,4-DPCA

    		HIF/HIF Prolyl-Hydroxylase Cancer
    1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
  • HY-123954
    Casein Kinase inhibitor A51

    		Casein Kinase CDK Apoptosis Cancer
    Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
  • HY-33549
    α-Methyl-p-tyrosine

    		Others Cancer
    α-Methyl-p-tyrosine is a competitive inhibitor of the enzyme tyrosine hydroxylase, which converts tyrosine to Levodopa (DOPA). α-Methyl-p-tyrosine is an orally active inhibitor of catecholamine synthesis which inhibits the hydroxylation of tyrosine to DOPA.
  • HY-151465
    HIF-1α-IN-4

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer.
  • HY-103204
    RS100329 hydrochloride

    		Adrenergic Receptor Endocrinology
    RS100329 hydrochloride is a potent and selective α1A-adrenoceptor antagonist with pKi values of 9.6, 7.9 and 7.5 for α1A, α1D, and α1B, respectively. RS100329 hydrochloride inhibits reflex urethral contractions. RS100329 hydrochloride can be used in research of benign prostatic hyperplasia.
  • HY-144699
    ERRα antagonist-2

    		Estrogen Receptor/ERR Cancer
    ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo.
  • HY-131404
    TPBM

    		Estrogen Receptor/ERR Cancer
    TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth.
  • HY-151921
    Anti-inflammatory agent 33

    		p38 MAPK Inflammation/Immunology
    Anti-inflammatory agent 33 is a potent p38α inhibitor. Anti-inflammatory agent 33 inhibits NO production. Anti-inflammatory agent 33 inhibits LPS-induced iNOS, COX-2, p-p38α, p-MK2 protein expression. Anti-inflammatory agent 33 shows anti-inflammatory activity.
  • HY-148922
    PPARα/γ agonist 2

    		PPAR Metabolic Disease
    PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent.
  • HY-146144
    HIF-IN-1

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity.
  • HY-P1266
    α-Conotoxin EI

    		nAChR Neurological Disease
    α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors.
  • HY-147777
    14α-Demethylase/DNA Gyrase-IN-2

    		Bacterial DNA/RNA Synthesis Infection
    14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-2 has antimicrobial activities.
  • HY-124314
    LEI-106

    		MAGL Metabolic Disease
    LEI-106 is a potent, dual sn-1-Diacylglycerol lipase α (DAGL-α)/ABHD6 inhibitor with an IC50 of 18 nM for DAGL-α and a Ki of 0.8 μM for ABHD6. LEI-106 inhibits the hydrolysis of [ 14C]-sn-1-oleoyl-2-arachidonoyl-glycerol, the natural substrate of DAGL-α, with a Ki of 0.7 μM.
  • HY-111022
    Icerguastat

    Sephin1; IFB-088

    		 Phosphatase Infection Inflammation/Immunology
    Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect.
  • HY-131335
    p38α inhibitor 2

    		p38 MAPK Inflammation/Immunology
    p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.
  • HY-119019
    ASB14780

    		Phosphatase Inflammation/Immunology
    ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM.
  • HY-U00090
    N-Methylmoranoline

    MOR 14; N-Methyl-1-deoxynojirimycin; N-Methylmoranolin

    		 Glucosidase Metabolic Disease
    N-Methylmoranoline (MOR 14) is an α-glucosidase inhibitor.
  • HY-147778
    14α-Demethylase/DNA Gyrase-IN-1

    		Bacterial DNA/RNA Synthesis Infection
    14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-1 has antimicrobial activities.
  • HY-153122
    YCT529 free acid

    		RAR/RXR Endocrinology
    YCT529 free acid is a potent, selective and orally active RAR-α inhibitor.
  • HY-19332
    Kifunensine

    FR-900494

    		 Others Inflammation/Immunology
    Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD.
  • HY-125713
    Ganoderic acid Y

    		Glucosidase Enterovirus Infection
    Ganoderic acid Y is a α-glucosidase inhibitor with an IC50 of 170 μM for yeast α-glucosidase. Ganoderic acid Y inhibits enterovirus 71 (EV71) replication through blocking EV71 uncoating.
  • 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-144696
    Dyrk1A/α-synuclein-IN-2

    		DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect.
  • HY-U00326
    PI3Kα/mTOR-IN-1

    		PI3K mTOR Cancer
    PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
  • HY-108469
    BI-6015

    		Others Cancer Metabolic Disease
    BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes.
  • HY-15893
    DMOG

    Dimethyloxallyl Glycine

    		 HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
  • HY-130437
    p-nitro-Pifithrin-α

    		MDM-2/p53 TGF-β Receptor Caspase Infection Metabolic Disease
    p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4]. non-alcoholic fatty liver disease.
  • HY-129113
    α-​Chaconine

    		COX Inflammation/Immunology
    α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
  • HY-146020
    Topoisomerase IIα-IN-1

    		Topoisomerase Cancer
    Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines.
  • HY-130264
    HIF-2α-IN-2

    		HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA).
  • HY-50855
    Silmitasertib

    CX-4945

    		 Casein Kinase Autophagy Cancer
    Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
  • HY-133807A
    (Rac)-Benpyrine

    		TNF Receptor Inflammation/Immunology
    (Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-14975
    R1487 Hydrochloride

    		p38 MAPK Autophagy Cancer
    R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively.
  • HY-148866
    Cavα2δ1&NET-IN-3

    		Calcium Channel Endocrinology Neurological Disease
    Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has Kis of 100-500 nM for human α2δ-1 subunit of Cav2.2 calcium channel and NET, respectively.
  • HY-N0492S
    α-Lipoic Acid-d5

    Thioctic acid-d5; (±)-α-Lipoic acid-d5; DL-α-Lipoic acid-d5

    		 NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid-d5 is the deuterium labeled α-Lipoic Acid. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4].
  • HY-N6782
    Oligomycin

    		ATP Synthase Fungal Antibiotic Cancer Infection
    Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
  • HY-131345
    PI3Kα-IN-4

    		PI3K Cancer
    PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity.
  • HY-100740C
    (1α,1'S,4β)-Lanabecestat

    (1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814

    		 Beta-secretase Neurological Disease
    (1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
  • HY-N3962
    Glycyrrhisoflavone

    		Glucosidase Metabolic Disease
    Glycyrrhisoflavone, an active prenylflavonoid, inhibits α-glucosidase.
  • HY-126306
    Deoxyfuconojirimycin hydrochloride

    Deoxyfuconojirimycin, Hydrochloride

    		 Others
    Deoxyfuconojirimycin hydrochloride is a specific competitive inhibitor of human liver α-L-fucosidase.
  • HY-15969
    Sal003

    		Phosphatase Apoptosis Cancer
    Sal003 is a potent, specific and cell-permeable inhibitor of the eukaryotic translation initiation factor 2α (eIF2α) phosphatase. Sal003 is a derivative of salubrinal.
  • HY-P3835
    Mating Factor α (1-6)

    		DNA/RNA Synthesis Endocrinology
    Mating Factor α (1-6) is a mating factor produced by α-mating type cells of Saccharomyces cerevisiae and an acts as an inhibitor of the initiation of DNA synthesis in the cells.
  • HY-10257
    BAY 11-7085

    BAY 11-7083

    		 NF-κB Ferroptosis Apoptosis Cancer
    BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
  • HY-131553
    D-α-Tocopherol Succinate

    Vitamin E succinate

    		 Apoptosis Cancer
    D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer.
  • HY-151138
    α-Glucosidase-IN-16

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-16 is a potent and orally active α-glucosidase inhibitor with an IC50 value of 3.28 μM. α-Glucosidase-IN-16 can reduce the level of blood glucose in Streptozotocin-induced diabetic rats. Antidiabetic activity.
  • HY-138097
    α-NETA

    		Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Apoptosis Cancer
    α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity.
  • HY-107641
    α-Cyano-4-hydroxycinnamic acid

    α-Cyano-4-hydroxycinnamate

    		 Monocarboxylate Transporter Metabolic Disease
    α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
  • HY-B0379A
    Adiphenine hydrochloride

    		nAChR Neurological Disease
    Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects.
  • HY-152479
    Topoisomerase IIα-IN-7

    		Topoisomerase Cancer
    Topoisomerase IIα-IN-7 is an DNA topoisomerase IIα inhibitor with an IC50 value of 7.7 µM. Topoisomerase IIα-IN-7 has broad-spectrum cytotoxicity to leukemia, lung, colon, melanoma, ovarian, kidney, prostate and breast cancer cells. Topoisomerase IIα-IN-7 has metabolic stability.
  • HY-U00179
    CDC801

    		Phosphodiesterase (PDE) TNF Receptor Cancer
    CDC801 is a potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α) inhibitor with IC50 of 1.1 μM and 2.5 μM, respectively.
  • HY-114368A
    Kira8 Hydrochloride

    AMG-18 Hydrochloride

    		 IRE1 Inflammation/Immunology
    Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-114368
    Kira8

    AMG-18

    		 IRE1 Inflammation/Immunology
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-N2223
    Ganoderol B

    Ganodermadiol

    		 Glucosidase Metabolic Disease
    Ganoderol B is a potent α-glucosidase inhibitor. Ganoderol B has high α-glucosidase inhibition with an IC50 of 48.5 μg/mL (119.8 μM).
  • HY-120823
    PF-05381941

    		MAP3K p38 MAPK Inflammation/Immunology
    PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively.
  • HY-15484
    Pifithrin-α hydrobromide

    Pifithrin hydrobromide; PFTα hydrobromide

    		 MDM-2/p53 Aryl Hydrocarbon Receptor Ferroptosis Apoptosis Cancer
    Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
  • HY-19707
    4μ8C

    IRE1 Inhibitor III

    		 IRE1 Metabolic Disease
    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
  • HY-147801
    Topoisomerase IIα-IN-3

    		Topoisomerase Apoptosis Cancer
    Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis.
  • HY-14126
    BIO-1211

    		Integrin Inflammation/Immunology
    BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively.
  • HY-19710
    MKC3946

    		IRE1 Cancer
    MKC3946 is a potent IRE1α inhibitor, used for cancer research.
  • HY-12285
    Serabelisib

    MLN1117; INK1117; TAK-117

    		 PI3K Cancer
    Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
  • 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-112401
    p38 MAP Kinase Inhibitor IV

    		p38 MAPK Inflammation/Immunology
    p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively.
  • HY-10328
    Neflamapimod

    VX-745

    		 p38 MAPK Autophagy Inflammation/Immunology
    Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
  • HY-129389
    Benzyl-α-GalNAc

    		Others Cancer
    Benzyl-α-GalNAc is a potent O-glycosylation inhibitor. Benzyl-α-GalNAc effectively inhibits the proliferation and activation of LX-2 cells and suppresses the expression of collagen I/III, which has good potential for investigation in liver fibrosis. Benzyl-α-GalNAc also significantly enhances the anti-tumour activity of 5-FU (HY-90006) (e.g. pancreatic cancer) by inhibiting O-glycosylation.
  • HY-N0877
    Bufalin

    		Na+/K+ ATPase Cancer
    Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
  • HY-116030
    JNJ-26076713

    		Integrin Metabolic Disease
    JNJ-26076713 is a potent and orally active alpha V integrin antagonist with IC50 values of 2.3 nM and 6.3 nM for alpha(V)beta(3) and alpha(V)beta(5), respectively. JNJ-26076713 inhibits retinal neovascularization.
  • HY-10231
    PX-478

    		HIF/HIF Prolyl-Hydroxylase Autophagy Cancer
    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
  • HY-103384
    TMCB

    		Casein Kinase Cancer
    TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively.
  • HY-W019838S
    D-Erythro-dihydrosphingosine-d7

    		Endogenous Metabolite Phospholipase Cancer
    D-Erythro-dihydrosphingosine-d7 is the deuterium labeled D-Erythro-dihydrosphingosine. D-Erythro-dihydrosphingosin directly inhibits cytosolic phospholipase A2α (cPLA2α) activity.
  • HY-B0219A
    Allopurinol sodium

    		Xanthine Oxidase Cancer Infection Inflammation/Immunology Neurological Disease
    Allopurinol sodium is a potent and orally active xanthine oxidase inhibitor with an IC50 value of 0.2-50 µM. Allopurinol sodium can be used in the treatment of hyperuricemia and gout. Allopurinol sodium decreases the expression of HIF-1α and HIF-2α protein. Allopurinol sodium shows anti-depressant and anti-nociception activity. Anti-leishmanial effect.
  • HY-B0219
    Allopurinol

    		Xanthine Oxidase Cancer Infection Inflammation/Immunology Neurological Disease
    Allopurinol is a potent and orally active xanthine oxidase inhibitor with an IC50 value of 0.2-50 µM. Allopurinol can be used in the treatment of hyperuricemia and gout. Allopurinol decreases the expression of HIF-1α and HIF-2α protein. Allopurinol shows anti-depressant and anti-nociception activity. Anti-leishmanial effect.
  • 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-100838
    cis-α-(Carboxycyclopropyl)glycine

    L-CCG III

    		 EAAT2 Neurological Disease
    cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes.
  • HY-123955
    Casein Kinase inhibitor A86

    		Casein Kinase CDK Apoptosis Cancer
    Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
  • HY-146305
    α-Glucosidase-IN-4

    		Glucosidase Cancer Infection Endocrinology Metabolic Disease Inflammation/Immunology Neurological Disease Cardiovascular Disease Others
    α-Glucosidase-IN-4 is a reversible and mixed type α-glucosidase inhibitor with an IC50 of 12.98 μM, a KI of 27.02 μM, and a KIS of 13.65 μM, respectively.
  • HY-10822
    Idetrexed

    BGC 945; ONX-0801

    		 Thymidylate Synthase Others
    Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L.
  • HY-12012
    SB 216763

    		GSK-3 Autophagy Neurological Disease Cancer
    SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
  • HY-16031
    AFP464 free base

    NSC710464 free base

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
  • HY-120337
    V-11-0711

    		Others Cancer
    V-11-0711 is a potent and selective choline kinase alpha (ChoKα) inhibitor with an IC50 of 20 nM. V-11-0711 causes a reversible growth arrest in HeLa cells.
  • HY-N0374
    Licochalcone C

    		Glucosidase Metabolic Disease
    Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.
  • HY-N3115
    Palbinone

    		Others Inflammation/Immunology
    Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity.
  • HY-108531
    ER 50891

    		RAR/RXR Cancer
    ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). ER-50891 significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis.
  • HY-N0466
    Rebaudioside A

    		Endogenous Metabolite Glucosidase Others
    Rebaudioside A is a steviol glycoside, α-glucosidase inhibitor with IC50 of 35.01 μg/ml.
  • HY-13261
    A66

    		PI3K Cancer
    A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
  • HY-W009783
    1-Deoxymannojirimycin hydrochloride

    		HIV Influenza Virus Infection
    1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity.
  • HY-147767
    PI3Kα-IN-6

    		PI3K Apoptosis Reactive Oxygen Species Cancer
    PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis.
  • HY-100536
    IWP-3

    		Wnt Cancer
    IWP-3 is an potent inhibitor of Wnt production with an IC50 of 40 nM. IWP-3 inhibits Porcupine (Porcn) function thereby blocking palmitoylation of Wnt proteins. IWP-3 inhibits CK1γ3 and CK1ε only moderately and does not inhibit CK1α.
  • 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-133807
    Benpyrine

    		TNF Receptor Inflammation/Immunology
    Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-125777A
    α-Conotoxin Vc1.1 TFA

    		nAChR Neurological Disease
    α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach.
  • HY-147708
    T-Type calcium channel inhibitor 2

    		Calcium Channel Cancer
    T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively.
  • HY-118091B
    LY300503

    		Others Others
    LY300503 is an enantiomer of LY191704. LY191704 is a human type I 5α-reductase inhibitor.
  • HY-136347
    3α-Hydroxy pravastatin sodium

    		HMG-CoA Reductase (HMGCR) Drug Metabolite Cardiovascular Disease
    3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor.
  • HY-13281
    PIK-75 hydrochloride

    		DNA-PK PI3K Apoptosis Cancer
    PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
  • HY-107834
    PIK-75

    		DNA-PK PI3K Apoptosis Cancer
    PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
  • HY-108623
    Atizoram

    CP-80,633

    		 Phosphodiesterase (PDE) Inflammation/Immunology
    Atizoram (CP-80,633), a cyclic nucleotide phosphodiesterase (PDE4) inhibitor, elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice.
  • HY-B0194S
    Tizanidine-d4

    		Adrenergic Receptor Neurological Disease Endocrinology Cancer
    Tizanidine-d4 is the deuterium labeled Tizanidine. Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons[1][2].
  • HY-N10413
    Diphlorethohydroxycarmalol

    		Glucosidase Metabolic Disease
    Diphlorethohydroxycarmalol, a kind of phlorotannin, is an orally active α-glucosidase and α-amylase inhibitor with IC50s of 0.16 mM and 0.53 mM, respectively. Diphlorethohydroxycarmalol has anti-diabetic activities.
  • HY-10401
    VX-702

    		p38 MAPK Autophagy Inflammation/Immunology
    VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
  • HY-N2566
    Euscaphic acid

    		DNA/RNA Synthesis PI3K Apoptosis Cancer
    Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
  • HY-111255
    SPD304

    		TNF Receptor Cancer
    SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
  • HY-111255A
    SPD304 dihydrochloride

    		TNF Receptor Inflammation/Immunology
    SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
  • HY-146021
    Topoisomerase IIα-IN-2

    		Topoisomerase Cancer
    Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase.
  • 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-16560
    Camptothecin

    Campathecin; (S)-(+)-Camptothecin; CPT

    		 Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Cancer Infection
    Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
  • HY-16194
    Emiglitate

    BAY o 1248

    		 Others Metabolic Disease
    Emiglitate (BAY o 1248) is a potent, selective and competitive inhibitor of α-glucoside hydrolase.
  • HY-14857
    Carotegrast

    		Integrin Inflammation/Immunology
    Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
  • HY-129619
    SNIPER(ER)-87

    		SNIPERs Estrogen Receptor/ERR Cancer
    SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
  • HY-116446
    Pironetin

    		Microtubule/Tubulin Cancer
    Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity.
  • HY-10801
    CAY10650

    		Phospholipase Inflammation/Immunology
    CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM. CAY10650 suppresses lipid droplets formation and PGE2 secretion.
  • HY-108697A
    (Rac)-PT2399

    		HIF/HIF Prolyl-Hydroxylase Cancer
    (Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM.
  • HY-U00037
    Ecopladib

    PLA 725

    		 Phospholipase Inflammation/Immunology
    Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
  • HY-135674
    SR-318

    		p38 MAPK TNF Receptor Cancer Inflammation/Immunology
    SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
  • HY-12399
    MKC9989

    		IRE1 Cancer
    MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
  • HY-N0255
    alpha-Hederin

    α-Hederin

    		 Apoptosis Others
    alpha-Hederin (α-Hederin), a monodesmosidic triterpenoid saponin, exhibits promising antitumor potential against a variety of human cancer cell lines. alpha-Hederin could inhibit the proliferation and induce apoptosis of gastric cancer accompanied by glutathione decrement and reactive oxygen species generation via activating mitochondrial dependent pathway.
  • HY-107553
    Chetomin

    		HSP Apoptosis Cancer
    Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule.
  • HY-144695
    Dyrk1A/α-synuclein-IN-1

    		DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect.
  • HY-152158
    α-Glucosidase-IN-22

    		Glucosidase Metabolic Disease
    α-Glucosidase-IN-22 (compound 7i), a benzimidazole, is a potent α-glucosidase inhibitor with an IC50 of 0.64 μM. α-Glucosidase-IN-22 is a potent anti-diabetic agent and has the potential for type 2 diabetes mellitus (T2DM) research.
  • HY-10403
    PH-797804

    		p38 MAPK Autophagy Inflammation/Immunology Cancer
    PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC50=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.
  • 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-16294
    LY2090314

    		GSK-3 Cancer
    LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
  • HY-B0661A
    Tamsulosin hydrochloride

    (R)-(-)-YM12617; LY253351

    		 Adrenergic Receptor Endogenous Metabolite Neurological Disease Endocrinology Cancer
    Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models.
  • HY-N6968
    α-Humulene

    Humulene; α-Caryophyllene

    		 NO Synthase COX Inflammation/Immunology
    α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression.
  • HY-143224
    NCGC00138783

    		Others Cancer
    NCGC00138783 is a selective inhibitor targeting CD47/SIRPα axis, with an IC50 of 50 µM. NCGC00138783 directly blocks the interaction between CD47 and SIRPα axis.
  • HY-U00266
    Cefetrizole

    		Glucosidase Infection Metabolic Disease
    Ceftezole is an α-Glucosidase inhibitor with an IC50 and a Ki of 2.1 μM and 0.578 μM, respectively.
  • HY-13864
    PF-4989216

    		PI3K Apoptosis Cancer
    PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
  • HY-145678
    α-HNJNAc

    		Others Metabolic Disease
    α-HNJNAc is a potent, competitive hexosaminidases inhibitor without interfering with other glycosidases.
  • HY-101272
    GDC-0326

    		PI3K Cancer
    GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
  • HY-16560S
    Camptothecin-d5

    Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5

    		 Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Cancer Infection
    Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
  • HY-115463
    EB-3D

    		AMPK Apoptosis Cancer
    EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
  • HY-12398A
    TEI-9648

    		VD/VDR Metabolic Disease Inflammation/Immunology
    TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research.
  • HY-15468
    IOX2

    		HIF/HIF Prolyl-Hydroxylase Cancer
    IOX2 is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 can be used in the study of thrombotic diseases.
  • HY-15468A
    IOX2 sodium

    		HIF/HIF Prolyl-Hydroxylase Cancer Cardiovascular Disease
    IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases.
  • HY-120111
    MW-150

    MW01-18-150SRM

    		 p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-128463S
    N-tert-Butyl-α-phenylnitrone-d14

    		COX Reactive Oxygen Species
    N-tert-Butyl-α-phenylnitrone-d14 is the deuterium labeled N-tert-Butyl-α-phenylnitrone[1]. N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier[2][3][4][5].
  • HY-148318
    CK2α-IN-1

    		Casein Kinase Cancer
    CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC50=7.0 µM; Ki=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies.
  • 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-116248
    Ro 41-5253

    		RAR/RXR Apoptosis Cancer
    Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity.
  • HY-147983
    PI3Kα-IN-8

    		PI3K Reactive Oxygen Species Apoptosis Cancer
    PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC50 of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrial membrane potential and induces apoptosis.
  • HY-122094
    Steppogenin

    		HIF/HIF Prolyl-Hydroxylase Cancer Cardiovascular Disease
    Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.
  • HY-15761
    AZD2858

    		GSK-3 Neurological Disease
    AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
  • HY-N0375
    18α-Glycyrrhetinic acid

    		Proteasome NF-κB Apoptosis Cancer Inflammation/Immunology Neurological Disease
    18α-Glycyrrhetinic acid, a diet-derived compound, is an inhibitor of NF-kB and an activator of proteasome, which serves as pro-longevity and anti-aggregation factor in a multicellular organism. 18α-Glycyrrhetinic acid induces apoptosis.
  • HY-126683
    Mal-C6-α-Amanitin

    		Drug-Linker Conjugates for ADC Cancer
    Mal-C6-α-Amanitin is a drug-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.
  • HY-143268
    HPA-IN-1

    		Amylases Glucosidase Metabolic Disease
    HPA-IN-1 (Compound 1) is a potent and selective human pancreatic α-amylase (HPA) inhibitor with IC50 values of 12.0 μM and 410.4 μM against HPA and α-glucosidase, respectively.
  • HY-108431
    MN58b

    		Apoptosis Cancer
    MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity.
  • HY-147712
    PKC-IN-4

    		PKC Inflammation/Immunology
    PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature.
  • HY-116626
    SM-7368

    		NF-κB p38 MAPK MMP Cancer
    SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation. SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
  • HY-18759
    BMS-751324

    		p38 MAPK TNF Receptor Inflammation/Immunology
    BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model.
  • HY-148413
    Aprinocarsen sodium

    ISIS 3521 sodium

    		 PKC Cancer
    Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers.
  • 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-W014049
    N'-Nitro-D-arginine

    		NO Synthase Others
    N'-Nitro-D-arginine, a nitric oxide synthesis inhibitor, also is a vasodilator that relaxes the smooth muscles and increases blood flow to the penis, improving erections. N'-Nitro-D-arginine also inhibits neutrophil migration by blocking receptors for tumour necrosis factor alpha (TNFα) and interleukin 8 (IL8).
  • HY-B0661
    Tamsulosin

    (R)-(-)-YM12617 free base; LY253351 free base

    		 Adrenergic Receptor Endogenous Metabolite Cancer Endocrinology Neurological Disease
    Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models.
  • HY-12825
    BHPI

    		Estrogen Receptor/ERR Cancer
    BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
  • HY-116301
    CAY10502

    		Phospholipase Inflammation/Immunology
    CAY10502 is a potent, calcium-dependent cytosolic phospholipase A2 α (cPLA2α) inhibitor with an IC50 of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases.
  • HY-U00458
    K-80003

    TX-803

    		 Akt Cancer
    K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
  • HY-147078
    EJMC-1

    		TNF Receptor Inflammation/Immunology
    EJMC-1 is a moderately potent TNF-α inhibitor with an IC50 value of 42 μM.
  • HY-100337
    WWL70

    		MAGL Neurological Disease
    WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM.
  • HY-16937
    ISA-2011B

    		Others Cancer
    ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .
  • HY-150001
    Thunbergol

    Isocembrol

    		 TNF Receptor Inflammation/Immunology
    Thunbergol (Isocembrol) (Compound 17) is a potent TNF-α inhibitor with an IC50 of 7.2 μM.
  • HY-135385
    Dihydro Dutasteride

    		Drug Metabolite Inflammation/Immunology
    Dihydro Dutasteride is a metabolite of Dutasteride. Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.
  • HY-108645
    AL 8697

    		p38 MAPK Autophagy Inflammation/Immunology
    AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity.
  • HY-12398
    TEI-9647

    		VD/VDR Metabolic Disease Inflammation/Immunology
    TEI-9647, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Paget's disease.
  • HY-131089
    MC-VC-PABC-C6-alpha-Amanitin

    		Antibody-Drug Conjugates (ADCs) Cancer
    MC-VC-PABC-C6-alpha-Amanitin is an antibody drug conjugate consisting of an anticancer toxin alpha-Amanitin (HY-19610) and a monoclonal antibody MC-VC-PABC-C6. Among them, alpha-Amanitin is a potent inhibitor of RNA polymerase IIα. MC-VC-PABC-C6-alpha-Amanitin accurately targets HER2 receptors, specifically recognizes HER2-positive tumor cells. It is widely used in breast cancer and gastric cancer research.
  • HY-147954
    α-Glycosidase-IN-1

    		Carbonic Anhydrase Cholinesterase (ChE) Metabolic Disease Neurological Disease
    α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy.
  • HY-U00460
    3,6-DMAD hydrochloride

    		IRE1 Cancer
    3,6-DMAD hydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer.
  • HY-101562
    Inavolisib

    GDC-0077; RG6114

    		 PI3K Apoptosis Cancer
    GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.
  • HY-U00460B
    3,6-DMAD dihydrochloride

    		IRE1 Cancer
    3,6-DMAD dihydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer.
  • HY-W263279
    (E)-Guanabenz

    (E)-Wy-8678

    		 Adrenergic Receptor Neurological Disease Cardiovascular Disease
    (E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease.
  • HY-106720
    Amosulalol

    YM 09538

    		 Adrenergic Receptor Cardiovascular Disease
    Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR).
  • HY-N4121
    Isocurcumenol

    		Estrogen Receptor/ERR Apoptosis Cancer
    Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively.
  • HY-143269
    HPA-IN-2

    		Amylases Glucosidase Metabolic Disease
    HPA-IN-2 (Compound 2a-1) is a potent and selective human pancreatic α-amylase (HPA) inhibitor with IC50 values of 8.2 μM and 450.7 μM against HPA and α-glucosidase, respectively.
  • HY-B0392
    (S)-(+)-Rolipram

    (+)-Rolipram; (S)-Rolipram

    		 Phosphodiesterase (PDE) Apoptosis Cancer Inflammation/Immunology Neurological Disease
    (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
  • HY-N8884
    Coelonin

    		PTEN Akt NF-κB Interleukin Related TNF Receptor Inflammation/Immunology
    Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein.
  • HY-110193
    SPP-86

    		RET Cancer
    SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
  • 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-13453
    BAY 11-7082

    BAY 11-7821

    		 IKK Deubiquitinase Autophagy Apoptosis NF-κB Cancer Inflammation/Immunology
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-136474
    Amidephrine

    (±)-Amidephrine

    		 Adrenergic Receptor Endocrinology
    Amidephrine is a selective agonist of alpha 1-adrenoceptor. Amidephrine inhibits inhibits monopulse field contraction of the vas deferens epithelium and prostate gland.
  • HY-101068
    TOFA

    RMI14514; MDL14514

    		 Acetyl-CoA Carboxylase Cancer
    TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).
  • HY-N0596
    Panaxadiol

    20(R)-Panaxadiol

    		 PD-1/PD-L1 HIF/HIF Prolyl-Hydroxylase STAT Cancer
    Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities.
  • HY-115983
    DMUP

    		Apoptosis Cancer
    DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity.
  • HY-128677
    NCC007

    		Casein Kinase Neurological Disease
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
  • HY-143224A
    NCGC00138783 free base

    		Others Cancer
    NCGC00138783 free base is a selective inhibitor targeting CD47/SIRPα axis, with an IC50 of 50 µM. NCGC00138783 free base directly blocks the interaction between CD47 and SIRPα axis.
  • HY-138688
    Cinnamyl-3,4-dihydroxy-α-cyanocinnamate

    CDC

    		 Lipoxygenase Metabolic Disease
    Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent 12/15-Lipoxygenases (LO) inhibitor. Cinnamyl-3,4-dihydroxy-α-cyanocinnamate has the potential for the research of type 1 diabetes mellitus.
  • HY-152089
    SB26019

    		Microtubule/Tubulin Inflammation/Immunology Neurological Disease
    SB26019 is a potent anti-neuroinflammatory agent. SB26019 regulates NF-κB activation by inducing monomeric α-tubulin formation. SB26019-induced α-tubulin monomer inhibits p65 translocation.
  • HY-107674
    bPiDDB

    		nAChR Neurological Disease
    bPiDDB is a potent nAChR antagonist. bPiDDB potently (IC50=2 nM) inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs.
  • HY-19931
    COH29

    RNR Inhibitor COH29

    		 DNA/RNA Synthesis Cancer
    COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
  • HY-149008
    α-Amylase-IN-3

    		Amylases Cancer Metabolic Disease
    α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease.
  • HY-150618
    PI3Kα-IN-9

    		PI3K Apoptosis Cancer
    PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research.
  • HY-117822
    BRD0209

    		GSK-3 Neurological Disease
    BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases.
  • HY-13229
    BOC-D-FMK

    		Caspase Apoptosis Cancer
    Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
  • HY-135902
    Synucleozid

    NSC 377363

    		 DNA/RNA Synthesis Neurological Disease
    Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-135902A
    Synucleozid hydrochloride

    NSC 377363 hydrochloride

    		 DNA/RNA Synthesis Neurological Disease
    Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
  • HY-19731
    SID 3712249

    MiR-544 Inhibitor 1

    		 MicroRNA Apoptosis Cancer
    SID 3712249 (MiR-544 Inhibitor 1) is a miR-544 biogenesis inhibitor. SID 3712249 binds directly to the precursor miRNA. SID 3712249 blocks production of the mature microRNA and decreases miR-544, HIF-1α, and ATM transcripts. SID 3712249 can be used in the research of cancers, such as breast cancer.
  • HY-122058A
    KRH-3955 hydrochloride

    		CXCR HIV Infection Inflammation/Immunology
    KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.
  • HY-108346
    JX401

    		p38 MAPK Inflammation/Immunology
    JX401 is a potent inhibitor of p38alpha, containing a 4-benzylpiperidine motif. p38alpha is hyperactive in inflammatory diseases, and various indications suggest that its inhibition would reverse inflammation. JX401 has the potential for the research of inflammation.
  • HY-111055
    BIP-135

    		GSK-3 Neurological Disease
    BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.
  • HY-110398
    5,6,7-Trimethoxyflavone

    Baicalein trimethyl ether

    		 p38 MAPK Inflammation/Immunology Cancer
    5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera.
  • HY-19383
    Ertiprotafib

    PTP 112

    		 Phosphatase IKK PPAR Metabolic Disease
    Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
  • HY-151453
    Topoisomerase IIα-IN-4

    		Topoisomerase Apoptosis Cancer
    Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.
  • HY-128463
    N-tert-Butyl-α-phenylnitrone

    		COX Reactive Oxygen Species Metabolic Disease Inflammation/Immunology Neurological Disease
    N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier.
  • HY-145904
    PDGFRα/FLT3-ITD-IN-3

    		PDGFR FLT3 Cancer
    PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of 0.153 and 0.004 μM, respectively. PDGFRα/FLT3-ITD-IN-3 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.
  • 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-A0009
    Galanthamine hydrobromide

    Galantamine hydrobromide

    		 Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
  • 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-142958
    NF-κB-IN-2

    		NF-κB Neurological Disease
    NF-κB-IN-2 inhibits TNF-α-induced canonical NF-κB signaling in PC-3 cells.
  • HY-U00206
    D2343

    		Adrenergic Receptor Endocrinology
    D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.
  • HY-100947
    VH-298

    		Ligands for E3 Ligase Others
    VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology.
  • HY-117721
    IHVR-11029

    		Glucokinase Infection Inflammation/Immunology
    IHVR-11029 is a small molecule inhibitor of ER α-glucosidases, with an EC50 of 0.09 μM.
  • HY-117771A
    DO34 analog

    		Others Metabolic Disease
    DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.
  • HY-128420
    Lobeline sulfate

    α-Lobeline sulfate; L-Lobeline sulfate

    		 Endogenous Metabolite Neurological Disease
    Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) is a nonstimulant medication that can alter dopamine uptake in brain. Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) inhibits nicotine-induced hyperactivity and is effective in smoking cessation.
  • HY-P9926
    Dupilumab

    REGN-668; SAR-231893

    		 Interleukin Related Inflammation/Immunology Cancer
    Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis.
  • HY-15483
    DY131

    GSK 9089

    		 Estrogen Receptor/ERR Smo Cancer Endocrinology
    DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ. DY131 also inhibits Smo signaling.
  • HY-145425
    PAIR2

    		IRE1 Cancer
    PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing.
  • HY-131504A
    Valienamine

    		Glucosidase Metabolic Disease
    Valienamine is the alpha-glucosidase inhibitor. Valienamine is the key functional component of many natural glycosidase inhibitors including the crop protectant validamycin A and the antidiabetic agent acarbose.
  • HY-15486
    Salubrinal

    		Phosphatase HSV Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
  • HY-143279
    Topoisomerase II inhibitor 3

    		Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential.
  • HY-114454
    INH14

    		IKK Cancer Inflammation/Immunology
    INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
  • HY-P1259
    PR-39

    		Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-131345A
    (S)-PI3Kα-IN-4

    		PI3K Cancer
    (S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer.
  • HY-P1189
    Echistatin

    		Integrin Metabolic Disease Inflammation/Immunology
    Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-120111A
    MW-150 hydrochloride

    MW01-18-150SRM hydrochloride

    		 p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-P1189A
    Echistatin TFA

    		Integrin Metabolic Disease Inflammation/Immunology
    Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
  • HY-138071
    8α-Tigloyloxyhirsutinolide 13-O-acetate

    		STAT Pyroptosis Apoptosis Reactive Oxygen Species c-Myc Bcl-2 Family TrxR Cancer
    8α-Tigloyloxyhirsutinolide 13-O-acetate is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo.
  • HY-128942
    MAC glucuronide α-hydroxy lactone-linked SN-38

    		Drug-Linker Conjugates for ADC Cancer
    MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 99 and 105 ng/mL, respectively.
  • HY-N6962
    α-Spinasterol

    		TRP Channel COX Bacterial Infection Neurological Disease
    α-Spinasterol, isolated from Melandrium firmum, has antibacterial activity. α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.
  • HY-145902
    PDGFRα/FLT3-ITD-IN-1

    		PDGFR FLT3 Cancer
    PDGFRα/FLT3-ITD-IN-1 (Compound 12d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.
  • HY-145903
    PDGFRα/FLT3-ITD-IN-2

    		PDGFR FLT3 Cancer
    PDGFRα/FLT3-ITD-IN-2 (Compound 13d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 20 and 1.654 μM, respectively. PDGFRα/FLT3-ITD-IN-2 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia.
  • HY-151382
    CK2-IN-3

    		Casein Kinase Cancer
    CK2-IN-3 is a selective and potent CK2 inhibitor (Kd: 12 nM), with IC50 values of 1.51 μM (CK2α) and 7.64 μM (CK2α’). CK2-IN-3 can be used in the research of cancers.
  • HY-B0661AS1
    Tamsulosin-d4 hydrochloride

    (R)-(-)-YM12617-d4; LY253351-d4

    		 Adrenergic Receptor Endogenous Metabolite Neurological Disease Endocrinology
    Tamsulosin-d4 (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
  • HY-N0328
    alpha-Mangostin

    α-Mangostin

    		 Reactive Oxygen Species Apoptosis Bacterial Fungal Virus Protease Cancer
    alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
  • HY-B0661AS
    Tamsulosin-d5 hydrochloride

    		Adrenergic Receptor Endogenous Metabolite Neurological Disease Endocrinology
    Tamsulosin-d5 (hydrochloride) is the deuterium labeled Tamsulosin hydrochloride. Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
  • HY-12407
    ZK168281

    		VD/VDR Metabolic Disease
    ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.
  • HY-137309
    4-Deoxy-4α-phorbol

    		HIV Others
    4-Deoxy-4α-phorbol is a tetracyclic diterpene found in E. desmondi. It has been used in the semisynthesis of inhibitors of the HIV-1-induced cytopathic effect on MT-4 cells and 4α-phorbol esters.
  • HY-N3101
    Pedalitin

    		Endogenous Metabolite Tyrosinase Glucosidase Endocrinology
    Pedalitin is a inhibitor of tyrosinase（IC50=0.28 mM） and α-glucosidase（IC50=0.29 mM）.
  • HY-101041
    (E)-AG 556

    (E)-Tyrphostin AG 556

    		 EGFR Inflammation/Immunology
    (E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production.
  • HY-19610
    α-Amanitin

    α-Amatoxin

    		 DNA/RNA Synthesis ADC Cytotoxin Cancer
    α-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
  • HY-N0472
    Geraniin

    		TNF Receptor Cancer Metabolic Disease Inflammation/Immunology
    Geraniin is a TNF-α releasing inhibitor with numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities, with an IC50 of 43 μM.
  • HY-12050
    CP-673451

    		PDGFR Cancer
    CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
  • HY-G0008
    O-Desmethyl Mebeverine alcohol

    Mebeverine metabolite O-desmethyl Mebeverine alcohol

    		 Adrenergic Receptor Drug Metabolite Metabolic Disease
    O-Desmethyl Mebeverine alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
  • HY-N0694
    Schisantherin A

    Gomisin-C; Schizantherin-A; Wuweizi ester-A

    		 NF-κB Inflammation/Immunology
    Schisantherin A is a dibenzocyclooctadiene lignan. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
  • HY-16596
    CNX-1351

    		PI3K Cancer
    CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
  • HY-100470
    NSC781406

    		PI3K mTOR Cancer
    NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
  • HY-U00459A
    GSK2850163 (S enantiomer)

    		IRE1 Others
    GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
  • HY-G0008A
    O-Desmethyl Mebeverine alcohol hydrochloride

    Mebeverine metabolite O-desmethyl Mebeverine alcohol hydrochloride

    		 Adrenergic Receptor Drug Metabolite Metabolic Disease
    O-Desmethyl Mebeverine alcohol hydrochloride is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
  • HY-U00125
    CGP-53153

    		5 alpha Reductase Endocrinology
    CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC50s of 36 and 262 nM in rat and human prostatic tissue, respectively.
  • HY-115738
    2-Acetamido-2,4-dideoxy-4-fluoro-α-D-glucopyranose

    		Others Metabolic Disease
    2-Acetamido-2,4-dideoxy-4-fluoro-α-D-glucopyranose (compound 13) is a hepatic glycosaminoglycan biosynthesis inhibitor.
  • HY-N0492
    α-Lipoic Acid

    Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid

    		 NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
  • HY-14648S3
    Dexamethasone-4,6α,21,21-d4

    		Glucocorticoid Receptor SARS-CoV Autophagy Complement System Mitophagy Bacterial Antibiotic
    Dexamethasone-4,6α,21,21-d4 is the deuterium labeled Dexamethasone-4,6α,21,21. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
  • HY-N0492A
    α-Lipoic Acid sodium

    Thioctic acid sodium; (±)-α-Lipoic acid sodium; DL-α-Lipoic acid sodium

    		 NF-κB HIV Mitochondrial Metabolism Endogenous Metabolite Apoptosis Cancer Infection Inflammation/Immunology
    α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
  • HY-P1259A
    PR-39 TFA

    		Proteasome Bacterial Inflammation/Immunology
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-N0613
    Sauchinone

    		NF-κB Inflammation/Immunology
    Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
  • HY-15544
    CCR1 antagonist 10

    		CCR Inflammation/Immunology
    CCR1 antagonist 10 (example 1) is a potent and orally active CCR1 antagonist. CCR1 antagonist 10 inhibits 125I-MIP-1α binding to THP-1 cell membranes with an Ki value of 2.3 nM.
  • HY-110114
    Gue1654

    		Others Others
    Gue1654 is a modulator of OXE-R. Gue1654 inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R. Gue1654 does not interfere nonspecifically with signaling directly at or downstream of Gβγ.
  • HY-12987
    Pimozide

    R6238

    		 Dopamine Receptor Adrenergic Receptor STAT Parasite Cancer Neurological Disease Endocrinology
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-13076
    CHIR-98014

    		GSK-3 Metabolic Disease
    CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
  • HY-108606
    PI-828

    		PI3K Casein Kinase Cancer
    PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
  • HY-120217
    VH032

    		Ligands for E3 Ligase Cancer
    VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd
  • HY-13228
    YM-201636

    		PIKfyve PI3K Autophagy Influenza Virus Cancer Infection
    YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with an IC50 of 3.3 μM. YM-201636 inhibits retroviral replication.
  • HY-W005308
    N-BOC-DL-serine methyl ester

    		Amino Acid Derivatives Cancer
    N-BOC-DL-serine methyl ester is a Serine derivative. N-BOC-DL-serine methyl ester is used for the synthesis of α,β-dehydro-α-amino acid. N-BOC-DL-serine methyl ester is also used for the synthesis of anti-cancer agent, such as quinazolinone derivative that inhibits PI3K activity, and tricyclic pyrolopyranopyridines that inhibits protein kinase activity.
  • HY-110112
    BTT-3033

    		Integrin Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease.
  • HY-N1029
    Norathyriol

    Mangiferitin

    		 Glucosidase PPAR Cancer Infection Inflammation/Immunology
    Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM. Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively. Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
  • HY-16134A
    Celgosivir hydrochloride

    MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride

    		 Glucosidase HCV HIV Infection
    Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
  • HY-16134
    Celgosivir

    MBI 3253; MDL 28574; MX3253

    		 Glucosidase HCV HIV Infection
    Celgosivir (MBI 3253; MDL 28574; MX3253) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
  • HY-112619
    TES-991

    		Others Metabolic Disease
    TES-991 is a potent and selective human α‑Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC50 of 3 nM.
  • HY-N7809
    Pelargonidin 3-galactoside chloride

    		Others Cancer
    Pelargonidin 3-galactoside chloride is a major anthocyanin with anticancer effects. Pelargonidin 3-galactoside chloride inhibits α-glucosidase.
  • HY-125833
    Alpha-Naphthoflavone

    		Cytochrome P450 Cancer
    Alpha-Naphthoflavone is a flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
  • HY-16715
    Acumapimod

    BCT197

    		 p38 MAPK Autophagy Inflammation/Immunology
    Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.
  • HY-112716
    N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride

    		Others Cancer
    N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death.
  • HY-N3625
    Coronalolic acid

    Coronalonic acid

    		 NF-κB Inflammation/Immunology
    Coronalolic acid, extract from the apical bud of Gardenia sootepenesis Hutch, inhibits TNF-α-induced NF-κB activity and NO production.
  • HY-16196
    ENMD-1198

    IRC-110160

    		 Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT Cancer
    ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
  • HY-103248
    Toyocamycin

    Vengicide

    		 IRE1 Fungal Antibiotic Apoptosis CDK Cancer Infection
    Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM.
  • HY-146163
    Topoisomerase II inhibitor 7

    		Topoisomerase Apoptosis Cancer
    Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis.
  • HY-132205
    DS45500853

    		Estrogen Receptor/ERR Metabolic Disease
    DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).
  • 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-10626
    T0901317

    		LXR FXR ROR Apoptosis Cancer Metabolic Disease Cardiovascular Disease
    T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
  • HY-16478
    Trifluridine/tipiracil hydrochloride mixture

    TAS-102

    		 Nucleoside Antimetabolite/Analog Thymidylate Synthase Cancer
    Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA.
  • HY-P2358
    PSMα3

    		Toll-like Receptor (TLR) Inflammation/Immunology
    PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA).
  • HY-143201
    DS20362725

    		Estrogen Receptor/ERR Metabolic Disease
    DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM).
  • HY-12040
    Elesclomol

    STA-4783

    		 Reactive Oxygen Species Apoptosis Cancer
    Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research.
  • HY-148252
    ADRA1D receptor antagonist 1 free base

    		Adrenergic Receptor Endocrinology
    ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
  • HY-120111B
    MW-150 dihydrochloride dihydrate

    MW01-18-150SRM dihydrochloride dihydrate

    		 p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-110261
    GS143

    		IKK E1/E2/E3 Enzyme NF-κB Inflammation/Immunology
    GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
  • HY-13241A
    Ralimetinib

    LY2228820

    		 p38 MAPK Autophagy Cancer Inflammation/Immunology
    Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
  • HY-151361
    AMPK-IN-3

    		AMPK Cancer
    AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer.
  • HY-N1919
    Ajmalicine

    Raubasine

    		 Adrenergic Receptor Cholinesterase (ChE) Endocrinology Neurological Disease
    Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity.
  • HY-N1919A
    Ajmalicine hydrochloride

    Raubasine hydrochloride

    		 Adrenergic Receptor Cholinesterase (ChE) Endocrinology Neurological Disease
    Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity.
  • 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-150739
    ODN 21158

    		Toll-like Receptor (TLR) Inflammation/Immunology
    ODN 21158 is a potent G-modified TLR3 and TLR9 inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 inhibits IFN-α secretion in a dose dependent manner.
  • HY-15845
    STF-083010

    		IRE1 Cancer
    STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
  • HY-112182
    UM-164

    DAS-DFGO-II

    		 Src p38 MAPK Autophagy Cancer
    UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
  • HY-15704
    LH846

    		Casein Kinase Cancer
    LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
  • HY-14622
    Necrostatin 2

    		RIP kinase Cancer
    Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. Necrostatin 2 is also a RIPK1 inhibitor.
  • 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-13468
    KW-2478

    		HSP Cancer
    KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
  • HY-16719
    Dapaconazole

    		Cytochrome P450 Infection
    Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM.
  • HY-13535
    ATN-161

    		Integrin Cancer
    ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  • HY-109190
    Seralutinib

    GB002; PK10571

    		 PDGFR Cardiovascular Disease
    Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
  • HY-10822A
    ONX 0801 trisodium

    BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium

    		 Thymidylate Synthase Cancer
    ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors.
  • HY-13535A
    ATN-161 trifluoroacetate salt

    ATN-161 TFA salt

    		 Integrin Cancer
    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  • HY-101028
    ZINC13466751

    		HIF/HIF Prolyl-Hydroxylase Cancer Cardiovascular Disease
    ZINC13466751 is a potent inhibitor of HIF-1α/von Hippel-Lindau interaction with an IC50 of 2.0 µM.
  • HY-148454
    Necroptosis-IN-3

    		Necroptosis 11β-HSD Cancer Inflammation/Immunology
    Necroptosis-IN-3 (Compound 69) is a necroptosis inhibitor that inhibits TNF-α induced necroptosis. Necroptosis-IN-3 (Compound STX1638) also inhibits 11β-HSD1.
  • HY-136010
    RIP2 Kinase Inhibitor 4

    		RIP kinase PROTACs Inflammation/Immunology
    RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α.
  • HY-131305
    HBDDE

    		PKC Apoptosis Neurological Disease
    HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis.
  • HY-122958
    Peucedanocoumarin III

    		α-synuclein Neurological Disease
    Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research.
  • HY-113649
    AKB-6899

    		HIF/HIF Prolyl-Hydroxylase Cancer
    AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects.
  • HY-N1881
    4',5-Dihydroxyflavone

    		Lipoxygenase Glucosidase Others
    4',5-Dihydroxyflavone is a soybean LOX-1 and yeast α-Glucosidase inhibitor, with an Ki of 102.6 μM for soybean LOX-1 and an IC50 of 66 μM for yeast α-glucosidase. LOX-1 isshort for Lectin-like oxidized low-density lipoprotein receptor-1.
  • HY-14415
    SR8278

    		REV-ERB Metabolic Disease Neurological Disease
    SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease.
  • 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-14282
    Lanoconazole

    		Fungal Infection Inflammation/Immunology
    Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
  • HY-150687
    ZINC12409120

    		ERK Metabolic Disease
    ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM.
  • HY-100339
    GSK583

    		RIP kinase Endocrinology
    GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
  • HY-150738
    ODN 2088

    		Toll-like Receptor (TLR) Inflammation/Immunology
    ODN 2088 is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.
  • HY-B0223
    Albendazole

    SKF-62979

    		 Parasite Microtubule/Tubulin Autophagy Apoptosis Reactive Oxygen Species VEGFR HIF/HIF Prolyl-Hydroxylase Antibiotic Bacterial Cancer Infection
    Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells.
  • HY-N2022
    Castanospermine

    		Glucosidase Cancer
    Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).
  • HY-N8816
    Stipuleanoside R2

    		NF-κB Inflammation/Immunology
    Stipuleanoside R2 inhibits NF-κB activation stimulated by TNFα in a dose-dependent manner with IC50 value of 4.1 μM.
  • HY-N0604
    Ginsenoside Rh1

    Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1

    		 PPAR TNF Receptor Interleukin Related Endogenous Metabolite Inflammation/Immunology
    Ginsenoside Rh1 (Prosapogenin A2) inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β.
  • HY-135386
    5β-​Dutasteride

    		Drug Metabolite Inflammation/Immunology
    5β-Dutasteride is the S configuration of Dutasteride. 5β-Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.
  • HY-12495
    ISRIB (trans-isomer)

    		PERK Autophagy Apoptosis Neurological Disease
    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).
  • HY-N0358
    1,4-Dicaffeoylquinic acid

    1,4-DCQA

    		 TNF Receptor Interleukin Related Inflammation/Immunology
    1,4-Dicaffeoylquinic acid (1,4-DCQA) is a phenylpropanoid from Xanthii fructus, inhibits LPS-stimulated TNF-α production.
  • HY-139830
    Dyrk1A-IN-1

    		DYRK Neurological Disease
    Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.
  • HY-N1470
    Plantagoside

    		Others Metabolic Disease
    Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM.
  • HY-N10111
    Siegesbeckialide I

    		IKK Inflammation/Immunology
    Siegesbeckialide I most potently inhibits LPS-induced NO production in RAW264.7 murine macrophages by directly binding to IKKα/β.
  • HY-14649S2
    11-cis-Retinoic Acid-d5

    		RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    11-cis-Retinoic Acid-d5 is the deuterium labeled Retinoic acid. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[1][2].
  • HY-A0009S
    Galanthamine-d3 hydrobromide

    Galantamine-d3 (hydrobromide)

    		 Cholinesterase (ChE) nAChR Neurological Disease
    Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
  • HY-101144
    RSM-932A

    TCD-717

    		 Others Cancer
    RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles.
  • HY-N1425
    Tiliroside

    		Others Metabolic Disease
    Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2  μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract.
  • HY-15466
    Izorlisib

    CH5132799

    		 PI3K Cancer
    Izorlisib (CH5132799) is a selective class I PI3K inhibitor. Izorlisib inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
  • HY-129571
    BioE-1115

    		Ser/Thr Protease Casein Kinase Metabolic Disease
    BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM.
  • HY-12030
    PIK-90

    		PI3K DNA-PK Cancer
    PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
  • HY-13862
    AZD1080

    		GSK-3 Neurological Disease
    AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
  • HY-119424
    SP4206

    		Interleukin Related Inflammation/Immunology
    SP4206 is an IL-2/IL-2Rα interaction inhibitor. SP4206 binds with high affinity (Kd=70 nM) to IL-2 and blocks binding to its natural receptor IL-2Rα (Kd=10 nM).
  • HY-101755
    Tedatioxetine hydrobromide

    Lu AA24530 hydrobromide

    		 5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology
    Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist
    . ,
  • 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-32015
    Cot inhibitor-1

    		MAP3K Inflammation/Immunology
    Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
  • HY-10172
    IMD-0354

    IKK2 Inhibitor V

    		 IKK Cancer
    IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
  • HY-151129
    nAChR-IN-1

    2,2,6,6-Tetramethylpiperidin-4-yl heptanoate

    		 nAChR Neurological Disease
    nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research.
  • 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-136794
    SB-284851-BT

    		p38 MAPK Epigenetic Reader Domain Cancer Inflammation/Immunology
    SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET).
  • 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-102040
    Hispidol

    (Z)-Hispidol

    		 TNF Receptor Inflammation/Immunology
    Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.
  • HY-139307
    MG-2119

    		Tau Protein Neurological Disease
    MG-2119 is a potent monomeric tau and α-syn aggregation inhibitor. MG-2119 is a potential agent for neurological disorders research.
  • HY-111365
    TES-1025

    		Others Metabolic Disease
    TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM.
  • HY-15846
    CPI-203

    		Epigenetic Reader Domain Apoptosis Cancer
    CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).
  • HY-N0629
    Maslinic acid

    Crategolic acid; 2α-Hydroxyoleanolic acid

    		 NF-κB Bacterial HIV Endogenous Metabolite Inflammation/Immunology Cancer
    Maslinic acid can inhibit the DNA-binding activity of NF-κB p65 and abolish the phosphorylation of IκB-α, which is required for p65 activation.
  • HY-122464
    (±)-Jasmonic acid

    		Others Others
    (±)-Jasmonic acid is a plant growth regulator and a derivative of α-linolenic acid. (±)-Jasmonic acid decreases chlorophyll levels in green and etiolated barley leaf segments and inhibits elongation of rice seedlings.
  • HY-122858
    PKCiota-IN-2

    		PKC Cancer
    PKCiota-IN-2 is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively.
  • HY-12338
    ON 146040

    		PI3K Bcr-Abl Cancer
    ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
  • HY-15244A
    Alpelisib hydrochloride

    BYL-719 hydrochloride

    		 PI3K Cancer
    Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. Alpelisib hydrochloride (BYL-719 hydrochloride) shows antineoplastic activity.
  • HY-116830
    BRD0705

    		GSK-3 Cancer
    BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.
  • HY-15205
    Ganetespib

    STA-9090

    		 HSP Apoptosis Cancer
    Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3.
  • HY-107531
    A 1070722

    		GSK-3 Cancer
    A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.
  • HY-14649
    Retinoic acid

    Vitamin A acid; all-trans-Retinoic acid; ATRA

    		 RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
  • HY-126052
    Gnetol

    		COX Tyrosinase HDAC Cancer Metabolic Disease
    Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.
  • HY-P1847
    IKKγ NBD Inhibitory Peptide

    		NF-κB Cancer
    IKKγ NBD Inhibitory Peptide is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits.
  • HY-128598
    MD2-TLR4-IN-1

    		Toll-like Receptor (TLR) Cancer Inflammation/Immunology
    MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
  • HY-119940
    MC180295

    (rel)-MC180295

    		 CDK Cancer
    MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
  • HY-14649S3
    Retinoic acid-d6

    		RAR/RXR PPAR Autophagy Endogenous Metabolite Cancer
    Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
  • HY-119307
    Apratastat

    TMI-005

    		 MMP TNF Receptor Cancer
    Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC).
  • HY-N10835
    Gnetumontanin B

    		Others Inflammation/Immunology
    Gnetumontanin B is a stilbenoid that can be found in Gnetum montanum f. megalocarpum. Gnetumontanin B inhibits TNF-α production with an IC50 value of 1.49 µM.
  • HY-N10426
    (+)-Cembrene A

    		Glucosidase Metabolic Disease
    (+)-Cembrene A (Compound 5) is a α-glucosidase inhibitor with an IC50 of 30.31 μM. (+)-Cembrene A is nontoxic towards human normal hepatocyte (LO2) cells.
  • HY-N9315
    Episappanol

    		TNF Receptor Interleukin Related Inflammation/Immunology
    Episappanol is a natural compound isolated from Caesalpinia sappan heartwood with anti-inflammatory activity. Episappanol significantly inhibits the IL-6 and TNF-α secretion.
  • HY-111484A
    GDC-0927 Racemate

    SRN-927 Racemate

    		 Estrogen Receptor/ERR Cancer
    GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases.
  • HY-N6602
    α-Solanine

    		Apoptosis Cancer
    α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in Solanum nigrum, has been observed to inhibit growth and induce apoptosis in cancer cells.
  • HY-120215
    KT203

    		MAGL Metabolic Disease
    KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
  • HY-19776
    3α-Aminocholestane

    		Phosphatase Cancer
    3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
  • HY-129131
    Chrysin 6-C-arabinoside 8-C-glucoside

    		Glucosidase Metabolic Disease
    Chrysin 6-C-arabinoside 8-C-glucoside is a α±-glucosidase inhibitors which are widely used in the study for type 2 diabetes.
  • HY-120177
    KT182

    		MAGL Others
    KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
  • HY-13743
    Roquinimex

    Linomide; FCF89; ABR212616

    		 TNF Receptor Inflammation/Immunology
    Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.
  • HY-109040
    Quilseconazole

    VT-1129

    		 Fungal Cytochrome P450 Infection
    Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
  • HY-103267A
    S32826

    		Phosphodiesterase (PDE) Inflammation/Immunology
    S32826 is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 inhibits LPA release from adipocytes.
  • HY-16569
    Colchicine

    		Microtubule/Tubulin Autophagy Apoptosis Cancer
    Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs).
  • HY-13867A
    Bisindolylmaleimide I hydrochloride

    GF109203X hydrochloride; Go 6850 hydrochloride

    		 PKC GSK-3 Cancer Metabolic Disease
    Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor.
  • HY-13867
    Bisindolylmaleimide I

    GF109203X; Go 6850

    		 PKC GSK-3 Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor.
  • HY-12707
    Piribedil

    		Dopamine Receptor Adrenergic Receptor Histone Methyltransferase Cancer Endocrinology Neurological Disease
    Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.
  • HY-12707A
    Piribedil dihydrochloride

    		Adrenergic Receptor Dopamine Receptor Histone Methyltransferase Cancer Endocrinology Neurological Disease
    Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
  • HY-125838
    J30-8

    		JNK Neurological Disease
    J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases.
  • HY-153091
    BMY 14802

    		Adrenergic Receptor 5-HT Receptor Sigma Receptor Neurological Disease
    BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM.
  • HY-12707C
    Piribedil hydrochloride

    		Dopamine Receptor Adrenergic Receptor Histone Methyltransferase Cancer Endocrinology Neurological Disease
    Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
  • HY-14282A
    (Z)-Lanoconazole

    		Fungal Infection Inflammation/Immunology
    (Z)-Lanoconazole is the Z configuration of Lanoconazole. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
  • HY-120087
    KG-548

    		HIF/HIF Prolyl-Hydroxylase Cancer
    KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β.
  • HY-135590
    Raloxifene 4-Monomethyl Ether

    		Estrogen Receptor/ERR
    Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6.
  • HY-135584
    Raloxifene 6-Monomethyl Ether

    		Estrogen Receptor/ERR
    Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6.
  • HY-122857
    PKCiota-IN-1

    		PKC Cancer
    PKCiota-IN-1 (compound 51) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.7 nM. PKCiota-IN-1 also inhibits PKC-α and PKC-ε with IC50s of 45 nM and 450 nM, respectively.
  • HY-122858A
    PKCiota-IN-2 formic

    		PKC Cancer
    PKCiota-IN-2 formic is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 formic also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively.
  • HY-12085
    Apremilast

    CC-10004

    		 Phosphodiesterase (PDE) Apoptosis TNF Receptor Inflammation/Immunology
    Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-N0014
    Icariin

    Ieariline

    		 Phosphodiesterase (PDE) PPAR Autophagy Inflammation/Immunology Cardiovascular Disease Cancer
    Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
  • HY-111630
    PluriSIn #2

    		Topoisomerase Cancer
    PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs).
  • HY-11105
    Pilaralisib analogue

    XL147 analogue

    		 PI3K Apoptosis Cancer
    Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
  • HY-10215
    Luminespib

    VER-52296; AUY922; NVP-AUY922

    		 HSP Autophagy Apoptosis Cancer
    Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
  • HY-12869
    AZD-8835

    		PI3K Cancer
    AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
  • HY-117771
    DO34

    		Others Metabolic Disease
    DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.
  • HY-14316A
    Tebanicline dihydrochloride

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    		 nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
  • HY-13689
    Go 6983

    Gö 6983; Goe 6983

    		 PKC Cancer
    Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
  • HY-12340
    ETP-46321

    		PI3K Cancer
    ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
  • HY-12437
    BDP5290

    		ROCK Cancer
    BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
  • HY-W086896
    α-Demethylnaproxen

    		Drug Metabolite Inflammation/Immunology
    α-Demethylnaproxen is the major metabolite of Nabumetone (HY-B0559), Nabumetone is an orally active COX-2 inhibitor with anti-inflammatory activity.
  • HY-N7637
    Tubuloside B

    		Apoptosis Cancer
    Tubuloside B, one of the phenylethanoids isolated from the stems of Cistanche salsa, inhibits TNFα-induced apoptosis. Tubuloside B possesses antioxidative effects.
  • HY-B2006
    Fenvalerate

    		Phosphatase Bacterial Infection
    Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide.
  • HY-146066
    α7 nAchR-JAK2-STAT3 agonist 1

    		nAChR JAK STAT NO Synthase Inflammation/Immunology
    α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis.
  • HY-10255A
    Sunitinib

    SU 11248

    		 VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • 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-108642
    AMG-548

    		p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • HY-P0097A
    Nonapeptide-1 acetate salt

    Melanostatine-5 acetate salt

    		 Melanocortin Receptor Cancer Endocrinology Metabolic Disease
    Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.
  • HY-17412A
    Minocycline

    		Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53 Potassium Channel Calcium Channel Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
  • HY-B0193A
    Prazosin hydrochloride

    		Adrenergic Receptor Autophagy Cardiovascular Disease Endocrinology Cancer
    Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
  • HY-P0097
    Nonapeptide-1

    Melanostatine-5

    		 Melanocortin Receptor Cancer Endocrinology Metabolic Disease
    Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.
  • HY-18862
    PF-03715455

    		p38 MAPK Inflammation/Immunology
    PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease).
  • HY-101855
    Anle138b

    		Amyloid-β Neurological Disease
    Anle138b, an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Anle138b has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.
  • HY-17412
    Minocycline hydrochloride

    		Bacterial Antibiotic HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53 Potassium Channel Calcium Channel Cancer Infection Metabolic Disease Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
  • HY-P1847A
    IKKγ NBD Inhibitory Peptide TFA

    		NF-κB Inflammation/Immunology
    IKKγ NBD Inhibitory Peptide TFA is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide TFA acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide TFA could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits.
  • HY-101438
    Darbufelone

    CI-1004

    		 Prostaglandin Receptor Leukotriene Receptor Inflammation/Immunology Endocrinology
    Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM).
  • HY-145564A
    Emprumapimod hydrochloride

    PF-07265803 hydrochloride

    		 p38 MAPK Inflammation/Immunology Cardiovascular Disease
    Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK. Emprumapimod hydrochloride can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
  • HY-147045
    UCB-5307

    		TNF Receptor Inflammation/Immunology
    UCB-5307 is a potent TNF signaling inhibitor with a KD of 9 nM for human TNFα. UCB-5307 can penetrate the preformed hTNF/hTNFR1 complex.
  • HY-N2270
    Chicanine

    		p38 MAPK ERK IKK Inflammation/Immunology
    Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity.
  • HY-150601
    Estrogen receptor-IN-1

    		Estrogen Receptor/ERR Metabolic Disease
    Estrogen receptor-IN-1 (compound 16) is a potent estrogen receptor (ER) inhibitor with IC50s of 13, 5µM for ERα and Erβ, respectively.
  • HY-13469
    Debio 0932

    CUDC-305

    		 HSP Cancer
    Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively.
  • HY-106523
    Nipradolol

    KT 210; K 351; Hypadil

    		 Adrenergic Receptor Cardiovascular Disease
    Nipradolol (KT-210; K-351) is a potent blocker of alpha-1-adrenergic receptors. Nipradolol inhibits the increase of intraocular pressure (IOP) in an albino rabbit model induced by Phenylephrine (HY-B0769). Nipradolo suppresses the noradrenaline (NA)-induced muscles contraction, also exhibits vasodilator activity on the dog coronary artery.
  • HY-145275
    EB-0176

    		Glucosidase Infection
    EB-0176 is a potent inhibitor of ER α-glucosidases (α-Glu) Iand II with IC50s of 0.6439 and 0.0011 μM, respectively. EB-0176 is a N-substituted derivative of valiolamine with broad-spectrum antiviral. EB-0176 has the potential for the reseach of broad-spectrum agent against the existing and emerging viruses.
  • HY-12987S1
    Pimozide-d5 N-Oxide

    		Dopamine Receptor Adrenergic Receptor STAT Cancer Neurological Disease Endocrinology
    Pimozide-d5 N-Oxide is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2].
  • HY-12987S
    Pimozide-d4

    R6238-d4

    		 Dopamine Receptor Adrenergic Receptor STAT Cancer Endocrinology Neurological Disease
    Pimozide-d4 is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3].
  • HY-110248
    MI 14

    		PI4K HCV Infection
    MI 14 is a selective PI4KIIIβ inhibitor with IC50s of 54 nM, >100 μM, >100 μM for PI4KIIIβ, PI4KIIIα, PI4KIIα, respectively. MI 14 has antiviral activity against HCV 1b, CVB3, HRVM, HVC 2a.
  • HY-145273
    EB-0150

    		Glucosidase Infection
    EB-0150 is a potent inhibitor of ER α-glucosidases (α-Glu) Iand II with IC50s of 0.73 and 0.0337 μM, respectively. EB-0150 is a N-substituted derivative of valiolamine with broad-spectrum antiviral. EB-0150 has the potential for the reseach of broad-spectrum agent against the existing and emerging viruses.
  • HY-N1987
    Cucurbitacin IIb

    		Apoptosis Inflammation/Immunology
    Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
  • HY-144307
    Aurora A/PKC-IN-1

    		Aurora Kinase PKC Cancer
    Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity.
  • HY-P3567
    (p-Iodo-Phe7)-ACTH (4-10)

    		Melanocortin Receptor Neurological Disease
    (p-Iodo-Phe7)-ACTH (4-10) is a adrenocorticotrophic hormone (ACTH) derivative, which is produced and secreted by the anterior pituitary gland. (p-Iodo-Phe7)-ACTH (4-10) serves as a melanocortin (MC) receptor antagonist and inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats.
  • HY-100886
    BAY1082439

    		PI3K Apoptosis Cancer
    BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
  • HY-32018
    Cot inhibitor-2

    		MAP3K Cancer
    Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
  • HY-101438A
    Darbufelone mesylate

    CI-1004 mesylate

    		 Prostaglandin Receptor Leukotriene Receptor Inflammation/Immunology Endocrinology
    Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
  • HY-103267
    S32826 disodium

    		Phosphodiesterase (PDE) Inflammation/Immunology
    S32826 disodium is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 disodium shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 disodium inhibits LPA release from adipocytes.
  • HY-10255
    Sunitinib Malate

    SU 11248 Malate

    		 PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-120877
    MRT199665

    		Salt-inducible Kinase (SIK) AMPK Apoptosis Cancer
    MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
  • HY-136393
    IKK-IN-4

    		IKK Inflammation/Immunology
    IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively.
  • HY-10527
    Telatinib

    Bay 57-9352

    		 c-Kit PDGFR VEGFR Cancer
    Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
  • HY-148231
    Dideoxy-amanitin

    		DNA/RNA Synthesis ADC Cytotoxin Cancer
    Dideoxy-amanitin (compound 2), an α-Amanitin (HY-19610) derivative, is a potent and selective RNA polymerase II allosteric inhibitor with an IC50 value of 74.2 nM.
  • HY-10402
    Losmapimod

    GSK-AHAB; GW856553X; SB856553

    		 p38 MAPK Autophagy Inflammation/Immunology Cancer
    Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
  • HY-12299
    WH-4-023

    Dual LCK/SRC inhibitor

    		 Src Cancer
    WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
  • HY-145330
    NSC639828

    		DNA/RNA Synthesis Cancer
    NSC639828 is a potent inhibitor of DNA polymerase α with an IC50 of 70 μM. NSC639828 has high antitumor activity. NSC639828 has the potential for researching cancer disease.
  • HY-N2989
    3-O-Acetyl-16α-hydroxydehydrotrametenolic acid

    		NO Synthase Inflammation/Immunology
    3-O-Acetyl-16α-hydroxydehydrotrametenolic acid, an anti-inflammatory triterpenoid, inhibits NO production and iNOS expression in LPS-stimulated Raw264.7 cells.
  • HY-103030
    PI3K-IN-32

    		PI3K Cancer
    PI3K-IN-32 (compound 35) is a potent PI3K p110α inhibitor with an pIC50 of 6.85.
  • HY-N1200
    Stigmasterol glucoside

    		5 alpha Reductase Inflammation/Immunology
    Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities, act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM.
  • HY-19708
    KIRA6

    		IRE1 Cancer Metabolic Disease Inflammation/Immunology
    KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM. KIRA6 can trigger an apoptotic response.
  • HY-117761
    MHY908

    		PPAR Cancer Metabolic Disease
    MHY908 is a potent dual agonist of PPARα and PPARγ. MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity.
  • HY-129121
    ML-​226

    		MAGL Neurological Disease
    ML226 is a potent α/β hydrolase domain-containing protein 11 (ABHD11) inhibitor in vitro and in situ with IC50s of 15 and 0.68 nM, respectively.
  • HY-100315
    Tyrosine kinase-IN-1

    		VEGFR PDGFR FGFR Cardiovascular Disease
    Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
  • HY-145274
    EB-0156

    		Glucosidase Infection
    EB-0156 is a potent inhibitor of ER α-glucosidases (α-Glu) Iand II with IC50s of 0.0479 and less than 0.001 μM, respectively. EB-0156 is a N-substituted derivative of valiolamine with broad-spectrum antiviral. EB-0156 has the potential for the reseach of broad-spectrum agent against the existing and emerging viruses.
  • HY-16903
    PKC-IN-1

    		PKC Inflammation/Immunology
    PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
  • HY-12987S2
    Pimozide-d4-1

    R6238-d4-1

    		 Dopamine Receptor Adrenergic Receptor STAT Parasite Cancer Endocrinology Neurological Disease
    Pimozide-d4-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2][3][4].
  • HY-44809A
    Izilendustat hydrochloride

    		HIF/HIF Prolyl-Hydroxylase Cancer Inflammation/Immunology
    Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1).
  • HY-120793
    CMC2.24

    TRB-N0224

    		 Ras Apoptosis MMP Cancer Inflammation/Immunology
    CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis.
  • HY-108642B
    AMG-548 dihydrochloride

    		p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • HY-108642A
    AMG-548 hydrochloride

    		p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
  • HY-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    		 IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-16187
    EL-102

    		HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer.
  • HY-147562
    ALPK1-IN-2

    		NF-κB Cancer Inflammation/Immunology
    ALPK1-IN-2 (compound T001) is a potent ALPK1 (alpha-kinase 1) inhibitor, with an IC50 of 95 nM. ALPK1-IN-2 also inhibits NF-κB, with an IC50 of 1.31 μM.
  • HY-10320
    Doramapimod

    BIRB 796

    		 p38 MAPK Raf Autophagy Inflammation/Immunology Cancer
    Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.
  • HY-143237
    ATX inhibitor 11

    		Phosphodiesterase (PDE) Others
    ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research.
  • HY-10255AS
    Sunitinib-d10

    SU 11248-d10

    		 VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
  • HY-N10606
    Uvagrandol

    		Glucosidase Metabolic Disease
    Uvagrandol potently inhibits α-glucosidase and porcine lipase (IC50: 15.2 μM, 11.2 μM respectively). Uvagrandol can be used in the research of Type 2 diabetes and obesity.
  • HY-12774
    IC261

    		Casein Kinase Apoptosis Cancer
    IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
  • HY-13514
    TG 100713

    		PI3K Cancer
    TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively.
  • HY-10527C
    Telatinib mesylate

    Bay 57-9352 mesylate

    		 VEGFR PDGFR c-Kit Cancer
    Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.
  • HY-124646
    KIRA-7

    		IRE1 Inflammation/Immunology
    KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect.
  • HY-N0907
    Ginsenoside Rg6

    		NF-κB Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
  • HY-13493
    AC710

    		PDGFR c-Kit FLT3 Cancer
    AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
  • HY-144697
    p38 MAPK-IN-3

    		p38 MAPK Apoptosis Reactive Oxygen Species Cancer
    p38 MAPK-IN-3 (Compound 2c) is a p38α MAPK inhibitor. p38 MAPK-IN-3 has antitumor activities and induces apoptosis and ROS.
  • HY-N10969
    (+)-5,7,4'-Trimethoxyafzelechin

    		Others Others
    (+)-5,7,4'-Trimethoxyafzelechin is a derivative of (+)-Afzelechin HY-N2821. (+)-Afzelechin is an α-glucosidase activity inhibitor. (+)-Afzelechin can be isolated from rhizomes of Bergenia ligulata.
  • HY-P2203A
    SAHM1 TFA

    		Notch
    SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.
  • HY-102076
    0990CL

    		Others Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP.
  • 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-N1949
    Homoplantaginin

    		TNF Receptor NF-κB Inflammation/Immunology
    Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
  • HY-107500
    UVI 3003

    		RAR/RXR Autophagy Others
    UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
  • HY-13493A
    AC710 Mesylate

    		PDGFR Cancer
    AC710 Mesylate is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
  • HY-15174
    Dactolisib Tosylate

    BEZ235 Tosylate; NVP-BEZ 235 Tosylate

    		 PI3K mTOR Autophagy Cancer
    Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
  • HY-150073
    DS01080522

    		Others Cancer
    DS01080522 is a Protein Kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor. DS01080522 inhibits PRKACA kinase activity and CREB phosphorylation with IC50s of 0.8 nM and 66 nM, respectively. DS01080522 can be used for the research of cancer.
  • HY-70013
    Abiraterone

    CB-7598

    		 Cytochrome P450 Cancer
    Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
  • HY-113342
    7-Ketocholesterol

    		Endogenous Metabolite Metabolic Disease
    7-Ketocholesterol, toxic oxysterol, inhibits the rate-limiting step in bile acid biosynthesis cholesterol 7 alpha-hydroxylase, as well as strongly inhibiting HMG-CoA reductase (the rate-limiting enzyme in cholesterol biosynthesis). 7-Ketocholesterol induces cell apoptosis.
  • HY-12046
    PIK-93

    		PI4K PI3K Virus Protease Cancer
    PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
  • HY-12085S
    Apremilast-d5

    CC-10004-d5

    		 Phosphodiesterase (PDE) TNF Receptor Apoptosis Inflammation/Immunology
    Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
  • HY-10683
    PKI-402

    		PI3K mTOR Cancer
    PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
  • HY-116830A
    (Rac)-BRD0705

    		GSK-3 Cancer
    (Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
  • HY-103457
    Y134

    		Estrogen Receptor/ERR Cancer
    Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.
  • HY-44809
    Izilendustat

    		HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Cardiovascular Disease
    Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1).
  • HY-151966
    TD1092

    		PROTACs IAP Caspase Cancer
    TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells Apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research.
  • HY-13982
    JSH-23

    		NF-κB Cancer Metabolic Disease Inflammation/Immunology
    JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
  • HY-W015445
    SD-169

    		p38 MAPK Metabolic Disease
    SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
  • HY-N6575
    7β-Hydroxybufalin

    		Glucosidase Cholinesterase (ChE) Metabolic Disease
    7β-Hydroxybufalin is a bufadienolide. 7β-Hydroxybufalin can be isolated from the venom of Bufo bufo gargarizans. 7β-Hydroxybufalin inhibits α-glucosidase and acetylcholinesterase.
  • HY-N7095
    Ceftezole

    CTZ

    		 Bacterial Antibiotic Infection
    Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
  • HY-100207
    CP21R7

    CP21

    		 GSK-3 Cancer
    CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
  • HY-15356
    BIO-acetoxime

    BIA

    		 GSK-3 Apoptosis HSV Infection Inflammation/Immunology Neurological Disease
    BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.
  • HY-N7096
    Ceftezole sodium

    CTZ sodium

    		 Bacterial Antibiotic Infection
    Ceftezole sodium (CTZ sodium) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole sodium (CTZ sodium) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
  • HY-118388
    AS604872

    		Prostaglandin Receptor Endocrinology
    AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour.
  • HY-146128
    Anti-hyperglycemic agent-1

    		Glucosidase Metabolic Disease
    Anti-hyperglycemic agent-1 (compound 10) is a potent α-Glucosidase inhibitor, with an IC50 of 0.53 μM. Anti-hyperglycemic agent-1 can be used for diabetes research.
  • HY-B0089
    Acarbose

    BAY g 5421

    		 Glucosidase Metabolic Disease
    Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin.
  • HY-N4095
    Brevifolincarboxylic acid

    		Aryl Hydrocarbon Receptor Glucosidase Metabolic Disease Inflammation/Immunology
    Brevifolincarboxylic acid is extracted from Polygonum capitatum, has inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarboxylic acid is an α-glucosidase inhibitor with an IC50 of 323.46 μM.
  • HY-124876
    SynuClean-D

    SC-D

    		 α-synuclein Neurological Disease
    SynuClean-D (SC-D) is an inhibitor of α-synuclein aggregation, disrupts mature amyloid fibrils, prevents fibril propagation, and abolishes the degeneration of dopaminergic neurons in an animal model of Parkinson’s disease.
  • HY-119248
    KRP-297

    MK-0767

    		 PPAR Metabolic Disease
    KRP-297 is a PPARα and PPARγ agonist potentially for the treatment of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver.
  • HY-14305A
    BMS-582949 hydrochloride

    		p38 MAPK Autophagy Inflammation/Immunology
    BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.
  • HY-139412
    Gilmelisib

    		PI3K Cancer
    Gilmelisib is an antineoplastic. Gilmelisib is a PI3K inhibitor (IC50 <1 nM for PI3K p110α) extracted from WO2017101847 A1, compound 1.
  • HY-10342
    Enzastaurin

    LY317615

    		 PKC Autophagy Apoptosis Cancer
    Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
  • HY-136392
    IKK-IN-3

    		IKK Inflammation/Immunology
    IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively.
  • HY-13812
    QNZ

    EVP4593

    		 NF-κB TNF Receptor Inflammation/Immunology Neurological Disease
    QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel.
  • HY-10255AS1
    Sunitinib-d4

    		VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
  • HY-112389
    p38 MAP Kinase Inhibitor III

    		p38 MAPK Inflammation/Immunology
    p38 MAP Kinase Inhibitor III (compound 7h) is a p38 MAPK inhibitor with an 50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with 50 values of 0.37 μM and 0.044 μM, respectively.
  • HY-A0077S1
    Perphenazine-d4

    		Histamine Receptor Dopamine Receptor Autophagy Apoptosis Adrenergic Receptor 5-HT Receptor Neurological Disease Endocrinology
    Perphenazine-d4 is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
  • HY-107589A
    BIO5192 hydrate

    		Integrin Inflammation/Immunology
    BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
  • HY-116830B
    BRD5648

    (R)-BRD0705

    		 GSK-3 Cancer
    BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
  • HY-107589
    BIO5192

    		Integrin Inflammation/Immunology
    BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
  • HY-15244
    Alpelisib

    BYL-719

    		 PI3K Cancer
    Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
  • HY-123938
    Risovalisib

    CYH33

    		 PI3K Cancer
    Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors.
  • HY-P2657
    Verucopeptin

    		HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite Cancer
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
  • HY-P0154
    Epsilon-V1-2

    ε-V1-2; EAVSLKPT

    		 PKC Inflammation/Immunology
    Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
  • HY-16569S
    Colchicine-d6

    		Microtubule/Tubulin Autophagy Apoptosis Cancer
    Colchicine-d6 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].
  • HY-16569S1
    Colchicine-d3

    		Microtubule/Tubulin Autophagy Apoptosis Cancer
    Colchicine-d3 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].
  • HY-100544
    FLLL32

    		STAT JAK Apoptosis Cancer
    FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
  • HY-148043
    Schnurri-3 inhibitor-1

    		Others Others
    Schnurri-3 inhibitor-1 is a potent schnurri-3 inhibitor which is an essential regulator of adult bone formation. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL with an AC50 value of 2.09 μM. Schnurri-3 inhibitor-1 can be used to research osteoporosis.
  • HY-100398
    PF-04979064

    		PI3K mTOR Cancer
    PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
  • HY-W067427
    BAY32-5915

    		IKK Cancer
    BAY32-5915 is a potent IKKα inhibitor with an IC50 value of 60 nM. BAY32-5915 has not affect Doxorubicin (HY-15142A)-induced NF-κB activation.
  • HY-P0224
    N-Formyl-Met-Leu-Phe

    fMLP; N-Formyl-MLF

    		 TNF Receptor Inflammation/Immunology
    N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
  • HY-135307
    SSF-109

    Huanjunzuo

    		 Fungal Infection
    SSF-109 is a broad-spectrum fungicide which has protective activity against plant disease. SSF-109 inhibits the biosynthesis of ergosterol at the 14α-demethylation step in Botrytis cinerea.
  • HY-15190
    NVP-HSP990

    HSP-990

    		 HSP Apoptosis Cancer
    NVP-HSP990 is a potent, selective and orally active Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
  • HY-151440
    Antifungal agent 42

    		Fungal Infection
    Antifungal agent 42 is an antifungal agent. Antifungal agent 42 has an inhibitory effect on lanosterol 14α-demethylase (CYP51) of C.alb.. Antifungal agent 42 inhibits biofilm formation.
  • HY-103245
    Cl-4AS-1

    		Androgen Receptor Cancer
    Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively).
  • HY-19498
    WAY-204688

    SIM-688

    		 NF-κB Inflammation/Immunology
    WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.
  • HY-100779
    Rimacalib

    SMP 114

    		 CaMK Autophagy Metabolic Disease
    Rimacalib (SMP 114) is a Ca 2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
  • HY-N0042
    Ginsenoside Rc

    Panaxoside Rc

    		 GABA Receptor TNF Receptor Interleukin Related Cancer Inflammation/Immunology Neurological Disease
    Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
  • HY-126414
    Methylenedihydrotanshinquinone

    		Others Inflammation/Immunology
    Methylenedihydrotanshinquinone is a natural product that can be isolated from the dried root of S. miltiorrhiza. Methylenedihydrotanshinquinone has anti-inflammatory effect by inhibiting expression of TNF-α, IL-1β, and IL-8.
  • HY-121750
    CCG-222740

    		Ras ROCK Cancer
    CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
  • HY-15271
    WYE-687

    		mTOR PI3K Cancer
    WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
  • HY-N0191
    Andrographolide

    Andrographis

    		 NF-κB SARS-CoV Influenza Virus Autophagy Parasite Cancer Infection Inflammation/Immunology
    Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
  • HY-10620
    PI3K-IN-22

    		PI3K mTOR Cancer
    PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer.
  • HY-111379
    EHT 5372

    		DYRK CDK GSK-3 Cancer Metabolic Disease Neurological Disease
    EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively.
  • HY-A0077
    Perphenazine

    		Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy Cancer Endocrinology Inflammation/Immunology Neurological Disease
    Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.
  • HY-136055
    (S,R,S)-AHPC-C5-COOH

    VH032-C5-COOH

    		 E3 Ligase Ligand-Linker Conjugates HIF/HIF Prolyl-Hydroxylase Cancer
    (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
  • HY-11068
    SB 239063

    		p38 MAPK Autophagy Inflammation/Immunology
    SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.
  • HY-19357
    E3330

    APX-3330

    		 DNA/RNA Synthesis NF-κB AP-1 HIF/HIF Prolyl-Hydroxylase VEGFR Reactive Oxygen Species Cancer Neurological Disease Cardiovascular Disease
    E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities.
  • HY-110282
    S3QEL-2

    		Mitochondrial Metabolism Metabolic Disease
    S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation.
  • HY-100936
    Etazolate hydrochloride

    SQ 20009; EHT 0202 hydrochloride

    		 Phosphodiesterase (PDE) GABA Receptor Inflammation/Immunology Neurological Disease
    Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
  • HY-B0135A
    Furosemide sodium

    		NKCC GABA Receptor Cancer Metabolic Disease
    Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
  • HY-B0135
    Furosemide

    		NKCC GABA Receptor Metabolic Disease Cancer
    Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
  • HY-A0077A
    Perphenazine dihydrochloride

    		Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy Cancer Endocrinology Inflammation/Immunology Neurological Disease
    Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation.
  • HY-B0683S
    Limaprost-d3

    		PGE synthase Inflammation/Immunology Cardiovascular Disease
    Limaprost-d3 (17α,20-dimethyl-δ2-PGE1-d3) is the deuterium labeled Limaprost. Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost pain relief, has antianginal effects, and can be used for ischaemic symptoms research[1][2].
  • HY-N1120
    Triptoquinone B

    (+)-Triptoquinone B

    		 Interleukin Related Inflammation/Immunology
    Triptoquinone B ((+)-Triptoquinone B), a sesquiterpene alkaloid, is an interleukin-1 inhibitor. Triptoquinone B shows potent inhibitory activities against interleukin 1α and β releases for human peripheral mononuclear cells.
  • HY-N2110
    Phellopterin

    		Akt Inflammation/Immunology
    Phellopterin is a natural product isolated from Angelica dahurica. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
  • HY-N0906
    Ginsenoside Rk3

    		NF-κB Inflammation/Immunology Cardiovascular Disease
    Ginsenoside Rk3 is present in the roots Panax ginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells.
  • HY-139202
    XVA143

    		Integrin Inflammation/Immunology
    XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo.
  • HY-122464S1
    Jasmonic acid-d5

    		Isotope-Labeled Compounds Others
    Jasmonic acid-d5 is deuterium labeled (±)-Jasmonic acid. (±)-Jasmonic acid is a plant growth regulator and a derivative of α-linolenic acid. (±)-Jasmonic acid decreases chlorophyll levels in green and etiolated barley leaf segments and inhibits elongation of rice seedlings.
  • HY-N3431
    Kaempferol-7-O-rhamnoside

    		Glucosidase Metabolic Disease
    Kaempferol-7-O-rhamnoside, isolated from Chimonanthus nitens Oliv. Leaves, is a potent α-glucosidase activity inhibitor. Kaempferol-7-O-rhamnoside has the potential for diabetes.
  • HY-13223
    Crenolanib

    CP-868596

    		 FLT3 PDGFR Autophagy Cancer
    Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
  • HY-12837
    EN460

    		Others Others
    EN460 is a selective endoplasmic reticulum oxidation 1 (ERO1) inhibitor. EN460 (IC50 of 1.9 μM) interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation.
  • HY-124722
    OHM1

    		HIF/HIF Prolyl-Hydroxylase Cancer
    OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM.
  • HY-B0089A
    Acarbose sulfate

    Bay-g 5421 sulfate

    		 Glucosidase Metabolic Disease
    Acarbose (BAY g 5421) sulfate, antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose sulfate can potentiate the hypoglycemic effects of sulfonylureas or insulin.
  • HY-N8517
    Malabaricone B

    		Glucosidase Apoptosis Cancer Infection Metabolic Disease
    Malabaricone B, a naturally occurring plant phenolic, is an orally active α-glucosidase inhibitor with an IC50 of 63.7 µM. Malabaricone B has anticancer, antimicrobial, anti-oxidation and antidiabetic activities.
  • HY-122464S2
    (±)-Jasmonic acid-d5

    		Isotope-Labeled Compounds Others
    (±)-Jasmonic acid-d5 is the deuterium labeled (±)-Jasmonic acid. (±)-Jasmonic acid is a plant growth regulator and a derivative of α-linolenic acid. (±)-Jasmonic acid decreases chlorophyll levels in green and etiolated barley leaf segments and inhibits elongation of rice seedlings.
  • HY-P1420
    TAT-cyclo-CLLFVY

    		HIF/HIF Prolyl-Hydroxylase Cancer
    TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
  • HY-150740
    ODN 21595

    		Toll-like Receptor (TLR) Inflammation/Immunology
    ODN 21595 is a Guanine-Modified TLR7 and TLR9 inhibitor. ODN 21595 inhibits the release of IFN-α and IL-6 with no cytotoxic. ODN 21595 reduces the expression of CD86 and HLA-DR. ODN 21595 has the potential for the research of systemic lupus erythematosus (SLE).
  • HY-N2350
    Cynaropicrin

    		MMP NF-κB TNF Receptor Cancer
    Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
  • HY-123938A
    CYH33 methanesulfonate

    		PI3K Cancer
    CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors.
  • HY-N1940
    β-Anhydroicaritin

    		Interleukin Related TNF Receptor MMP Inflammation/Immunology
    β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
  • HY-B2006S
    Fenvalerate-d5

    		Phosphatase Bacterial Infection
    Fenvalerate-d5 is the deuterium labeled Fenvalerate. Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide[1].
  • HY-122521
    Sootepin D

    		NF-κB Inflammation/Immunology
    Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity.
  • HY-108647
    EO 1428

    		p38 MAPK Inflammation/Immunology
    EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation.
  • HY-10721
    PF-AKT400

    AKT protein kinase inhibitor

    		 Akt Cancer
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  • HY-50094
    Pictilisib

    GDC-0941

    		 PI3K Autophagy Apoptosis Cancer
    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
  • HY-P1453
    CMD178

    		STAT Cancer
    CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits Treg cell development.
  • HY-12036
    GSK1059615

    		PI3K mTOR Apoptosis Cancer
    GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
  • HY-P1872
    OV-1, sheep

    		Bacterial Infection
    OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa.
  • HY-148711
    STL1267

    		REV-ERB Cancer Metabolic Disease Inflammation/Immunology
    STL1267 is a potent and cross-the-blood-brain barrier REV-ERB agonist with a Ki value of 0.16 µM for REV-ERBα. STL1267 shows no cytotoxicity. STL1267 inhibits the gene expression of BMAL1.
  • HY-135808
    BIZ 114

    		NF-κB Inflammation/Immunology
    BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases.
  • HY-N0722
    Neochlorogenic acid

    trans-5-O-Caffeoylquinic acid

    		 NF-κB Interleukin Related TNF Receptor COX Inflammation/Immunology Cancer
    Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
  • HY-107588
    TC-I 15

    		Integrin Cardiovascular Disease
    TC-I 15 (TC-I-15) is an allosteric, collagen-binding integrin α2β1 inhibitor with IC50 values of 26.8 μM and 0.4 μM for GFOGER and GLOGEN, respectively. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition.
  • HY-17514
    Itraconazole

    R51211

    		 Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Bacterial Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
  • HY-P1453A
    CMD178 TFA

    		STAT Cancer
    CMD178 TFA is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits Treg cell development.
  • HY-N6073
    Soyasapogenol A

    		Apoptosis Inflammation/Immunology
    Soyasapogenol A, a triterpene compound, isolated from soybean. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model.
  • HY-15506
    TAK-593

    		PDGFR VEGFR Cancer
    TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
  • HY-107550
    HDAC6-IN-7

    		HDAC Cancer
    TCS HDAC6 20b is a HDAC6-selective inhibitor. TCS HDAC6 20b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells.
  • HY-115528
    FF-10502

    		Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Cancer
    FF-10502, a structural analog of Gemcitabine, is a pyrimidine nucleoside antimetabolite. FF-10502 inhibits DNA polymerase α and β. FF-10502 shows beneficial anticancer activity via a mechanism of action on dormant cells.
  • HY-139486
    AM-8123

    		Apelin Receptor (APJ) Cardiovascular Disease
    AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.
  • HY-10291
    Tarenflurbil

    (R)-Flurbiprofen; MPC7869

    		 RAR/RXR Autophagy Inflammation/Immunology Neurological Disease
    Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [ 3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.
  • HY-139553
    Zunsemetinib

    ATI-450; CDD-450

    		 MAPKAPK2 (MK2) Inflammation/Immunology
    Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.
  • HY-13049
    Cediranib maleate

    AZD-2171 maleate

    		 VEGFR Autophagy PDGFR Cancer
    Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-N2821
    (+)-Afzelechin

    		Glucosidase Metabolic Disease
    (+)-Afzelechin, isolated from rhizomes of Bergenia ligulata, is an alpha-glucosidase activity inhibitor with an ID50 (50% inhibition dose) value of 0.13 mM. (+)-Afzelechin can delay the absorption of carbohydrates in food to suppress postprandial hyperglycemia and hyperinsulinemia.
  • HY-70013S
    Abiraterone-D4

    CB-7598-d4

    		 Cytochrome P450 Cancer
    Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
  • HY-N3421
    Koaburaside

    		Interleukin Related TNF Receptor Influenza Virus Cancer Infection Inflammation/Immunology
    Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase.
  • HY-N6084
    Humulone

    α-Lupulic acid

    		 COX GABA Receptor Apoptosis Cardiovascular Disease
    Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.
  • HY-108847
    Etanercept

    		TNF Receptor Bacterial Inflammation/Immunology Cancer
    Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
  • HY-107597
    SU3327

    		JNK Metabolic Disease Inflammation/Immunology
    SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.
  • HY-103489
    PI-273

    		PI4K Apoptosis Cancer
    PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
  • HY-P1420A
    TAT-cyclo-CLLFVY TFA

    		HIF/HIF Prolyl-Hydroxylase Cancer
    TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
  • HY-100211
    TAPI-2

    TNF Protease Inhibitor 2

    		 MMP SARS-CoV Cancer
    TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.
  • HY-17406S
    Tolcapone D7

    Ro 40-7592 d7

    		 COMT Amyloid-β Neurological Disease
    Tolcapone-d7 is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells[1][2].
  • HY-148757
    TIM-063

    		CaMK Metabolic Disease
    TIM-063 is a selective and cell-permeable CaMKK inhibitor, ATP competitive inhibitor, can directly target the catalytic domain of CaMKK, with the Ki values of 0.35 μM and 0.2 μM for CaMKKα and CaMKKβ, respectively, the IC50 values are 0.63 μM and 0.96 μM, respectively.
  • HY-W010041
    Scyllo-Inositol

    		Amyloid-β Endogenous Metabolite Neurological Disease
    Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model.
  • HY-P1106
    K41498

    		CRFR Cardiovascular Disease
    K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study.
  • HY-131972
    PF-06843195

    		PI3K Cancer
    PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
  • 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-114263
    NXT629

    		PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
  • 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-12511
    SKF-86002

    		p38 MAPK Inflammation/Immunology
    SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
  • HY-108641
    SKF-86002 dihydrochloride

    		p38 MAPK Inflammation/Immunology
    SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
  • HY-114009
    AKR1C1-IN-1

    		Others Neurological Disease
    AKR1C1-IN-1 is a potent and selective inhibitor of human 20α-hydroxysteroid dehydrogenase (AKR1C1), with a Ki value of 4 nM for AKR1C1.
  • HY-N6722
    Swainsonine

    Tridolgosir

    		 Apoptosis Antibiotic Cancer Infection
    Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversible α-mannosidase inhibitor. Swainsonine induces apoptosis and cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity.
  • HY-10205
    Cediranib

    AZD2171

    		 VEGFR Autophagy PDGFR Cancer
    Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-N8593
    Undecane

    		TNF Receptor Infection
    Undecane has anti-allergic and anti-inflammatory activities on sensitized rat basophilic leukemia (RBL-2H3) mast cells and HaCaT keratinocytes. In sensitized mast cells, Undecane inhibits degranulation and the secretion of histamine and TNF-α[
  • HY-17044
    Duvelisib

    IPI-145; INK1197

    		 PI3K Cancer
    Duvelisib (IPI-145) is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
  • HY-100376
    CPI-1189

    		TNF Receptor Infection Neurological Disease
    CPI-1189 is a TNF-α release inhibitor with antioxidant and neuroprotective properties. CPI-1189 is used for researches of HIV-associated neurotoxicity and thus is a candidate for neuroprotective therapy in humans suffered from HIV-associated CNS disease.
  • HY-126114
    Lupeol acetate

    		COX Interleukin Related Inflammation/Immunology
    Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
  • HY-20180
    Pictilisib dimethanesulfonate

    GDC-0941 dimethanesulfonate; GDC-0941 2 MeSO3H salt

    		 PI3K Autophagy Apoptosis Cancer
    Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
  • HY-16782
    Pexmetinib

    ARRY-614

    		 p38 MAPK Autophagy Cancer
    Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
  • HY-15310
    Ivermectin

    MK-933

    		 Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • HY-15271A
    WYE-687 dihydrochloride

    		mTOR PI3K Cancer
    WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
  • HY-N7661
    4β-Hydroxywithanolide E

    		PPAR Metabolic Disease
    4β-Hydroxywithanolide E, isolated from Physalis peruviana L., inhibits adipocyte differentiation of 3T3-L1 cells through modulation of mitotic clonal expansion. 4β-Hydroxywithanolide E is an adipogenesis inhibitor and inhibits PPARγ, C/EBPα, and the adipocyte-specific molecule aP2 mRNA expression.
  • HY-146765
    AMS-17

    		NOD-like Receptor (NLR) Inflammation/Immunology Neurological Disease
    AMS-17 is a potent NLRP3 inhibitor, inhibiting microglia activation in vitro and in vivo. AMS-17 also inhibits cytokines such as caspase-1, TNF-α, IL-1β and inducible nitric oxide synthase (iNOS) in N9 cells. AMS-17 can be used for researching inflammation-associated neurological disorders.
  • HY-N0822
    Shikonin

    C.I. 75535; Isoarnebin 4

    		 Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2 Cancer
    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
  • HY-145564
    Emprumapimod

    PF-07265803

    		 p38 MAPK Inflammation/Immunology Cardiovascular Disease
    Emprumapimod (PF-07265803) is a potent, orally active and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain.
  • HY-B0006A
    Carvedilol phosphate hemihydrate

    BM 14190 phosphate hemihydrate

    		 Adrenergic Receptor Autophagy Bacterial Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 blocker. Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome.
  • HY-D0162
    Malachite green oxalate

    		IKK NF-κB Apoptosis Cancer
    Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.
  • HY-100950
    ABC1183

    		GSK-3 CDK Cancer Inflammation/Immunology
    ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.
  • HY-12047
    Ponatinib

    AP24534

    		 Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-N7377
    Butyl isobutyl phthalate

    		Glucosidase Metabolic Disease
    Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment.
  • HY-118091A
    Bexlosteride

    LY300502

    		 Others Cancer
    Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer.
  • HY-124036
    DS-7423

    		PI3K mTOR Cancer
    DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity.
  • HY-101457
    JZP-430

    		MAGL Metabolic Disease
    JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).
  • HY-117610A
    Bisindolylmaleimide XI hydrochloride

    Ro 32-0432; Ro 31-8830 hydrochloride

    		 PKC Inflammation/Immunology
    Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively.
  • HY-100608
    BMS453

    BMS-189453

    		 RAR/RXR Cancer
    BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
  • HY-B0135S
    Furosemide-d5

    		NKCC GABA Receptor Metabolic Disease Cancer
    Furosemide-d5 is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2[1]. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema[2].
  • HY-P1106A
    K41498 TFA

    		CFTR Cardiovascular Disease
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study.
  • HY-148561
    CDK8-IN-12

    		CDK GSK-3 PKC Cancer
    CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent.
  • HY-146440
    LSD1/ER-IN-1

    		Histone Demethylase Estrogen Receptor/ERR Apoptosis Cancer
    LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM.
  • HY-12688
    Succinyl phosphonate

    		Endogenous Metabolite Reactive Oxygen Species Neurological Disease
    Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-15509A
    Semapimod tetrahydrochloride

    CNI-1493; CPSI-2364 tetrahydrochloride

    		 TNF Receptor Interleukin Related p38 MAPK Inflammation/Immunology
    Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
  • HY-148837
    c-Myc inhibitor 7

    		c-Myc Casein Kinase Cancer Infection Cardiovascular Disease
    c-Myc inhibitor 7 is a c-Myc inhibitor and a multiple target protein degrader. c-Myc inhibitor 7 effective degrades c-MYC, CK1α, GSPT1 and IKZF1/2/3 proteins in a variety of tumor cells. c-Myc inhibitor 7 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection.
  • HY-13894
    Tyrphostin AG1296

    AG1296

    		 PDGFR c-Kit FLT3 Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
  • HY-B0032S
    Lurasidone-d8 hydrochloride

    SM-13496-d8 (hydrochloride)

    		 Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor Neurological Disease
    Lurasidone-d8 (hydrochloride) is the deuterium labeled Lurasidone, which is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C.
  • HY-126067
    (-)-Pinoresinol

    		Glucosidase Apoptosis Inflammation/Immunology
    (-)-Pinoresinol is a plant-derived tetrahydrofuran lignan that inhibits α-glucosidase and acts as a hypoglycemic agent. (-)-Pinoresinol has some anti-inflammatory effects and acts as a chemopreventive agent, inducing increased apoptosis and cell cycle G2/M arrest.
  • HY-131081
    γ-Amanitin

    		DNA/RNA Synthesis ADC Cytotoxin Cancer
    γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin.
  • HY-N0029
    Forsythoside B

    		TNF Receptor NF-κB Inflammation/Immunology
    Forsythoside B is a phenylethanoid glycoside isolated from Forsythia suspensa (Thunb.) Vahl, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
  • HY-124607
    (R)-BRD3731

    		GSK-3 Neurological Disease
    (R)-BRD3731 is a GSK3 inhibitor extracted from patent US20160375006A1, compound example 273, has IC50s of 1.05 and 6.7 μM for GSK3β and GSK3α, respectively.
  • HY-126125
    CHIR-98023

    		GSK-3 Metabolic Disease Neurological Disease
    CHIR-98023 is a potent, selective and reversible inhibitor of GSK3, with IC50s of 10 nM and 6.7 nM for GSK3α and GSK3β, respectively. CHIR-98023 can improve insulin action and glucose metabolism.
  • HY-14860A
    1-Deoxynojirimycin hydrochloride

    Duvoglustat hydrochloride

    		 Glucosidase PI3K Bacterial Antibiotic Infection Metabolic Disease
    1-Deoxynojirimycin hydrochloride (Duvoglustat hydrochloride) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin hydrochloride suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin hydrochloride possesses antihyperglycemic, anti-obesity, and antiviral features.
  • HY-14860
    1-Deoxynojirimycin

    Duvoglustat

    		 Glucosidase PI3K Metabolic Disease
    1-Deoxynojirimycin (Duvoglustat) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin possesses antihyperglycemic, anti-obesity, and antiviral features.
  • HY-101146
    SF2523

    		PI3K Epigenetic Reader Domain DNA-PK Cancer
    SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
  • HY-B1494
    Picrotoxinin

    		Chloride Channel GABA Receptor Neurological Disease
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
  • HY-150505
    DC-U4106

    		Deubiquitinase Apoptosis Cancer
    DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer.
  • HY-17406
    Tolcapone

    Ro 40-7592

    		 COMT Amyloid-β Apoptosis Cancer Neurological Disease
    Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma.
  • HY-B1423
    Lobeline

    α-Lobeline; L-Lobeline

    		 nAChR Dopamine Transporter Neurological Disease
    Lobeline (α-Lobeline; L-Lobeline), a lipophilic alkaloidal, is a nicotinic receptor agonist. Lobeline inhibits d-methamphetamine self-administration with no dopaminergic toxicity. Lobeline rescues d-amphetamine abuse induced addictive effect. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage.
  • HY-B0006
    Carvedilol

    BM 14190

    		 Adrenergic Receptor Autophagy Bacterial Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol (BM 14190) is a non-selective β/α-1 blocker. 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. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
  • HY-108355
    R59949

    		PKC Cancer
    R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
  • HY-108264
    TCS 21311

    NIBR3049

    		 JAK PKC GSK-3 Cancer
    TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
  • HY-15785
    Pimitespib

    TAS-116

    		 HSP Cancer
    Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. Pimitespib demonstrates less ocular toxicity.
  • HY-132299
    PI3Kγ inhibitor 4

    		PI3K Inflammation/Immunology
    PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation.
  • HY-12688A
    Succinyl phosphonate trisodium salt

    		Endogenous Metabolite Reactive Oxygen Species Cancer Metabolic Disease Neurological Disease
    Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
  • HY-17514S2
    Itraconazole-d9

    R51211-d9

    		 Fungal Hedgehog Bacterial Autophagy Cytochrome P450 Antibiotic
    Itraconazole-d9 is the deuterium labeled Itraconazole[1]. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor[2][3][4][5].
  • HY-146200
    PI3K/mTOR Inhibitor-8

    		PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cells apoptosis and arrests cell cycle at the G1/S phase.
  • HY-70063
    Buparlisib

    BKM120; NVP-BKM120

    		 PI3K Apoptosis Cancer
    Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
  • HY-19822
    Elacestrant

    RAD1901

    		 Estrogen Receptor/ERR Cancer
    Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo.
  • HY-124607B
    BRD3731

    		GSK-3 Metabolic Disease Neurological Disease
    BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 is potentail for the research of post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorders.
  • HY-N11322
    Bitis Arietans Venom

    Puff Adder Venom

    		 Others Cardiovascular Disease
    Bitis Arietans Venom (Puff Adder Venom) is a snake venom that can be obtained from Bitis Arietans. Bitis Arietans Venom inhibits platelet aggregation. The fibrinogenase can be purified from the Bitis Arietans Venom, and cleaves the Aα and Bβ chain of fibrinogen.
  • HY-P9947
    Efalizumab

    		Integrin Others
    Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research.
  • HY-19822A
    Elacestrant dihydrochloride

    RAD1901 dihydrochloride

    		 Estrogen Receptor/ERR Cancer
    Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo.
  • HY-136198
    SRX3207

    		Syk PI3K Cancer
    SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.
  • HY-N7433
    4,6-O-Ethylidene-α-D-glucose

    Ethylidene-glucose

    		 GLUT Endogenous Metabolite Metabolic Disease
    4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport.
  • HY-13728
    Plevitrexed

    ZD 9331; BGC9331

    		 Thymidylate Synthase Cancer
    Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical.
  • HY-107222
    Lysionotin

    		Others Inflammation/Immunology
    Lysionotin is a flavonoid isolated from Gesneriaceae family. Lysionotin efficiently inhibit α-Toxin (a pore-forming protein) expression and shows significant protection against S. aureus in vitro and in vivo. Lysionotin has the potential for the treatment of S. aureus induced pneumonia.
  • HY-B0760
    Fenofibric acid

    FNF acid

    		 PPAR COX Metabolic Disease
    Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
  • HY-N0835
    (20S)-Protopanaxatriol

    20(S)-APPT; g-PPT

    		 Glucocorticoid Receptor Estrogen Receptor/ERR LXR Apoptosis Endocrinology Cardiovascular Disease
    (20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
  • HY-10182G
    Laduviglusib

    CHIR-99021; CT99021

    		 GSK-3 Wnt β-catenin Autophagy Cancer Metabolic Disease
    Laduviglusib (CHIR-99021) (GMP) is Laduviglusib (HY-10182) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Laduviglusib is a potent, orally active and selective GSK-3α/β inhibitor.
  • HY-108766
    Ponatinib hydrochloride

    AP24534 hydrochloride

    		 Bcr-Abl FGFR PDGFR VEGFR Src Autophagy Cancer
    Ponatinib (AP24534) hydrochloride is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-N3078
    p-Hydroxyphenethyl trans-ferulate

    		Glucosidase Endocrinology
    p-Hydroxyphenethyl trans-ferulate has anti-hyperglycemic（yeast α-glucosidase，IC50 19.24 ± 1.73 µmol L-1）, antioxidant, and anti-inflammatory activities. p-Hydroxyphenethyl trans-ferulate shows inhibiting cancer preve
  • HY-148174
    JNJ-3790339

    		DGK Cancer
    JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation.
  • HY-147950
    PDE4-IN-10

    		Phosphodiesterase (PDE) TNF Receptor Inflammation/Immunology
    PDE4-IN-10 (compound 7a) is a potent PDE4 inhibitor, with an IC50 of 7.01 μM for PDE4B. PDE4-IN-10 shows selectivity, microsomal stability, inhibition of TNF-α and no major toxicities in vitro.
  • HY-107427
    PF-3644022

    		MAPKAPK2 (MK2) p38 MAPK Inflammation/Immunology
    PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
  • HY-11109
    Resatorvid

    TAK-242; CLI-095

    		 Toll-like Receptor (TLR) TNF Receptor Interleukin Related Autophagy Inflammation/Immunology Cancer
    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.
  • HY-Z0816
    Dehydronitrosonisoldipine

    		Calcium Channel Others
    Dehydronitrosonisoldipine, a derivative of Nisoldipine (HY-17402), is an irreversible and cell-permeant sterile alpha and TIR motif-containing 1 (SARM1) inhibitor. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. Dehydronitrosonisoldipine can be used for researching neurodegenerative disorders.
  • HY-B1367
    Carbenoxolone disodium

    		Gap Junction Protein Orthopoxvirus 11β-HSD Infection Inflammation/Immunology
    Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation. Carbenoxolone disodium inhibits Vaccinia virus replication.
  • HY-12034
    WYE-354

    		mTOR Autophagy Apoptosis Cancer
    WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro.
  • HY-32329A
    Setiptiline maleate

    MO-8282

    		 5-HT Receptor Neurological Disease
    Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate 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-136351
    THZ-P1-2

    		Autophagy Cancer
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
  • HY-N9283
    1,2-Diacetoxy-4,7,8-trihydroxy-3-(4-hydroxyphenyl)dibenzofuran

    		Reactive Oxygen Species Cancer Neurological Disease
    1,2-Diacetoxy-4,7,8-trihydroxy-3-(4-hydroxyphenyl)dibenzofuran, isolated from the edible mushroom Sarcodon leucopus, has antioxidant effects in the DPPH scavenging assay with the IC50 of 28 μM, inhibits malondialdehyde (MDA) with the IC50 of 71 μM, and inhibits α-glucosidase with the IC50 of 6.22 μM.
  • HY-N6733
    Aphidicolin

    		DNA/RNA Synthesis HSV Apoptosis Antibiotic Orthopoxvirus Infection Inflammation/Immunology
    Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is an antibiotic produced by mold Cephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line.
  • HY-103450
    G36

    		Estrogen Receptor/ERR Endocrinology
    G-36 is a cell permeable non-steroidal antagonist of G-protein-coupled estrogen receptor (GPER/GPR30) which selectively inhibits estrogen-mediated activation of PI3K by GPER, but not by ERα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM).
  • HY-130240
    GCN2-IN-6

    		Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).
  • HY-19805
    STO-609

    		CaMK AMPK Autophagy Metabolic Disease
    STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
  • HY-147506
    NOD2 antagonist 1

    		NOD-like Receptor (NLR) Inflammation/Immunology
    NOD2 antagonist 1 (compound 32) is a potent and selective NOD2 antagonist with an IC50 of 5.23 μM. NOD2 antagonist 1 inhibits Muramyl dipeptide (MDP)-induced IL-8 secretion in THP-1 cells and inhibits MDP-induced IL-6, IL-10, TNF-α release in PBMCs.
  • HY-146419
    Anti-inflammatory agent 20

    		NF-κB COX TNF Receptor Inflammation/Immunology
    Anti-inflammatory agent 20 (compound 5a) is a potent inhibitor of NO activity. Anti-inflammatory agent 20 shows anti-inflammatory activity. Anti-inflammatory agent 20 suppresses LPS-induced inflammation via inhibiting the activation of NF-κB and MAPK signaling and thereby reducing IL-6, TNF-α, iNOS, and COX-2 upregulation.
  • HY-N2574
    Gitogenin

    		Glucosidase Metabolic Disease
    Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms.
  • HY-14590
    Kaempferol

    Kempferol; Robigenin

    		 Estrogen Receptor/ERR Autophagy Mitophagy Apoptosis HIV Parasite Endogenous Metabolite Cancer
    Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
  • HY-W013636
    2-Ketoglutaric acid

    Alpha-Ketoglutaric acid

    		 Tyrosinase Endogenous Metabolite Others
    2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-103435
    Vialinin A

    Terrestrin A

    		 Deubiquitinase Cancer Inflammation/Immunology
    Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research.
  • HY-N7599
    Chrysophanol triglucoside

    		Phosphatase Glucosidase Metabolic Disease
    Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research.
  • HY-15177
    PF-04691502

    		PI3K mTOR Autophagy Cancer
    PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
  • HY-13613S
    Dutasteride-13C6

    GG 745-13C6; GI 198745-13C6

    		 Apoptosis 5 alpha Reductase Cancer
    Dutasteride- 13C6 is the 13C labeled Dutasteride[1]. 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[2].
  • HY-N9445
    Lacto-N-neotetraose

    LNnT

    		 Endogenous Metabolite TNF Receptor Inflammation/Immunology
    Lacto-N-neotetraose (LNnT) is an endogenous metabolite. Lacto-N-neotetraose can inhibit TNF-α induced IL-8 secretion in immature epithelial cells. Lacto-N-neotetraose has anti-inflammatory avtivity, and can improve the wound closure.
  • HY-B0258
    Gemfibrozil

    CI-719

    		 PPAR Cytochrome P450 Metabolic Disease Cardiovascular Disease Cancer
    Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
  • HY-N1956
    Rubiadin-1-methyl ether

    		NF-κB Metabolic Disease
    Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.
  • HY-N3552
    Catalposide

    		NF-κB Inflammation/Immunology
    Catalposide, an iridoid glycoside that could be isolated from Catalpa ovate G. Don (Bignoniaceae), inhibits TNF-α, IL-1β, and IL-6 productions and NF-κB (p65) activation in lipopolysaccharide-activated RAW 264.7 macrophages.
  • HY-151437
    Antifungal agent 40

    		Fungal Infection
    Antifungal agent 40 is an antifungal agent which extends into the narrow hydrophobic pocket II of C.alb. CYP51. Antifungal agent 40 has an inhibitory effect on lanosterol 14α-demethylase (CYP51). Antifungal agent 40 inhibits biofilm formation.
  • HY-N6857
    Armepavine

    		NF-κB Inflammation/Immunology
    Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades.
  • HY-76200
    Voriconazole

    UK-109496

    		 Fungal Bacterial Infection Cancer
    Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
  • HY-152238
    PI3K/mTOR Inhibitor-12

    		PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-12 is a potent, orally active and selective PI3K/mTOR inhibitor with IC50 values of 0.06 nM and 3.12 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity.
  • HY-118266
    BTdCPU

    		Phosphatase Apoptosis Cancer
    BTdCPU is a potent heme regulated inhibitor kinase (HRI) activator that promotes eIF2α phosphorylation and induces apoptosis in Dexamethasone (HY-14648) (Dex)-resistant cancer cells. BTdCPU can be used in the study of cancers such as multiple myeloma and Dex-resistant multiple myeloma.
  • HY-123037
    Triadimefon

    		Fungal Infection
    Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
  • 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-17547
    NMS-E973

    		HSP Cancer
    NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
  • HY-W013636A
    2-Ketoglutaric acid Sodium

    Alpha-Ketoglutaric acid Sodium

    		 Tyrosinase Endogenous Metabolite Metabolic Disease
    2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM).
  • HY-14794
    Dextromilnacipran

    (1R,2S)-milnacipran; F2696

    		 Serotonin Transporter Metabolic Disease
    Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).
  • HY-133680
    β-Tocopherol

    		Tyrosinase Metabolic Disease
    β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.
  • HY-119857
    AGK7

    SIRT2 Inhibitor,Inactive Control

    		 Sirtuin Neurological Disease
    AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease.
  • HY-N7466
    Mezerein

    		PKC Cancer
    Mezerein is a PKC activator that exhibits antileukemic properties. Mezerein inhibits the growth of yeast expressing PKC alpha (IC50=1190 nM), PKC beta1 (IC50=908 nM), and PKC delta (IC50=141 nM) but not of yeast expressing PKC.
  • HY-13504
    PIK-293

    		PI3K Cancer Metabolic Disease
    PIK-293, an analog of IC87114, is a PI3K inhibitor, with IC50 values of 0.24 μM, 10 μM, 25 μM and 100 μM for p110δ, p110β, p110γ and p110α, respectively.
  • HY-100706
    AMA-37

    		DNA-PK Cancer
    AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively.
  • HY-N11311
    Naja Melanoleuca Venom

    Forest Cobra Venom

    		 GABA Receptor Neurological Disease
    Naja Melanoleuca Venom (Forest Cobra Venom) is a snake venom that can be obtained from Naja Melanoleuca. Naja Melanoleuca Venom has hemolytic activities toward human erythrocytes. α-neurotoxins can be isolated from Naja Melanoleuca Venom, and inhibit GABAA receptor.
  • HY-10343
    Sotrastaurin

    AEB071

    		 PKC Inflammation/Immunology Cancer
    Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
  • HY-N9000
    Loganic acid 6′-O-β-D-glucoside

    		TNF Receptor Inflammation/Immunology
    Loganic acid 6′-O-β-D-glucoside, a iridoidal glucoside, is isolated from the whole plant of Gentiana rhodantha (Gentianaceae). Loganic acid 6′-O-β-D-glucoside inhibits LPS-induced NO and TNF-α production in macrophage RAW264.7 cells.
  • HY-138153
    JKE-1674

    		Glutathione Peroxidase Ferroptosis Cancer
    JKE-1674 is an orally active glutathione peroxidase 4 (GPX4) inhibitor and an active metabolite of GPX4 inhibitor ML-210. JKE-1674, an analog of ML-210 in which the nitroisoxazole ring is replaced with an α-nitroketoxime. JKE-1674 can convert into a nitrile oxide JKE-1777. JKE-1674 kills LOX-IMVI cells in a manner that is equipotent to ML-210 and is completely rescued by ferroptosis inhibitors.
  • HY-115976
    COX-2-IN-10

    		COX Inflammation/Immunology
    COX-2-IN-10 is a potent COX-2 inhibitor. COX-2-IN-10 inhibits the production of PGE2 in concentration dependent manner (IC50=2.54 µM). COX-2-IN-10 inhibits the expression of iNOS and COX-2 on mRNA and protein level . COX-2-IN-10 inhibits the production of IL-6, TNF-α and IL-1β.
  • HY-147284
    PI3K-IN-37

    		PI3K mTOR Others
    PI3K-IN-37 (Example 84.1) is a PI3K α/β/δ inhibitor with IC50s of 6, 8, 4 nM, respectively. PI3K-IN-37 can also inhibit mTOR (IC50=4 nM).
  • HY-12330
    AZD8186

    		PI3K Cancer
    AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
  • HY-113756A
    Latanoprost acid

    		Prostaglandin Receptor Inflammation/Immunology
    Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
  • HY-N10047
    7,8-Didehydrocimigenol

    		NF-κB PPAR Cardiovascular Disease
    7,8-Didehydrocimigenol is an active triterpenoid that can be isolated from Cimicifugae rhizoma. 7,8-Didehydrocimigenol inhibits TNF-α-induced VCAM-1 expression, inhibits NF-kB activity and phosphorylation of ERK1/2 and Akt, increases PPAR-γ expression. 7,8-Didehydrocimigenol can be used for the research of cardiovascular disorders such as atherosclerosis.
  • HY-13241
    Ralimetinib dimesylate

    LY2228820 dimesylate

    		 p38 MAPK Autophagy Apoptosis Cancer Inflammation/Immunology
    Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
  • HY-125065
    MK-4541

    		Androgen Receptor 5 alpha Reductase Cancer Endocrinology
    MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model.
  • HY-131707
    LEO 39652

    		Phosphodiesterase (PDE) Inflammation/Immunology
    LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .
  • HY-10108A
    LY294002 hydrochloride

    		PI3K Casein Kinase DNA-PK Apoptosis Cancer
    LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research.
  • HY-123984
    LTβR-IN-1

    		NF-κB Metabolic Disease
    LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor. LTβR-IN-1 also selectively inhibits the nuclear translocation of p52 depended on TNF12A, instead of the nuclear translocation of p65 mediated by TNF-α receptor. LTβR-IN-1 regulates the NF-kB signaling pathway IN a ligand-independent manner.
  • HY-15800
    CZC-25146 hydrochloride

    		LRRK2 Inflammation/Immunology Neurological Disease
    CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases.
  • HY-N1990
    Gypenoside XLIX

    		PPAR Inflammation/Immunology Cardiovascular Disease
    Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
  • HY-107385
    Epristeride

    ONO-9302; SKF105657

    		 5 alpha Reductase Cancer
    Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne.
  • HY-145422
    KIRA9

    		IRE1 Apoptosis Others
    KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis.
  • HY-15245
    GSK2636771

    		PI3K Cancer
    GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
  • HY-N6005
    Methyl caffeate

    		Bacterial Cancer Infection
    Methyl caffeate, an antimicrobial agent, shows moderate antimicrobial and prominent antimycobacterial activities. Methyl caffeate also exhibits α-glucosidase inhibition activity, oxidative stress inhibiting activity, anti-platelet activity, antiproliferative activity in cervix adenocarcinoma and anticancer activity in lung and leukmia cell lines.
  • HY-101569
    Darovasertib

    LXS196; IDE196

    		 PKC Cancer
    Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research.
  • HY-125263
    OP-1074

    		Estrogen Receptor/ERR Cancer
    OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
  • HY-122594
    BNS-22

    		Topoisomerase Cancer
    BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity.
  • HY-106359
    Delmitide

    RDP-58

    		 TNF Receptor IFNAR Reactive Oxygen Species Cancer Infection Inflammation/Immunology
    Delmitide (RDP58) is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide can be used for the research of ulcerative colitis.
  • HY-121538
    CUDA

    		Epoxide Hydrolase PPAR Cardiovascular Disease
    CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
  • HY-76200B
    Voriconazole camphorsulfonate

    UK-109496 camphorsulfonate

    		 Fungal Bacterial Infection
    Voriconazole (UK-109496) camphorsulfonate is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole camphorsulfonate exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
  • HY-12047S
    Ponatinib-d8

    AP24534-d8

    		 Bcr-Abl PDGFR VEGFR FGFR Src Autophagy Cancer
    Ponatinib-d8 is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
  • HY-101392
    Harmane

    		Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor Cancer Neurological Disease
    Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect.
  • HY-32329S
    Setiptiline-d3

    		5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline-d3 is the deuterium labeled Setiptiline. 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[1][2].
  • HY-10571A
    Delavirdine mesylate

    U 90152 mesylate; BHAP-U 90152 mesylate

    		 HIV Reverse Transcriptase Infection
    Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
  • HY-147285
    PI3K/mTOR Inhibitor-9

    		mTOR PI3K Neurological Disease
    PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC50 values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively.
  • HY-13335
    PKCβ inhibitor 1

    		PKC Apoptosis Cancer
    PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
  • HY-107390A
    AX-024 hydrochloride

    		TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-10571
    Delavirdine

    U 90152; BHAP-U 90152

    		 HIV Reverse Transcriptase Infection
    Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
  • HY-107390
    AX-024

    		TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-13333
    NVP-BAG956

    BAG 956

    		 PI3K Cancer
    NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
  • HY-N6775
    Sonolisib

    PX-866

    		 PI3K Cancer
    Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
  • HY-12185
    BRD7389

    		Ribosomal S6 Kinase (RSK) Cancer Metabolic Disease
    BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.
  • HY-120110
    IOX4

    		HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology Neurological Disease
    IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2.
  • HY-124108
    Eicosatetraynoic acid

    ETYA

    		 COX PPAR Orthopoxvirus Others
    Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM. Eicosatetraynoic acid specifically interferes with the replication of the cowpox virus both in vivo and in vitro.
  • HY-A0270
    Diphenidol

    		Others Neurological Disease
    Diphenidol is an orally active antiemetic. Diphenidol reduces abnormal neuropathic pain and TNF-α overexpression in rats following chronic compression injury. Diphenidol also has local anaesthetic activity and inhibits sodium currents. Diphenidol can be used in studies of meniere′s disease, anti-vertigo, antiemetic and analgesia.
  • HY-12235
    PI-3065

    		PI3K Inflammation/Immunology Cancer
    PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
  • HY-17514S
    Itraconazole-d5

    R51211-d5

    		 Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole-d5 is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects[1][2][3].
  • HY-137466
    ARN-21934

    		Topoisomerase Cancer
    ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
  • HY-17406S1
    Tolcapone-d4

    Ro 40-7592-d4

    		 COMT Amyloid-β Apoptosis Cancer Neurological Disease
    Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
  • 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-114855
    BT2

    		Bcl-2 Family Metabolic Disease
    BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM.
  • HY-10230S
    Midostaurin-d5

    PKC412-d5; CGP 41251-d5

    		 Isotope-Labeled Compounds PKC Syk Akt PKA c-Kit Cancer
    Midostaurin-d5 is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1].
  • HY-151427
    TGFβ1-IN-1

    		TGF-β Receptor Inflammation/Immunology
    TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies.
  • HY-120595
    JNJ-49095397

    RV568

    		 p38 MAPK Src Inflammation/Immunology
    JNJ-49095397 (RV568) is an inhaled narrow-spectrum kinase inhibitor (NSKI) against both the α and γ isoforms of p38 MAPK. JNJ-49095397 also inhibits SRC kinase family, specifically haematopoietic kinase (HCK) JNJ-49095397 shows potent anti-inflammatory effects and can be used for the research of chronic obstructive pulmonary disease (COPD) and asthma.
  • HY-101448
    TMI-1

    WAY-171318

    		 MMP Apoptosis Cancer Inflammation/Immunology
    TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood. TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines.
  • HY-18285
    Longdaysin

    		Casein Kinase ERK CDK Cancer
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
  • HY-N1356
    Reticuline

    		JAK STAT NF-κB Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3. Reticuline exhibits cardiovascular effects.
  • HY-B0986
    Hexylresorcinol

    4-Hexylresorcinol

    		 Parasite Bacterial Apoptosis Glucosidase Endogenous Metabolite Cancer Infection Metabolic Disease
    Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
  • HY-135312
    AZ'6421

    		Estrogen Receptor/ERR PROTACs Cancer
    AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer.
  • HY-137005
    CS1

    		Topoisomerase Apoptosis Cancer
    CS1 is a potent DNA Topo II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis.
  • HY-B0164A
    Mizolastine dihydrochloride

    		Histamine Receptor Inflammation/Immunology
    Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial.
  • HY-112613
    UCB9608

    		PI4K Inflammation/Immunology
    UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent.
  • HY-112130
    AGI-24512

    		Methionine Adenosyltransferase (MAT) Cancer
    AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer.
  • HY-147916
    RNA polymerase II-IN-1

    		DNA/RNA Synthesis Cancer
    RNA polymerase II-IN-1 (compound 19iv) is a amatoxin, inhibiting RNA polymerase II (Pol II) with an IC50 value of 36.66 nM. RNA polymerase II-IN-1 has higher cytotoxicity against cancer cells and less toxic in normal cells than α-Amanitin.
  • HY-B0164
    Mizolastine

    		Histamine Receptor Inflammation/Immunology
    Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial.
  • HY-107365
    PQR530

    		PI3K mTOR Cancer
    PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.
  • 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-117395
    PU-H54

    		HSP Cancer
    PU-H54, a Grp94-selective inhibitor, can be used for the research of breast cancer. Hsp90 chaperone family, comprised in humans of four paralogs, Hsp90α, Hsp90β, Grp94 and Trap-1, has important roles in malignancy.
  • HY-N0633
    Muscone

    		Interleukin Related TNF Receptor NF-κB NOD-like Receptor (NLR) Inflammation/Immunology Cardiovascular Disease
    Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate.
  • HY-143412
    MIR002

    		HDAC DNA/RNA Synthesis Apoptosis Cancer
    MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo.
  • HY-P2170
    XMP-629

    XOMA-629

    		 Antibiotic Bacterial Infection Inflammation/Immunology
    XMP-629 (XOMA-629), a cationic α-helical peptide, is a potent endotoxin inhibitor. XMP-629 exhibits broad-spectrum antimicrobial activity via an immunomodulatory mechanism. XOMA 629 has antimicrobial activity against Propionibacterium acnes, Staphylococcus aureus and Streptococcus pyogenesand.
  • HY-108473
    CU-CPT 4a

    TLR3-IN-1

    		 Toll-like Receptor (TLR) Cancer
    CU-CPT 4a (TLR3-IN-1) is a potent, highly selective TLR3 signaling inhibitor. CU-CPT 4a represses the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-α and IL-1β.
  • HY-19717
    DCVC

    S-[(1E)-1,2-dichloroethenyl]--L-cysteine

    		 TNF Receptor Inflammation/Immunology
    DCVC (S-[(1E)-1,2-dichloroethenyl]--L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures.
  • HY-19306
    SB-267268

    		Integrin Cancer
    SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
  • HY-101392S1
    Harmane-d2

    		Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor Cancer Neurological Disease
    Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
  • HY-100513A
    Dehydroaltenusin

    		Apoptosis DNA/RNA Synthesis Antibiotic Cancer
    Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
  • HY-N0515
    Ophiopogonin D

    		PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
  • HY-101392S
    Harmane-d1

    		Imidazoline Receptor Monoamine Oxidase Adrenergic Receptor Cancer Neurological Disease
    Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
  • HY-122026
    PF-04802367

    PF-367

    		 GSK-3 Neurological Disease
    PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.
  • HY-112461A
    NF449 octasodium

    		P2X Receptor Cardiovascular Disease
    NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
  • HY-101489A
    GZD856 formic

    		PDGFR Bcr-Abl Apoptosis Cancer
    GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
  • HY-P1740
    RGD peptide (GRGDNP)

    		Integrin Apoptosis Inflammation/Immunology
    RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation.
  • HY-101489
    GZD856

    		PDGFR Bcr-Abl Apoptosis Cancer
    GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
  • HY-B0006S
    Carvedilol-d3

    		Adrenergic Receptor Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol-d3 is the 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-139439
    SBI-581

    		Ser/Thr Protease Cancer
    SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity.
  • HY-B0006S1
    Carvedilol-d4

    BM 14190-d4

    		 Adrenergic Receptor Autophagy Cancer Inflammation/Immunology Cardiovascular Disease
    Carvedilol-d4 is the 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-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-18766
    EW-7195

    		TGF-β Receptor p38 MAPK Cancer
    EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breas