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Results for "

selective inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5 alpha Reductase (1) 5-HT Receptor (9) Adenosine Deaminase (1) Adenosine Receptor (4) Adenylate Cyclase (2) Adrenergic Receptor (8) Akt (4) AMPK (1) Amyloid-β (3) Anaplastic lymphoma kinase (ALK) (3) Androgen Receptor (3) Angiotensin Receptor (1) Antibiotic (1) Apoptosis (36) ATM/ATR (3) Aurora Kinase (1) Autophagy (17) Bacterial (8) Bcl-2 Family (1) Beta-secretase (1) Biochemical Assay Reagents (1) Btk (3) c-Fms (2) c-Kit (1) c-Met/HGFR (4) c-Myc (1) Calcium Channel (4) CaMK (1) Cannabinoid Receptor (1) Carbonic Anhydrase (5) Casein Kinase (5) Caspase (1) Cathepsin (1) CCR (4) CDK (13) CETP (1) CFTR (2) Cholinesterase (ChE) (11) COMT (2) COX (3) CXCR (2) Cytochrome P450 (6) Dihydrofolate reductase (DHFR) (1) Dihydroorotate Dehydrogenase (1) Dipeptidyl Peptidase (1) Discoidin Domain Receptor (1) DNA Methyltransferase (2) DNA/RNA Synthesis (4) Dopamine Receptor (2) Dopamine Transporter (1) Dopamine β-hydroxylase (2) Drug Metabolite (3) DYRK (1) E1/E2/E3 Enzyme (1) EGFR (2) Endogenous Metabolite (3) Endothelin Receptor (1) Epigenetic Reader Domain (4) ERK (5) Estrogen Receptor/ERR (2) Eukaryotic Initiation Factor (eIF) (1) Farnesyl Transferase (1) Fatty Acid Synthase (FASN) (1) Ferroptosis (2) FGFR (2) Filovirus (1) FLT3 (3) Fungal (1) GABA Receptor (6) Glucocorticoid Receptor (1) Glutathione Peroxidase (2) GPR109A (1) GPR119 (1) GSK-3 (3) HDAC (15) Histamine Receptor (4) Histone Acetyltransferase (3) Histone Demethylase (3) Histone Methyltransferase (6) HIV (1) HSP (1) Influenza Virus (3) IRAK (4) Isocitrate Dehydrogenase (IDH) (2) Isotope-Labeled Compounds (10) JAK (2) JNK (1) Kallikrein (1) Kinesin (1) Leukotriene Receptor (1) Ligands for Target Protein for PROTAC (1) Lipoxygenase (1) LOX-1 (1) MAGL (2) MAP3K (2) MAP4K (1) MDM-2/p53 (1) MEK (2) mGluR (3) Microtubule/Tubulin (2) MMP (1) Monoamine Oxidase (6) Monocarboxylate Transporter (1) mTOR (5) Myosin (2) Na+/Ca2+ Exchanger (1) Na+/HCO3- Cotransporter (1) nAChR (3) Neuropeptide Y Receptor (1) NF-κB (2) NO Synthase (1) Notch (1) Opioid Receptor (1) Organoid (1) Orthopoxvirus (1) P-glycoprotein (2) P2Y Receptor (1) p38 MAPK (8) PAK (1) Parasite (5) PARP (2) Phosphatase (3) Phosphodiesterase (PDE) (12) Phospholipase (1) PI3K (8) Piezo Channel (1) Pim (1) PKA (2) PKC (4) Polo-like Kinase (PLK) (2) Potassium Channel (6) Prolyl Endopeptidase (PREP) (1) Prostaglandin Receptor (2) PROTACs (4) Proteasome (2) Proton Pump (1) Raf (2) RAR/RXR (2) Ras (2) Reactive Oxygen Species (1) RET (1) ROCK (1) ROS Kinase (3) Salt-inducible Kinase (SIK) (1) SARS-CoV (1) Ser/Thr Protease (1) Serotonin Transporter (1) Sigma Receptor (1) Sirtuin (1) Sodium Channel (5) Src (2) Syk (1) TAM Receptor (1) TGF-β Receptor (4) Thrombin (1) TNF Receptor (4) Topoisomerase (1) Trk Receptor (1) TRP Channel (3) TrxR (1) ULK (2) Vasopressin Receptor (3) VEGFR (4) γ-secretase (5)
By Research Areas:	Cancer (166) Cardiovascular Disease (23) Endocrinology (18) Infection (20) Inflammation/Immunology (47) Metabolic Disease (20) Neurological Disease (73)
Click Chemistry:	Alkynes (1)

329

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15546

BMS-817399	CCR	Inflammation/Immunology
BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC₅₀), respectively. BMS-817399 can be used for the research of rheumatoid arthritis .

HY-N1377

Nevadensin	Bacterial	Infection Metabolic Disease Inflammation/Immunology
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC₅₀ of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive .

HY-147984

hCAXII-IN-3

Carbonic Anhydrase Cancer

hCAXII-IN-3 (Compound 6o) is a selective human carbonic anhydrase XII (hCAXII) inhibitor with a K_i of 10.0 nM .

hCAXII-IN-3	Carbonic Anhydrase	Cancer
hCAXII-IN-3 (Compound 6o) is a selective human carbonic anhydrase XII (hCAXII) inhibitor with a K_i of 10.0 nM .

HY-147985

hCA I-IN-1	Carbonic Anhydrase	Cancer
hCA I-IN-1 (Compound 6q) is a human carbonic anhydrase I (hCA I) inhibitor with K_i values of 38.3, 716.4, 940.1 and 192.8 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .

HY-147986

hCA I-IN-2	Carbonic Anhydrase	Cancer
hCA I-IN-2 (Compound 6d) is a selective human carbonic anhydrase I (hCA I) inhibitor with K_i values of 18.8, 375.1, 1721 and 283.9 nM against hCA I, hCA II, hCAIX and hCAXII, respectively .

HY-12960

SKLB4771 FLT3-IN-1	FLT3 c-Kit Apoptosis	Cancer
SKLB4771 is a potent and selective Flt3 inhibitor with an IC₅₀ value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .

HY-143465

BChE-IN-5	Cholinesterase (ChE)	Neurological Disease
BChE-IN-5 is a potent and selective BChE inhibitor of hBChE over hAChE with an IC₅₀ of 2.8 nM for BChE. BChE-IN-5 has the potential for the research of alzheimer’s disease .

HY-134904

RMC-6272 RM-006	mTOR	Cancer
RMC-6272 (RM-006) is a bi-steric *mTORC1*-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors .

HY-129496

NP-313	Thrombin	Cardiovascular Disease
NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca ²⁺ inward flow .

HY-139001

JKE-1716	Glutathione Peroxidase Ferroptosis	Others
JKE-1716 is a potent and selective nitrolic acid-containing GPX4 inhibitor. JKE-1716 is able of inducing ferroptosis selectively through covalent GPX4 inhibition .

HY-130199

Psoromic acid Parellic acid	Others	Metabolic Disease
Psoromic acid is a potent and selective RabGGTase (Rab geranylgeranyl transferase) inhibitor with an IC₅₀ value of 1.3 µM. Psoromic acid is an antioxidative agent. Psoromic acid exhibits a competitive type of HMGR inhibition and mixed type of ACE (angiotensin converting enzyme) inhibition .

HY-106951

MK 386

L-733692
5 alpha Reductase Cancer

MK 386 (L-733692) is a selective 5-α-reductase I inhibitor, used for prostate cancer inhibition .
HY-N12747

Dichlorogelignate

Topoisomerase Others

Dichlorogelignate (compound 4) is a selective inhibitor of topoisomerase II (Topo II). Dichlorogelignate has 100% inhibition at 50 μM .

MK 386 L-733692	5 alpha Reductase	Cancer
MK 386 (L-733692) is a selective 5-α-reductase I inhibitor, used for prostate cancer inhibition .

Dichlorogelignate	Topoisomerase	Others
Dichlorogelignate (compound 4) is a selective inhibitor of topoisomerase II (Topo II). Dichlorogelignate has 100% inhibition at 50 μM .

HY-101578

2614W94	Monoamine Oxidase	Neurological Disease
2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC₅₀ of 5 nM and K_i of 1.6 nM with serotonin as substrate.

HY-15979A

H-89 dihydrochloride Maximum Cited Publications 96 Publications Verification	PKA Autophagy	Others
H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC₅₀ of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.

HY-12528

DBPR108	Dipeptidyl Peptidase	Metabolic Disease
DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.

HY-112082

BAY885

ERK Cancer

BAY885 is a highly potent and selective ERK5 inhibitor with an IC₅₀ of 35 nM. BAY885 shows weak inhibition on others kinases .

BAY885	ERK	Cancer
BAY885 is a highly potent and selective ERK5 inhibitor with an IC₅₀ of 35 nM. BAY885 shows weak inhibition on others kinases .

HY-139852

PLAP-IN-1	Phosphatase	Cancer
PLAP-IN-1 is a potent (IC₅₀ = 32 nM) and selective PLAP inhibitor, with no detectable inhibition of tissue non-specific alkaline phosphatase (TNAP) activity.

HY-14719

RO4987655

4 Publications Verification

CH4987655
MEK Cancer

RO4987655 is an orally active and highly selective MEK inhibitor with an IC₅₀ of 5.2 nM for inhibition of MEK1/MEK2.
HY-157889

ZINC000028464438

HDAC Cancer

ZINC000028464438 is a selective HDAC11 inhibitor with an IC₅₀ of 3.5 µM. ZINC000028464438 shows almost no inhibition for other HDAC subtypes .

RO4987655 4 Publications Verification CH4987655	MEK	Cancer
RO4987655 is an orally active and highly selective MEK inhibitor with an IC₅₀ of 5.2 nM for inhibition of MEK1/MEK2.

ZINC000028464438	HDAC	Cancer
ZINC000028464438 is a selective HDAC11 inhibitor with an IC₅₀ of 3.5 µM. ZINC000028464438 shows almost no inhibition for other HDAC subtypes .

HY-153398

Enpp-1-IN-17	Phosphodiesterase (PDE)	Infection Cancer
Enpp-1-IN-17 (example 274) is a potent ENPP1 inhibitor, with the inhibition constants (Ki values) toward cGAMP and ATP hydrolysis of 100 nM-1 μM and > 1 μM, respectively. The selectivity ratio for inhibition of cGAMP hydrolysis versus ATP hydrolysis is >6.4 .

HY-104013

Aminopurvalanol A	CDK Apoptosis	Cancer
Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .

HY-15418

RS 504393 15+ Cited Publications	CCR	Inflammation/Immunology Endocrinology
RS 504393 is a selective CCR2 chemokine receptor antagonist (IC₅₀ values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).

HY-15663

IPA-3

10+ Cited Publications

PAK Cancer

IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC₅₀ of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).

IPA-3 10+ Cited Publications	PAK	Cancer
IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC₅₀ of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).

HY-12089

Torcetrapib CP-529414	CETP	Endocrinology
Torcetrapib (CP-529414) is a selective, potent cholesteryl ester transfer protein (CETP) inhibitor. A typical inhibition curve for whole human plasma, having a CETP concentration of 37 nM .

HY-N3035

Tetrahydroepiberberine	Fungal Influenza Virus	Infection
Tetrahydroepiberberine is a isoquinoline alkaloid isolated from Corydalis impatiens (Pall). Tetrahydroepiberberine has antifungal and selective inhibition against the PI-3 virus activities .

HY-144706

Axl-IN-3

TAM Receptor Cancer

Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC₅₀ of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases .
HY-147655

CQ211

Others Cancer

CQ211 is a potent and selective RIOK2 inhibitor with a K_d of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines .

Axl-IN-3	TAM Receptor	Cancer
Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC₅₀ of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases .

CQ211	Others	Cancer
CQ211 is a potent and selective RIOK2 inhibitor with a K_d of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines .

HY-115908

ZDLD13	CDK Apoptosis	Cancer
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC₅₀ value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .

HY-108530

MM11253	RAR/RXR	Cancer
MM11253 is a potent and selective RARγ antagonist with an IC₅₀ of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists .

HY-19972

ML243
ML243 is a selective small-molecule inhibitor of breast cancer stem cells. ML243 has 32-fold greater selective inhibition in the breast CSC-like cell line HMLE_shECad than the control cell line HMLE_shGFP .

HY-162257

BTK-IN-34	Btk	Cancer
BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway .

HY-116482

Desmedipham	Others	Others
Desmedipham is a selective systemic phenyl-carbamate herbicide. Desmedipham acts by disrupting CO₂ fixation and the production of intermediary energy components-ATP and NADPH₂ and inhibition of Hill reaction .

HY-147664

hCAXII-IN-1	Carbonic Anhydrase	Cancer
These compounds show selective inhibition on tumor related subtypes HCA IX and XII, and are also considered as the leading molecules for the development of future cancer therapeutic drugs based on new mechanisms of action.

HY-150095

YE6144	Others	Inflammation/Immunology
YE6144 is a prototypical interferon regulatory factor 5 (IRF5) inhibitor. YE6144 selectively suppresses IRF5 activity through inhibition of IRF5 phosphorylation .

HY-148799

Sevasemten	Myosin	Others
Sevasemten is an allosteric inhibitor of skeletal muscle myosin. Sevasemten exhibits selectively myosin inhibition with IC₅₀s of ≤10 μM (skeletal), >100 μM (cardiac), respectively .

HY-119288

BC-23 NSC 45382	Proteasome	Cancer
BC-23 (NSC 45382) is a proteasome inhibitor. BC-23 exhibits good inhibition of CT-L activity of the proteasome and is selective for malignant over normal cells .

HY-119649

Flonicamid IKI220	Parasite	Infection
Flonicamid (IKI220) is a novel systemic insecticide with selective activity against hemipterous pests. The main insecticidal mechanism of flonicamid is starvation based on the inhibition of stylet penetration to plant tissues .

HY-162100

MR-2088	ULK Autophagy	Cancer
MR-2088 is a selective ULK1/ULK2 inhibitor with pEC₅₀ values of 8.3 and 8.7, respectively. MR-2088 selectively inhibits autophagy through ULK1/2 mediated inhibition .

HY-139664

GSK-3685032 3 Publications Verification	DNA Methyltransferase	Cancer
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible *DNMT1*-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-145072

BSJ-01-175	CDK	Cancer
BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells .

HY-15979

H-89 Maximum Cited Publications 96 Publications Verification	PKA Autophagy	Neurological Disease
H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC₅₀ of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.

HY-108488

KB SRC 4	Src	Cancer
KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a K_i of 44 nM and a K_d of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.

HY-132808

Atuzabrutinib SAR 444727; PRN473	Btk	Inflammation/Immunology
Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling .

HY-157135

hCAIX-IN-19	Carbonic Anhydrase	Cancer
hCAIX-IN-19 is a sulfonamides inhibitor against hCA IX with an inhibition constant (K_I) of 6.2 nM and show good selectivity over hCA I (hCA I/ hCA IX = 117) .

HY-144687

ATM Inhibitor-4	ATM/ATR PI3K mTOR	Cancer
ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC₅₀ of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .

HY-13909

RGFP966 25+ Cited Publications	HDAC	Cancer
RGFP966 is a highly selective HDAC3 inhibitor with an IC₅₀ of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).

HY-12299

WH-4-023 4 Publications Verification 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-10966

SB-590885 4 Publications Verification	Raf	Cancer
SB-590885 is a potent B-Raf* inhibitor* with K_i of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.

HY-12504

Pyr6 1 Publications Verification N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide	TRP Channel	Others
Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).

Cat. No.	Product Name

HY-L036P

Covalent Screening Library Plus

2988 compounds

Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.

MCE covalent inhibitor library contains 2988 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

HY-L036

Covalent Screening Library

1670 compounds

MCE covalent inhibitor library contains 1670 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

HY-L130

Non-steroidal Anti-Inflammatory Compound Library

597 compounds

Non-steroidal anti-inflammatory drugs (NSAIDs) are members of a therapeutic drug class with potent anti-inflammatory, analgesic and antipyretic activity, and are among the most widely used drugs worldwide. The most prominent NSAIDs are aspirin, ibuprofen, and naproxen.

The main mechanism of action of NSAIDs is the inhibition of the enzyme cyclooxygenase (COX), based on which NSAIDs can be classified into two types: non-selective and COX-2 selective. Most NSAIDs are non-selective and inhibit both COX-1 and COX-2 activity.

MCE offers a unique collection of 597 non-steroidal compounds with identified anti-inflammatory activity. MCE non-steroidal anti-inflammatory library is a useful tool for the study of anti-inflammatory drugs and pharmacology.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1377

Nevadensin	Flavonoids other families Classification of Application Fields Flavones Source classification Phenols Polyphenols Metabolic Disease Plants Disease Research Fields Inflammation/Immunology	Bacterial
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC₅₀ of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive .

HY-N3035

Tetrahydroepiberberine	Infection Alkaloids Classification of Application Fields Source classification Ranunculaceae Coptis chinensis Franch. Plants Isoquinoline Alkaloids Disease Research Fields	Fungal Influenza Virus
Tetrahydroepiberberine is a isoquinoline alkaloid isolated from Corydalis impatiens (Pall). Tetrahydroepiberberine has antifungal and selective inhibition against the PI-3 virus activities .

HY-116506

Bigelovin	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Acacia auriculiformis A.Cunn. ex Benth Plants Compositae Disease Research Fields Cancer	RAR/RXR Reactive Oxygen Species Apoptosis Autophagy
Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation .

HY-130199

Psoromic acid Parellic acid	Structural Classification Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Metabolic Disease Disease Research Fields	Others
Psoromic acid is a potent and selective RabGGTase (Rab geranylgeranyl transferase) inhibitor with an IC₅₀ value of 1.3 µM. Psoromic acid is an antioxidative agent. Psoromic acid exhibits a competitive type of HMGR inhibition and mixed type of ACE (angiotensin converting enzyme) inhibition .

HY-N12747

Dichlorogelignate	Structural Classification Source classification Phenols Polyphenols Plants Boraginaceae Arnebia euchroma (Royle) Johnst.	Topoisomerase
Dichlorogelignate (compound 4) is a selective inhibitor of topoisomerase II (Topo II). Dichlorogelignate has 100% inhibition at 50 μM .

HY-N0071

Crotonoside Isoguanosine	Alkaloids Structural Classification Classification of Application Fields Croton tiglium Linn. Source classification Euphorbiaceae Plants Disease Research Fields Cancer	FLT3 HDAC
Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the research of AML .

HY-N7598

Chrysophanol-1-O-β-gentiobioside	Seeds of Cassia tora Linn. Quinones Monophenols other families Leguminosae Anthraquinones Source classification Phenols Plants	Monoamine Oxidase
Chrysophanol-1-O-β-gentiobioside, an anthraquinone glycoside isolated from Cassia obtusifolia seeds. Chrysophanol-1-O-β-gentiobioside shows selective inhibition of hMAO-A isozyme activity (IC₅₀=96.15 μM) .

HY-B0199

Mycophenolate Mofetil 5+ Cited Publications RS 61443; TM-MMF	Structural Classification Monophenols Classification of Application Fields Source classification Phenols Endogenous metabolite Disease Research Fields Cancer	Drug Metabolite Apoptosis Endogenous Metabolite Bacterial
Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation .

HY-N10132

Microgrewiapine A	Malvaceae Structural Classification Alkaloids Microcos paniculata L. Other Alkaloids Source classification Plants	nAChR
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC₅₀ of 6.8 μM .

HY-N0069

Solamargine Maximum Cited Publications 11 Publications Verification Solamargin; δ-Solanigrine	Structural Classification Alkaloids Piperidine Alkaloids Solanum Classification of Application Fields Plants Solanaceae Disease Research Fields Saccharides Steroids Cancer	P-glycoprotein Apoptosis
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity .

HY-N0749

Jatrorrhizine	Alkaloids Monophenols other families Source classification Phenols Plants Isoquinoline Alkaloids	Cholinesterase (ChE) 5-HT Receptor Bacterial
Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine is a potent and orally active inhibitor of AChE (IC₅₀=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .

HY-N0740

Jatrorrhizine chloride	Alkaloids Monophenols Source classification Ranunculaceae Coptis chinensis Franch. Phenols Plants Isoquinoline Alkaloids	Cholinesterase (ChE) 5-HT Receptor Bacterial
Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC₅₀=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .

HY-N0747

Oxypeucedanin	Cardiovascular Disease Structural Classification Chrysanthemum × morifolium (Ramat.) Hemsl. Classification of Application Fields Source classification Coumarins Phenylpropanoids Plants Umbelliferae Disease Research Fields	Potassium Channel Apoptosis
Oxypeucedanin is a furocoumarin derivative isolated from Angelica dahurica. Oxypeucedanin is a selective open-channel blocker, inhibits the hKv1.5 current with an IC₅₀ value of 76 nM. Oxypeucedanin prolongs cardiac action potential duration (APD), is a potential antiarrhythmic agent for atrial fibrillation . Oxypeucedanin induces cell apoptosis through inhibition of cancer cell migration .

HY-N10649

PTP1B-IN-21	Quinones Structural Classification Anthraquinones Rubiaceae Knoxia valerianoides Thorel ex Pitard Plants	Phosphatase
PTP1B-IN-21 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC₅₀=1.56 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC₅₀>100 μM), which is a key target for type 2 diabetes inhibition .

HY-111557

YM-254890 5+ Cited Publications	Cardiovascular Disease Structural Classification Natural Products Microorganisms Classification of Application Fields Source classification Disease Research Fields	P2Y Receptor
YM-254890 is a selective G_αq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y₁ signal transduction pathway, with an IC₅₀ value below 0.6 μM .

HY-N10648

PTP1B-IN-20	Quinones Structural Classification Anthraquinones Rubiaceae Knoxia valerianoides Thorel ex Pitard Plants	Phosphatase
PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC₅₀=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC₅₀=78.0 μM), which is a key target for type 2 diabetes inhibition .

HY-N0749A

Jatrorrhizine hydroxide	Alkaloids Monophenols Source classification Ranunculaceae Coptis chinensis Franch. Phenols Plants Isoquinoline Alkaloids	Cholinesterase (ChE) 5-HT Receptor Bacterial
Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC₅₀=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .

HY-B0199R

Mycophenolate Mofetil (Standard) RS 61443 (Standard); TM-MMF (Standard)	Structural Classification Monophenols Source classification Phenols Endogenous metabolite	Drug Metabolite Apoptosis Endogenous Metabolite Bacterial
Mycophenolate Mofetil (Standard) is the analytical standard of Mycophenolate Mofetil. This product is intended for research and analytical applications. Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation .

HY-N6796

Manumycin A	Infection Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Disease Research Anticancer Disease Research Fields Other Antibiotics	Farnesyl Transferase Ras Apoptosis Phospholipase
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (K_i=1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling . Manumycin A is a nSMase inhibitor (EC₅₀=0.25 μM) .

HY-N1638

1-Methyl-2-undecyl-4(1H)-quinolone	Alkaloids Source classification Evodia rutaecarpa (Juss.) Benth. Rutaceae Quinoline Alkaloids Plants	Monoamine Oxidase
1-Methyl-2-undecyl-4(1H)-quinolone is a potent, irreversible and selective inhibitor of type B monoamine oxidase (MAO-B). 1-Methyl-2-undecyl-4(1H)-quinolone shows a selective inhibition of MAO-B activity with the IC₅₀ and K_i values of 15.3 μM and 9.91 μM, respectively, but did not inhibit type A MAO (MAO-A) activity. Methyl-2-undecyl-4(1H)-quinolone, as a quinolone alkaloid, is isolated from fresh leaves and fruits of Evodia rutaecarpa HOOK. f. et THOMS .

HY-N0632

Esculentoside A 2 Publications Verification	Triterpenes Structural Classification Classification of Application Fields Terpenoids Source classification Phytolacca acinosa Roxb. Plants Inflammation/Immunology Disease Research Fields Phytolaccaceae	COX NF-κB
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta . Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitory activity towards cyclooxygenase-2 (COX-2) . Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .

Cat. No.	Product Name	Chemical Structure

HY-17000S

Tolvaptan-d7
Tolvaptan-d₇ is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation[1][2].

HY-17385S

Atomoxetine-d5 hydrochloride
Atomoxetine-d₅ (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively)[1][2].

HY-107370AS

(Rac)-Atomoxetine-d7 hydrochloride
(Rac)-Atomoxetine-d₇ (hydrochloride) is a deuterium labeled (Rac)-Atomoxetine hydrochloride. (Rac)-Atomoxetine hydrochloride is a racemic form of Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively)[1].

HY-118827S

Vedaprofen-d3
Vedaprofen-d₃ is the deuterium labeled Vedaprofen. Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition [1]. Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM[2].

HY-10195BS

Ruboxistaurin-d6 hydrochloride
Ruboxistaurin-d₆ (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].

HY-B1396S

Nefazodone-d6 hydrochloride
Nefazodone-d₆ (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

HY-B1396S1

Nefazodone-d6 dihydrochloride
Nefazodone-d₆ (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

HY-B0199S

Mycophenolate Mofetil-d4

Mycophenolate Mofetil-d₄ is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443) is the morpholinoethylester proagent of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation[1].

HY-B0007S

Baclofen-d4

Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].

HY-17406S1

Tolcapone-d4

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-B0007S2

Baclofen-d5 hydrochloride

Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-50878AS

Crizotinib-d9 hydrochloride

Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .

HY-103309S

ML218-d9

ML218-d₉ is the deuterium labeled ML218. ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier[1].

HY-126242S

Tyk2-IN-7

Tyk2-IN-7 is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model[1].

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