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Results for "

reversible activator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AMPK (1) Apoptosis (4) Autophagy (2) Bcr-Abl (1) Cathepsin (2) Chloride Channel (1) Cholinesterase (ChE) (1) CRISPR/Cas9 (1) DNA Methyltransferase (2) DOCK (1) Endogenous Metabolite (2) Epigenetic Reader Domain (1) Factor Xa (1) Glucocorticoid Receptor (2) Histone Acetyltransferase (1) Keap1-Nrf2 (1) Ligands for Target Protein for PROTAC (1) Microtubule/Tubulin (2) P2Y Receptor (1) Phosphatase (1) Phosphodiesterase (PDE) (3) Phospholipase (1) PKA (1) Potassium Channel (1) Protease Activated Receptor (PAR) (3) Proteasome (1) Proton Pump (2) Sodium Channel (2) STAT (1) TRP Channel (3) Wnt (2) β-catenin (2)
By Research Areas:	Cancer (14) Cardiovascular Disease (6) Endocrinology (2) Inflammation/Immunology (10) Metabolic Disease (7) Neurological Disease (7)

By Targets:

AMPK (1)

Apoptosis (4)

Autophagy (2)

Bcr-Abl (1)

Cathepsin (2)

Chloride Channel (1)

Cholinesterase (ChE) (1)

CRISPR/Cas9 (1)

DNA Methyltransferase (2)

DOCK (1)

Endogenous Metabolite (2)

Epigenetic Reader Domain (1)

Factor Xa (1)

Glucocorticoid Receptor (2)

Histone Acetyltransferase (1)

Keap1-Nrf2 (1)

Ligands for Target Protein for PROTAC (1)

Microtubule/Tubulin (2)

P2Y Receptor (1)

Phosphatase (1)

Phosphodiesterase (PDE) (3)

Phospholipase (1)

PKA (1)

Potassium Channel (1)

Protease Activated Receptor (PAR) (3)

Proteasome (1)

Proton Pump (2)

Sodium Channel (2)

STAT (1)

TRP Channel (3)

Wnt (2)

β-catenin (2)

By Research Areas:

Cancer (14)

Cardiovascular Disease (6)

Endocrinology (2)

Inflammation/Immunology (10)

Metabolic Disease (7)

Neurological Disease (7)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112472

S3969	Sodium Channel	Metabolic Disease
S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). The apparent EC₅₀ for S3969 activation of hENaC is 1.2 μm .

HY-50662

A-769662

25+ Cited Publications

AMPK Cancer

A-769662 is a potent, reversible AMPK activator with EC₅₀ of 0.8 μM.

A-769662 25+ Cited Publications	AMPK	Cancer
A-769662 is a potent, reversible AMPK activator with EC₅₀ of 0.8 μM.

HY-113221

Isovalerylcarnitine	Proteasome Endogenous Metabolite	Metabolic Disease
Isovalerylcarnitine is a product of the catabolism of L-leucine. Isovalerylcarnitine is also a selective and reversible calpain activator that induces apoptosis .

HY-N0826

Corynoline 2 Publications Verification	Cholinesterase (ChE) Keap1-Nrf2	Neurological Disease Inflammation/Immunology Cancer
Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC₅₀ of 30.6 μM . Corynoline exhibits anti-inflammatory activity by activating Nrf2 .

HY-144813

Gü2602	Cathepsin	Inflammation/Immunology Cancer
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a K_i of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen .

HY-144812

Gü1303	Cathepsin	Inflammation/Immunology Cancer
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a K_i of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen .

HY-12809

Optovin 1 Publications Verification	TRP Channel	Neurological Disease
Optovin is a reversible photoactivated TRPA1 ligand that enables light-mediated neuronal excitation. Optovin activates TRPA1 via structure-dependent photochemical reactions with redox-sensitive cysteine residues .

HY-109079A

Abeprazan hydrochloride DWP14012 hydrochloride; Fexuprazan hydrochloride	Proton Pump	Metabolic Disease
Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H ⁺, K ⁺- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .

HY-109079

Abeprazan DWP14012; Fexuprazan	Proton Pump	Metabolic Disease
Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H ⁺, K ⁺- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .

HY-13030

(+)-JQ-1 Maximum Cited Publications 199 Publications Verification JQ1	Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC	Cancer
(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)) . (+)-JQ-1 also activates autophagy .

HY-13520

Nocodazole 50+ Cited Publications Oncodazole; R17934	Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis	Cancer
Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.

HY-W008956

Myoseverin	Microtubule/Tubulin	Inflammation/Immunology
Myoseverina, a microtubule-binding molecule, induces the reversible fission of multinucleated myotubes into mononucleated fragments. Myoseverina affects the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration .

HY-18200

Atopaxar E5555; ER-172594-00	Protease Activated Receptor (PAR)	Cardiovascular Disease
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor *protease-activated* receptor-1 (PAR-1)** antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease .

HY-19837

BMS-986120
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC₅₀s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .

HY-118628

N-(p-amylcinnamoyl) Anthranilic Acid 2 Publications Verification ACA	Phospholipase TRP Channel	Cardiovascular Disease
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A₂ (PLA₂) inhibitor and TRP channel blocker . N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of *calcium-activated* chloride channels**, has potential to treat arrhythmia .

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-18200B

Atopaxar hydrobromide E5555 hydrobromide; ER 172594-06	Protease Activated Receptor (PAR)	Cardiovascular Disease
Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor *protease-activated* receptor-1 (PAR-1)** antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease .

HY-19638A

Cangrelor tetrasodium 1 Publications Verification AR-C69931MX tetrasodium	P2Y Receptor	Cardiovascular Disease Inflammation/Immunology
Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist .

HY-147049

PAL-4	Others	Metabolic Disease
PAL-4 (compound 4) is a potent, selective and reversible Lysophospholipase-like 1 (LYPLAL1) activator with EC₅₀ value of 0.39 μM and 0.49 μM for mice LYPLAL1 and huamn LYPLAL1, respectively. PAL-4 can be used for researching metabolic disorders .

HY-128358

MR-L2	Phosphodiesterase (PDE)	Neurological Disease
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC₅₀ of 1.2 µM .

HY-117290

BMS-962212	Factor Xa	Cardiovascular Disease
BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity .

HY-115537

NAE-IN-M22	Apoptosis	Cancer
NAE-IN-M22 is a potent, selective and reversible inhibitor of *NEDD8 activating* enzyme (NAE)**, with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo .

HY-19638

Cangrelor AR-C69931MX
Cangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist .

HY-E70028

UDP-sugar pyrophosphorylase (BlUSP)	Endogenous Metabolite	Metabolic Disease
UDP-sugar pyrophosphorylase (BlUSP) is the enzyme capable of activating glucose-1-phosphate (Glc-1-P) to UDP-glucose (UDP-Glc). UDP-sugar pyrophosphorylase (BlUSP) catalyzes a reversible transfer of the uridyl group from UTP to sugar-1-phosphate, producing UDP-sugar and pyrophosphate (PPi) .

HY-161125

(+)-JQ1-OH	Others	Others
(+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC_50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy .

HY-14930A

Mirodenafil dihydrochloride SK-3530 dihydrochloride	Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc) .

HY-14930

Mirodenafil SK3530	Phosphodiesterase (PDE) Glucocorticoid Receptor Wnt β-catenin Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc) .

HY-139664A

(R)-GSK-3685032	DNA Methyltransferase	Cancer
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. 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-153128

DOCK2-IN-1	DOCK	Inflammation/Immunology
DOCK2-IN-1 (compound 3), a CPYPP (HY-110100) analogue, is an inhibitor of DOCK2 as well (IC₅₀=19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and T cell activation .

HY-139664B

(S)-GSK-3685032	Others	Cancer
(S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. 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-100671

L002	Histone Acetyltransferase STAT	Inflammation/Immunology Cancer
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC₅₀ of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment .

HY-103371

DCPIB 5 Publications Verification	Chloride Channel Potassium Channel	Neurological Disease
DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK, and inhibits TRESK, TASK1 and TASK3 (IC₅₀s: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (I_Cl,swell), with an IC₅₀ of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels .

HY-107146

PZ-128 P1pal-7	Protease Activated Receptor (PAR)	Cardiovascular Disease Cancer
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible *protease-activated* receptor-1 (PAR1)** antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .

HY-108464A

Phenamil methanesulfonate	Sodium Channel TRP Channel	Metabolic Disease Inflammation/Immunology
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC₅₀ of 400 nM . Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca ²⁺ transport with an IC₅₀ of 140 nM in a Ca ²⁺ uptake assay . Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway . Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease .

HY-155848

LYP-IN-4	Phosphatase	Cancer
LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models.

HY-N6789

KT5720 3 Publications Verification	PKA	Neurological Disease Cancer
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC₅₀=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 ⁺ concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .

UDP-sugar pyrophosphorylase (BlUSP)	Biochemical Assay Reagents
UDP-sugar pyrophosphorylase (BlUSP) is the enzyme capable of activating glucose-1-phosphate (Glc-1-P) to UDP-glucose (UDP-Glc). UDP-sugar pyrophosphorylase (BlUSP) catalyzes a reversible transfer of the uridyl group from UTP to sugar-1-phosphate, producing UDP-sugar and pyrophosphate (PPi) .

PZ-128 P1pal-7	Protease Activated Receptor (PAR)	Cardiovascular Disease Cancer
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible *protease-activated* receptor-1 (PAR1)** antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .

Isovalerylcarnitine	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Other Diseases Endogenous metabolite Disease Research Fields	Proteasome Endogenous Metabolite
Isovalerylcarnitine is a product of the catabolism of L-leucine. Isovalerylcarnitine is also a selective and reversible calpain activator that induces apoptosis .

Corynoline 2 Publications Verification	Alkaloids other families Classification of Application Fields Neurological Disease Source classification Plants Isoquinoline Alkaloids Disease Research Fields Cancer	Cholinesterase (ChE) Keap1-Nrf2
Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC₅₀ of 30.6 μM . Corynoline exhibits anti-inflammatory activity by activating Nrf2 .

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