Search Result
Results for "
Do Inhibitors
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-114157
-
DO-264
1 Publications Verification
|
MAGL
|
Neurological Disease
|
DO-264 is a selective and in vivo-active inhibitor of Abhydrolase Domain Containing 12 (ABHD12), with an IC50 of 11 nM.
|
-
-
- HY-108419
-
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JNK
|
Cancer
|
WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM .
|
-
-
- HY-117771A
-
|
Others
|
Metabolic Disease
|
DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.
|
-
-
- HY-N8659
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Uzarigenin 3-β-sophoroside
|
Others
|
Others
|
Uzarin is a steroid glycoside. Uzarin does not
inhibit cell proliferation or induce apoptosis .
|
-
-
- HY-50683S
-
|
c-Met/HGFR
|
Cancer
|
JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
|
-
-
- HY-117200
-
Nec-7
|
Necroptosis
|
Cancer
|
Necrotatin-7 (Nec-7) is a potent necroptosis inhibitor with an EC50 of 10.6 μM. Necrotatin-7 does not inhibit recombinant RIP1 kinase .
|
-
-
- HY-152214
-
|
Sirtuin
|
Cancer
|
SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD + -binding pocket and acts as a substrate-competitive inhibitor .
|
-
-
- HY-123070
-
|
Phospholipase
|
Inflammation/Immunology
|
ONO-RS-082 is an inhibitor of phospholipase A (PLA) . ONO-RS-082 inhibits PLA2 with the IC50 of 1.0 μM, but does not inhibit PLC even at 100 μM .
|
-
-
- HY-13802
-
SC-514
5 Publications Verification
GK 01140
|
IKK
|
Cancer
|
SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
|
-
-
- HY-103348
-
Boc-Asp(OMe)-FMK
|
Caspase
|
Inflammation/Immunology
|
Boc-Asp(OME)-Fluoromethyl Ketone is a broad range caspase inhibitor that inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8 .
|
-
-
- HY-112715
-
|
ATP Synthase
|
Cardiovascular Disease
|
ATP synthase inhibitor 1 is a potent inhibitor of c subunit of the F1/FO-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels .
|
-
-
- HY-N7091
-
|
Others
|
Metabolic Disease
|
Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term .
|
-
-
- HY-117765
-
|
Calcium Channel
|
Neurological Disease
|
RS-5773 is a calcium channel inhibitor and a diltiazem congener. RS-5773 has antianginal effect and does not cause excessive hypotension or depression of atrioventricular conduction .
|
-
-
- HY-119874
-
|
Pyruvate Kinase
|
Inflammation/Immunology
Cancer
|
Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent .
|
-
-
- HY-117771
-
DO34
2 Publications Verification
|
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-149258
-
-
-
- HY-107621
-
|
MEK
|
Cancer
|
U0124, an inactive U0126 analog, has no effect on c-Fos and c-Jun protein or mRNA levels. U0126 is a MEK inhibitor. U0124 does not inhibit MEK at concentrations up to 100 μM .
|
-
-
- HY-110335
-
|
ROCK
|
Cancer
|
OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis .
|
-
-
- HY-U00441
-
DPBQ
1 Publications Verification
|
MDM-2/p53
Apoptosis
|
Cancer
|
DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells .
|
-
-
- HY-120951
-
|
Endonuclease
|
Cancer
|
PFM39, a Mirin analog, is a potent and selective MRE11 exonuclease inhibitor. PFM39 inhibits phosphate rotation for dsDNA exonuclease activity. PFM39 does not inhibit TmMre11 or human MRE11/MRN endonuclease activity .
|
-
-
- HY-130538
-
|
HDAC
|
Cancer
|
1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity .1-Naphthohydroxamic acid can induce tubulin acetylation .
|
-
-
- HY-16658B
-
Z-VAD(OH)-FMK
|
Caspase
Apoptosis
|
Cancer
|
Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM .
|
-
-
- HY-P3278
-
|
Proton Pump
|
Metabolic Disease
|
Caloxin 2A1 is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
|
-
-
- HY-112543
-
|
Influenza Virus
|
Infection
|
S119-8 is a broad spectrum inhibitor of influenza A and B viruses, showing activity against multiple influenza B viruses and an oseltamivir-resistant influenza A virus, but does not inhibit a non-influenza virus, vesicular stomatitis nirus (VSV) .
|
-
-
- HY-18963
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RG-14355
|
|
|
Lavendustin A (RG-14355) is a potent, selective and ATP-competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, with an IC50 of 11 nM. Lavendustin A does not inhibit protein kinase A or C. Lavendustin A can suppress VEGF-induced angiogenesis .
|
-
-
- HY-125143
-
|
MAGL
|
Metabolic Disease
|
ABC34 is an inactive control compound of JJH260. ABC34 does not inhibit the fluorophosphonate reactivity or fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1. ABC34 can inhibit both ABHD6 and PPT122 .
|
-
-
- HY-153540
-
|
Others
|
Others
|
AP-C4 is an inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 5.2. AP-C3 does not inhibit cGKII-dependent anion secretion .
|
-
-
- HY-10250A
-
TCN-P sodium
|
ATP Synthase
|
Metabolic Disease
|
Triciribine phosphate sodium inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate sodium also inhibits IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity .
|
-
-
- HY-141551
-
|
Estrogen Receptor/ERR
|
Cancer
|
GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research .
|
-
-
- HY-P2222
-
-
-
- HY-136194
-
-
-
- HY-136195
-
-
-
- HY-P3278A
-
|
Proton Pump
|
Metabolic Disease
|
Caloxin 2A1 TFA is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
|
-
-
- HY-P0190A
-
|
Potassium Channel
|
Others
|
Iberiotoxin (TFA) is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels .
|
-
-
- HY-100444
-
|
|
|
SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. SIS3 free base does not affect the phosphorylation of Smad2 .
|
-
-
- HY-14406A
-
|
|
|
L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent .
|
-
-
- HY-10250
-
TCN-P
|
ATP Synthase
|
Metabolic Disease
|
Triciribine phosphate (TCN-P) inhibits amidophosphoribosyltransferase by an allosteric mechanism which affects the first committed step of de novo purine biosynthesis. Triciribine phosphate also inhibits IMP dehydrogenase which is the first committed step of guanosine nucleotide synthesis. Tricilibine phosphate does not affect ligase activity .
|
-
-
- HY-149810
-
|
Bacterial
Parasite
|
Infection
|
AcrB-IN-2 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. AcrB-IN-22 inhibits Nile Red (a known substrate of AcrB) efflux.AcrB-IN-2 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
-
- HY-P5786
-
-
-
- HY-N7091S2
-
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
Atrazine-d5 is deuterium labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
-
- HY-P2222A
-
-
-
- HY-100536
-
|
|
|
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-116304
-
1G244
3 Publications Verification
|
Dipeptidyl Peptidase
Apoptosis
|
Cancer
|
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects .
|
-
-
- HY-110150
-
UNC3230
5 Publications Verification
|
Others
|
Inflammation/Immunology
Cancer
|
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects .
|
-
-
- HY-N7091S
-
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
Atrazine- 15N is the 15N-labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
-
- HY-123604A
-
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity .
|
-
-
- HY-W717329
-
|
Aminopeptidase
|
Cardiovascular Disease
|
EC33 is a selective aminopeptidase A (APA) inhibitor. EC33 blocks the pressor response of exogenous Ang II. EC33 does not cross the blood-brain barrier. EC33 has the potential for salt-dependent model of hypertension research .
|
-
-
- HY-10439
-
|
PGE synthase
|
Inflammation/Immunology
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX .
|
-
-
- HY-P5422
-
|
Calcium Channel
|
Others
|
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
|
-
-
- HY-126326
-
|
Epoxide Hydrolase
|
Metabolic Disease
|
SWE101 (compound 22 b) is a potent soluble epoxide hydrolase (sEH)-P inhibitor with IC50s of 4 μM and 2.8 μM for human and rat sEH-P, respectively. SWE101 does not inhibit neither hydrolase nor phosphatase activity of the mouse sEH .
|
-
- HY-136172
-
|
Ras
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation .
|
-
- HY-19384
-
E 6087
|
|
|
Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2). Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models .
|
-
- HY-123604
-
TH1834
1 Publications Verification
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity .
|
-
- HY-111014
-
|
Calcium Channel
|
Cardiovascular Disease
|
VK-II-36 is a carvedilol analog that suppresses sarcoplasmic reticulum Ca 2+release but does not block the β-receptor.VK-II-36 inhibits triggered activities evoked by both early and delayed after depolarizations .
|
-
- HY-N7091R
-
|
Others
|
Metabolic Disease
|
Atrazine (Standard) is the analytical standard of Atrazine. This product is intended for research and analytical applications. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term .
|
-
- HY-10403
-
-
- HY-149811
-
|
Bacterial
Parasite
|
Infection
|
Efflux pump-IN-3 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-3 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-3 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-149812
-
|
Bacterial
Parasite
|
Infection
|
Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-113628
-
VML-530
|
Leukotriene Receptor
|
Inflammation/Immunology
|
ABT-080 is an orally active inhibitor of leukotriene biosynthesis. ABT-080 simultaneously blocks the leukotriene pathways leading to the synthesis of LTB4 and LTC4, but does not inhibit PGH2 biosynthesis. ABT-080 can block bronchoconstriction and be used in the research of asthma and related inflammations
|
-
- HY-110249
-
CINPA1
1 Publications Verification
|
Constitutive Androstane Receptor
|
Metabolic Disease
|
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .
|
-
- HY-P4114
-
|
HIV
|
Others
|
TAT-NSF700scr consists the intact TAT domain and glycine linker, followed by the NSF amino acids in a random order. TAT-NSF700scr is used as a control peptide that does not inhibit SNAREmediated exocytosis .
|
-
- HY-149665
-
|
DGK
|
Cancer
|
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes .
|
-
- HY-15681
-
|
CDK
|
Cancer
|
Senexin A is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters .
|
-
- HY-15681A
-
|
CDK
|
Cancer
|
Senexin A hydrochloride is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters .
|
-
- HY-N8537
-
|
Fungal
|
Infection
|
Enfumafungin, a triterpene glycoside, is isolated from extracts derived from fungus Hormonema carpetanum. Enfumafungin is an antifungal compound that is acting on the fungal cell wall, as the (1,3)-beta-D-glucan synthase inhibitor. Enfumafungin is specific for yeasts and fungi (excluding Cryptococcus) and does not inhibit the growth of Bacillus subtilis .
|
-
- HY-157068
-
|
Ferroptosis
|
Cancer
|
icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition .
|
-
- HY-P0190
-
|
|
|
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels .
|
-
- HY-18832
-
|
|
|
AWL-II-38.3 is a potent ephrin-A receptor (EphA3) kinase inhibitor. AWL-II-38.3 does not exhibit significant cellular activity against Src-family kinases nor against b-raf .
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-
- HY-142619
-
|
Bacterial
|
Infection
|
TP0586352 is a LpxC inhibitor that is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk. TP0586352 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-113960
-
|
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 .
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-
- HY-13521
-
|
TGF-β Receptor
|
Cancer
|
SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-13521A
-
|
TGF-β Receptor
|
Cancer
|
SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-P1136B
-
-
- HY-136658
-
|
STAT
Apoptosis
|
Cancer
|
STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit kinase activity and has anticancer effects .
|
-
- HY-152108
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M pro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .
|
-
- HY-15290
-
AIM-100
3 Publications Verification
|
Ack1
|
Cancer
|
AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr 267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect .
|
-
- HY-103347
-
|
Apoptosis
|
Inflammation/Immunology
|
M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia .
|
-
- HY-14833
-
TP300
|
Topoisomerase
|
Cancer
|
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .
|
-
- HY-124257
-
D-Citronellol; (R)-(+)-β-Citronellol
|
Endogenous Metabolite
|
Inflammation/Immunology
|
(R)-Citronellol (D-Citronellol) is an alcoholic monoterpene found in geranium essential oil. (R)-Citronellol inhibits degranulation of mast cells and does not affect caffeine bitterness perception. (R)-Citronellol can be used in decorative cosmetics, toiletries as well as in non-cosmetic products .
|
-
- HY-128579
-
|
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-110114
-
|
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-15508
-
JANEX-1
4 Publications Verification
WHI-P131; Jak3 inhibitor I
|
JAK
|
Cancer
|
JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
|
-
- HY-P1136C
-
-
- HY-126972A
-
|
RAD51
|
Cancer
|
RI(dl)-2 TFA is a potent and selective RAD51-mediated D-loop formation inhibitor with an IC50 of 11.1 μM. RI(dl)-2 TFA does not influence RAD51 binding to ssDNA and inhibits homologous recombination (HR) activity in human cells (IC50 of 3.0 μM) .
|
-
- HY-114785
-
|
MMP
|
Cancer
|
BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with IC50s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC50s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects .
|
-
- HY-133016
-
|
MetAP
|
Cardiovascular Disease
Cancer
|
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM) . M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity .
|
-
- HY-139188
-
|
PI5P4K
|
Metabolic Disease
Cancer
|
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-12290
-
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
|
-
- HY-103381
-
|
CDK
GSK-3
|
Cancer
|
NSC693868 is a selective inhibitor of CDK1 and CDK5 with IC50s of 600 nM and 400 nM, respectively. NSC693868 less potently inhibits GSK3β with an IC50 of 1 µM) and does not block CDC25 activity. NSC693868 is used to help define the roles of CDK1 and CDK5 in various signaling pathways .
|
-
- HY-19747
-
HPOB
2 Publications Verification
|
HDAC
Apoptosis
|
Cancer
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6 .
|
-
- HY-156736
-
|
17β-HSD
|
Cancer
|
HSD17B13-IN-3 (compound 2) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor. HSD17B13-IN-3 does not have cell experimental activity .
|
-
- HY-13642
-
N-Phthalyl-L-tryptophan
|
DNA Methyltransferase
|
Cancer
|
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC50=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .
|
-
- HY-109785A
-
|
Bacterial
|
Infection
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-N7091S1
-
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
Atrazine- 13C3, 15N3 is the 13C-labeled and 15N-labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
- HY-149919
-
|
Parasite
|
Infection
|
Antimalarial agent 23 is an antimalarial benzimidazole with IC50s of 0.08 μM and 0.10 μM for PfNF54 and PfK1, respectively. Antimalarial agent 23 has potent β-hematin inhibition activity. Antimalarial agent 23 does not directly inhibit the conversion of heme to hemozoin .
|
-
- HY-116211
-
WIN-25978
|
Biochemical Assay Reagents
|
Neurological Disease
|
Amfonelic acid (WIN-25978) is a highly selective dopamine reuptake inhibitor. Amfonelic acid interferes with the in vitro neuronal uptake of norepinephrine in the iris of rats, but does not alter the concentrations of norepinephrine or dopamine in the whole mouse brain. Amfonelic acid can be used as a pharmacological tool to study the brain reward system, dopamine pathway and dopamine transporter .
|
-
- HY-163145
-
|
α-synuclein
|
Neurological Disease
|
α-Synuclein inhibitor 11 (compound 1) is a selective α-synuclein (α-syn) oligomer formation inhibitor. α-Synuclein inhibitor 11 does not inhibits tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synuclein inhibitor 11 can be used for Parkinson's disease (PD) research .
|
-
- HY-N2574
-
|
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-135841
-
|
Aldehyde Dehydrogenase (ALDH)
|
Metabolic Disease
Cancer
|
CM10 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC50s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity .
|
-
- HY-107345
-
Ombolan
|
Others
|
Inflammation/Immunology
|
Droxicam (Ombolan) is a non-steroidal anti-inflammatory agent, with strong analgesic activity. Droxicam acts by inhibiting PGE2 varies, and is characterised by being a pro-drug of Piroxicam (HY-B0253). Droxicam is well tolerated with slight side effects in the said mucosa. Droxicam does not show cardiovascular or respiratory effects in cats, and inhibits peritoneal capillary permeability in mouse .
|
-
- HY-110077
-
|
Akt
Apoptosis
|
Cancer
|
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL) .
|
-
- HY-12290A
-
RGDS peptide TFA; Fibronectin tetrapeptide TFA
|
Integrin
|
Inflammation/Immunology
|
Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1 .
|
-
- HY-W795264
-
|
Parasite
|
Infection
|
FR900098 is an antimalarial agent that inhibits 1-deoxy-d-xylulose-5-phosphate (DXP) reductoisomerase. FR900098 has no significant acute toxicity or genotoxicity, and does not have the ability to cause chromosome breakage or heterogeneity. FR900098 has no effect on bone marrow red blood cells in NMRI mice .
|
-
- HY-155077
-
|
JNK
|
Cancer
|
JNK-IN-12 (compound P2) is a mitochondrial-targeted JNK inhibitor (IC50=66.3 nM), consisting of a mitochondrial-specific cell-penetrating peptide and a specific inhibitor of JNK, SP600125 (HY-12041). JNK-IN-12 doesn't inhibit nuclear JNK signaling, but does inhibit mitochondrial JNK phosphorylation. JNK-IN-12 helps to improve the Parkinson's disease (PD) both in vitro and in vivo .
|
-
- HY-12646
-
|
Ras
Apoptosis
|
Cancer
|
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
|
-
- HY-12646A
-
|
Ras
Apoptosis
|
Cancer
|
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
|
-
- HY-124811
-
|
c-Myc
|
Cancer
|
IRES-C11 is a spectfic c-MYC internal ribosome entry site (IRES) translation inhibitor. IRES-C11 blocks the interaction of a requisite c-MYC IRES trans-acting factor, heterogeneous nuclear ribonucleoprotein A1, with its IRES. IRES-C11 does not inhibits BAG-1, XIAP and p53 IRESes .
|
-
- HY-145953
-
|
Others
|
Cancer
|
VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer .
|
-
- HY-151361
-
|
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-128439
-
|
DYRK
|
Cancer
|
BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway .
|
-
- HY-15643
-
|
TNF Receptor
Potassium Channel
|
Cancer
|
LY303511 is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K + currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
|
-
- HY-15643A
-
|
TNF Receptor
Potassium Channel
|
Cancer
|
LY 303511 hydrochloride is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K + currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.
|
-
- HY-122051
-
AC1903
1 Publications Verification
|
TRP Channel
|
Metabolic Disease
|
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model .
|
-
- HY-137457
-
IDX-1197
|
PARP
|
Cancer
|
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research .
|
-
- HY-114252
-
|
Na+/K+ ATPase
|
Cardiovascular Disease
|
Strophanthidin is a naturally available cardiac glycoside . Strophanthidin 0.1 and 1 nmol/L increases and 1~100 µmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal . Strophanthidin increases both diastolic and systolic intracellular Ca 2+ concentration .
|
-
- HY-P3463
-
GLP-1 (human)
|
GCGR
|
Metabolic Disease
Inflammation/Immunology
|
Beinaglutide is a human GLP-1 polypeptide that shares almost 100% homology with human GLP-1 (7–36). Beinaglutide displays does-dependent effects in glycemic control, inhibiting food intake and gastric empty and promoting weight loss. Beinaglutide has the potential for the research of overweight/obesity and nonalcoholic steatohepatitis (NASH) .
|
-
- HY-147071
-
DAPE
|
Liposome
|
Metabolic Disease
|
1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine (DAPE) is a phospholipid phosphatidylethanolamine. Unlike other phospholipid phosphatidylethanolamines, 1,2-Diarachidonoyl-sn-glycero-3-phosphoethanolamine has no significant effect on protein phosphatase PP2A activity and does not inhibit insulin-stimulated GLUT4 translocation .
|
-
- HY-122817
-
|
Antibiotic
Parasite
|
Infection
|
FR900098 sodium is an antimalarial agent that inhibits 1-deoxy-d-xylulose-5-phosphate (DXP) reductoisomerase. FR900098 sodium has no significant acute toxicity or genotoxicity, and does not have the ability to cause chromosome breakage or heterogeneity. FR900098 sodium has no effect on bone marrow red blood cells in NMRI mice .
|
-
- HY-N6701
-
|
Arp2/3 Complex
|
Cancer
|
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport . Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis . Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca 2+increase in the mucosal scrapings .
|
-
- HY-16576A
-
TCS-PIM-1-4a
|
Pim
|
Cancer
|
SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity .
|
-
- HY-110261
-
|
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-144724
-
|
HSP
Apoptosis
|
Cancer
|
HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC50 value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis .
|
-
- HY-100360
-
|
Histone Methyltransferase
|
Cancer
|
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-129056
-
|
Thrombin
|
Cardiovascular Disease
|
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia . Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion .
|
-
- HY-Z0283
-
Benzenecarboxamide; Phenylamide
|
Endogenous Metabolite
PARP
|
Others
|
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
|
-
- HY-100360A
-
|
Histone Methyltransferase
|
Cancer
|
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-14521
-
DDATHF
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
|
-
- HY-14521B
-
DDATHF hydrate
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
|
-
- HY-126396
-
|
CaMK
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
Sordarin is a potent diphthamide-dependent eEF2 inhibitor with antifungal properties. Sordarin targets eEF2 so as to inhibit protein translation by blocking eEF2-mediated translocation of tRNAs. Sordarin inhibits translation specifically in certain fungi (e.g. C. albicans, C. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae) .
|
-
- HY-18944
-
|
|
|
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
|
-
- HY-144261
-
|
Beta-lactamase
Bacterial
|
Infection
|
Metallo-β-lactamase-IN-3 (compound 35) is a potent metallo-β-lactamases (MBL) inhibitor. Metallo-β-lactamase-IN-3 shows high activity against VIM-1 and NDM-1, with IC50 of 0.6 and 1.0 μM, respectively. Metallo-β-lactamase-IN-3 does not show inhibition of IMP-7 .
|
-
- HY-A0170
-
|
|
|
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
|
-
- HY-103399
-
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1 .
|
-
- HY-123981
-
|
Phosphatase
|
Cancer
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
- HY-14521A
-
DDATHF disodium
|
Antifolate
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor .
|
-
- HY-146459
-
|
Akt
|
Cancer
|
Akt1-IN-1 (compound 5b) is a potent and selective Akt1 inhibitor with an IC50 value of 18.79 nM in MIA Paca-2 cells. Akt1-IN-1 does not exhibit obvious teratogenicity, hepatotoxicity and cardiotoxicity (No Observed Adverse Effect Level > 100 µM). Akt1-IN-1 can be used for researching anticancer .
|
-
- HY-137975
-
|
Others
|
Endocrinology
|
Exo2 is a secretion inhibitor. Exo2 perturbs trafficking of Shiga toxin between endosomes and the trans-Golgi network. Exo2 blocks secretory cargo exit from the ER (endoplasmic reticulum) and disrupts the Golgi apparatus, but does not affect the morphology of the TGN (trans-Golgi network) Exo2 can stimulate calcium-dependent exocytosis in permeabilized adrenal chromaff in cells .
|
-
- HY-153663
-
|
Ras
|
Cancer
|
TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM .
|
-
- HY-116871
-
|
CDK
|
Cancer
|
YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 WT and Cdk7 as, although Cdk7 as is relatively resistant to this compound as well .
|
-
- HY-157131
-
|
TRP Channel
|
Neurological Disease
|
TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca 2+ influx in macrophages, and inhibits macrophage phagocytosis .
|
-
- HY-124798
-
|
mTOR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity .
(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
|
-
- HY-15648A
-
GSK-J2
2 Publications Verification
|
Others
|
Cancer
|
GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
|
-
- HY-124691
-
D-I03
2 Publications Verification
|
DNA/RNA Synthesis
|
Cancer
|
D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin .
|
-
- HY-150622
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent nsp13 (non-structural protein 13) inhibitor. SARS-CoV-2 nsp13-IN-1 only inhibits nsp13 ssDNA + ATPase, with an IC50 of 6 μM. SARS-CoV-2 nsp13-IN-1 does not inhibit ssDNA - ATPase. SARS-CoV-2 nsp13-IN-1 can be used for COVID-19 research .
|
-
- HY-149208
-
|
HDAC
Apoptosis
|
Cancer
|
HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer .
|
-
- HY-155300
-
|
Leukotriene Receptor
|
Inflammation/Immunology
|
BLT2 antagonist-1 (compound 15b) is a selective BLT2 antagonist that inhibits the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM. BLT2 antagonist-1 does not inhibits the chemotaxis of CHO-BLT1 cells. BLT2 antagonist-1 also inhibits the binding of LTB4 and BLT2 with a Ki value of 132 nM. BLT2 antagonist-1 can be used for the research of the inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease .
|
-
- HY-145749
-
|
PARP
|
Cancer
|
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells .
|
-
- HY-123076
-
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-133033
-
|
Others
|
Metabolic Disease
|
COQ7-IN-1, a highly potent inhibitor of human coenzyme Q (COQ7), interferes with ubiquinone (UQ) synthesis. COQ7-IN-1 does not disturb physiological cell growth of human normal culture cells. COQ7-IN-1 can be used for the research of the balance between UQ supplementation pathways: de novo UQ synthesis and extracellular UQ uptake .
|
-
- HY-145827
-
|
Microtubule/Tubulin
|
Cancer
|
KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity .
|
-
- HY-110056
-
|
CRFR
|
Neurological Disease
|
NBI 35965 hydrochloride is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 hydrochloride does not inhibit CRF2. NBI 35965 hydrochloride reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 hydrochloride shows anxiolytic effects .
|
-
- HY-106005
-
|
Parasite
PI4K
|
Infection
|
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kd app=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent .
|
-
- HY-100277
-
SR-202
|
PPAR
|
Metabolic Disease
|
Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
|
-
- HY-110105
-
|
Potassium Channel
|
Neurological Disease
|
NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively) .
|
-
- HY-N6785
-
|
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
|
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation .
|
-
- HY-N6785A
-
|
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
|
Okadaic acid sodium, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid (sodium) has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid sodium increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid sodium induces tau phosphorylation .
|
-
- HY-144123
-
|
HIV
|
Infection
|
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
|
-
- HY-12755
-
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
|
-
- HY-131404
-
|
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-128341
-
|
ERK
|
Cardiovascular Disease
Cancer
|
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
|
-
- HY-110282
-
|
Oxidative Phosphorylation
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-103378
-
|
CRFR
|
Neurological Disease
|
NBI 35965 methanesulfonate is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a Ki value of 4 nM and a pKi value of 8.5. NBI 35965 methanesulfonate does not inhibit CRF2. NBI 35965 methanesulfonate reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC50 values of 7.1 and 6.9, respectively. NBI 35965 methanesulfonate shows anxiolytic effects .
|
-
- HY-162390
-
|
Amylases
Glucosidase
|
Endocrinology
|
α-Amylase/α-Glucosidase-IN-11 (Compound 5d) is a isoxazolidine-isatin hybrid with significant antidiabetic activity. α-Amylase/α-Glucosidase-IN-11 competitively inhibits α-amylase (IC50 = 30.39 μM) and α-glucosidase (IC50 = 65.1 μM), two key digestive enzymes. α-Amylase/α-Glucosidase-IN-11 does not cross the blood-brain barrier .
|
-
- HY-115760
-
|
Phosphatase
|
Neurological Disease
Cancer
|
Okadaic acid ammonium salt, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid ammonium salt has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid ammonium salt increases of phosphorylation of a number of proteins by inhibiting PP, and acts as a tumor promoter. Okadaic acid ammonium salt induces tau phosphorylation .
|
-
- HY-156237
-
|
Autophagy
|
Others
|
Beclin1-ATG14L interaction inhibitor 1 (com 19) is a selective Beclin1-ATG14L interaction inhibitor. This protein interaction mechanism specifically targets complex I of the lipid kinase VPS34 without affecting complex II. Because the integrity of VPS34 complex II depends on the Beclin 1-UVRAG interaction. Beclin1-ATG14L interaction inhibitor 1 can disrupt the formation of VPS34 complex I and inhibit autophagy, but does not affect complex II-related vesicle transport .
|
-
- HY-117724
-
|
PAI-1
|
Cardiovascular Disease
|
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay .
|
-
- HY-10256
-
Adezmapimod
Maximum Cited Publications
408 Publications Verification
SB 203580; RWJ 64809
|
Organoid
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
|
-
- HY-149269
-
|
COX
Carbonic Anhydrase
LOX-1
|
Inflammation/Immunology
|
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
|
-
- HY-145102
-
|
HSP
Apoptosis
|
Cancer
|
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
|
-
- HY-118119
-
|
PGE synthase
|
Cancer
|
CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
|
-
- HY-W728005
-
|
SARS-CoV
|
Infection
|
Covidcil-19 (compound C5) avidly binds to the revised attenuator hairpin structure of the SARS-CoV-2 frameshifting element (FSE) with a Kd of 11 nM. Covidcil-19 stabilizes the hairpin’s folded state and impairs frameshifting in cells. Covidcil-19 reduces frameshifting efficiency of the SARS-CoV-2 FSE and does not affect SARS-CoV-2 FSE RNA levels. Covidcil-19 inhibits a process essential for SARS-CoV-2 viral propagation .
|
-
- HY-160477
-
|
PIKfyve
NF-κB
IKK
|
Inflammation/Immunology
|
DC-SX029 is a potent SNX10 protein-protein interaction (PPI) inhibitor with an estimated KD constant of ~0.935 μM by surface plasmon resonance (SPR). DC-SX029 blocks the SNX10-PIKfyve interaction, thereby decreased the TBK1/c-Rel signaling activation. DC-SX029 does not affect the protein level of SNX10. DC-SX029 has the potential for inflammatory bowel disease (IBD) research .
|
-
- HY-15648I
-
|
Others
|
Cancer
|
GSK-J2 sodium is the sodium form of GSK-J2 (HY-15648A). GSK-J2 is an isomer of GSK-J1, and does not have any specific activity. GSK-J1 (HY-15648) is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A .
|
-
- HY-155983
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 nsp14-IN-4 (Compound 12q) is a selective SARS-CoV-2 nsp14 methyltransferase inhibitor with an IC50 value of 19 ± 2.5 nM. SARS-CoV-2 nsp14-IN-4 (Compound 12q) do not have a zwitterionic character and can penetrate into cells. SARS-CoV-2 nsp14-IN-4 (Compound 12q) can be used for COVID-19 and its causative agent SARS-CoV-2 research .
|
-
- HY-P990090
-
CBP-201
|
Interleukin Related
|
Inflammation/Immunology
|
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
|
-
- HY-162373
-
|
Amylases
Glucosidase
P-glycoprotein
|
Metabolic Disease
|
α-Amylase/α-Glucosidase-IN-10 (compound 5d) is an α-amylase and α-glucosidase inhibitor (IC50: 30.39 μM and 65.1 μM) with potential diabetes inhibitory effects. α-Amylase/α-Glucosidase-IN-10 exhibits high gastrointestinal (GI) absorption in ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) prediction. While α-Amylase/α-Glucosidase-IN-10 acts as a substrate for P-gp and does not cross the blood-brain barrier (BBB), there may be a risk of central nervous system side effects .
|
-
- HY-130311
-
2-Monolinolein; 2-Monolinoleoylglycerol
|
Cannabinoid Receptor
|
Neurological Disease
|
2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
|
-
-
-
HY-L083
-
|
2068 compounds
|
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.
MCE provides a unique collection of 2068 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3278A
-
|
Proton Pump
|
Metabolic Disease
|
Caloxin 2A1 TFA is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 TFA does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
|
-
- HY-P0190A
-
|
Potassium Channel
|
Others
|
Iberiotoxin (TFA) is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels .
|
-
- HY-P3278
-
|
Proton Pump
|
Metabolic Disease
|
Caloxin 2A1 is an extracellular plasma membrane Ca 2+-ATPase (PMCA) peptide inhibitor. Caloxin 2A1 does not affect basal Mg 2+-ATPase or Na +-K +-ATPase .
|
-
- HY-118534
-
BRN-2209058
|
Peptides
|
Endocrinology
|
Cyclobutyrol is a potent choleretic agent. Cyclobutyrol also inhibits biliary lipid secretion. Cyclobutyrol induces choleretic is unrelated to bile acids. Cyclobutyrol and bile acids do not compete for the hepatobiliar transport mechanisms[1]
|
-
- HY-P2222
-
-
- HY-P5786
-
-
- HY-P2222A
-
-
- HY-P5422
-
|
Calcium Channel
|
Others
|
Caloxin 3A1 is a biological active peptide. (This peptide belongs to caloxins, the extracellular plasma membrane (PM) Ca2+ pump inhibitors. Caloxin 3A1 inhibits plasma membrane calcium pumps (PMCAs) but not the sarcoplasmic reticulum Ca2+-pump. This peptide does not inhibit formation of the acylphosphate intermediate from ATP.)
|
-
- HY-P4114
-
|
HIV
|
Others
|
TAT-NSF700scr consists the intact TAT domain and glycine linker, followed by the NSF amino acids in a random order. TAT-NSF700scr is used as a control peptide that does not inhibit SNAREmediated exocytosis .
|
-
- HY-P1136B
-
-
- HY-P1136C
-
-
- HY-12290
-
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
|
-
- HY-12290A
-
RGDS peptide TFA; Fibronectin tetrapeptide TFA
|
Integrin
|
Inflammation/Immunology
|
Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1 .
|
-
- HY-P3463
-
GLP-1 (human)
|
GCGR
|
Metabolic Disease
Inflammation/Immunology
|
Beinaglutide is a human GLP-1 polypeptide that shares almost 100% homology with human GLP-1 (7–36). Beinaglutide displays does-dependent effects in glycemic control, inhibiting food intake and gastric empty and promoting weight loss. Beinaglutide has the potential for the research of overweight/obesity and nonalcoholic steatohepatitis (NASH) .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P990090
-
CBP-201
|
Interleukin Related
|
Inflammation/Immunology
|
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N8537
-
-
-
- HY-124257
-
-
-
- HY-N2574
-
-
-
- HY-N8659
-
-
-
- HY-119874
-
-
-
- HY-114252
-
-
-
- HY-Z0283
-
-
-
- HY-N6785
-
|
Structural Classification
Animals
Ketones, Aldehydes, Acids
Marine natural products
Source classification
Other marine organisms
|
Phosphatase
Apoptosis
|
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-N7091S2
-
|
Atrazine-d5 is deuterium labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
-
- HY-50683S
-
|
JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
|
-
-
- HY-N7091S
-
|
Atrazine- 15N is the 15N-labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
-
- HY-N7091S1
-
|
Atrazine- 13C3, 15N3 is the 13C-labeled and 15N-labeled Atrazine. Atrazine is principally used for control of certain annual broadleaf and grass weeds. Atrazine inhibits photophosphorylation but typically does not result in lethality or permanent cell damage in the short term[1].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-116423
-
|
|
Alkynes
|
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145749
-
|
|
Alkynes
|
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells .
|
-
- HY-116423A
-
|
|
Alkynes
|
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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