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Results for "

allosteric mechanism

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Angiotensin-converting Enzyme (ACE) (1) ATP Synthase (3) Bacterial (1) Cholinesterase (ChE) (1) DNA/RNA Synthesis (1) Dopamine Transporter (1) E1/E2/E3 Enzyme (2) Endogenous Metabolite (2) Enterovirus (1) Filovirus (1) GABA Receptor (1) HCN Channel (1) HIV (2) iGluR (1) Interleukin Related (1) Isotope-Labeled Compounds (1) LXR (1) mAChR (3) Molecular Glues (1) NAMPT (1) NF-κB (1) p97 (1) PARP (1) PPAR (1) Reference Standards (1) RSV (1) RXFP Receptor (1) SARS-CoV (1) Serotonin Transporter (1) Smo (1)
By Research Areas:	Cancer (8) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (1) Metabolic Disease (5) Neurological Disease (5)

By Targets:

Angiotensin-converting Enzyme (ACE) (1)

ATP Synthase (3)

Bacterial (1)

Cholinesterase (ChE) (1)

DNA/RNA Synthesis (1)

Dopamine Transporter (1)

E1/E2/E3 Enzyme (2)

Endogenous Metabolite (2)

Enterovirus (1)

Filovirus (1)

GABA Receptor (1)

HCN Channel (1)

HIV (2)

iGluR (1)

Interleukin Related (1)

Isotope-Labeled Compounds (1)

LXR (1)

mAChR (3)

Molecular Glues (1)

NAMPT (1)

NF-κB (1)

p97 (1)

PARP (1)

PPAR (1)

Reference Standards (1)

RSV (1)

RXFP Receptor (1)

SARS-CoV (1)

Serotonin Transporter (1)

Smo (1)

By Research Areas:

Cancer (8)

Cardiovascular Disease (2)

Infection (2)

Inflammation/Immunology (1)

Metabolic Disease (5)

Neurological Disease (5)

Inhibitors & Agonists

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-16940

24(S)-Hydroxycholesterol 24S-OHC; 24S-HC; Cerebrosterol	LXR iGluR Endogenous Metabolite	Metabolic Disease
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .

HY-12316

20(S)-Hydroxycholesterol 3 Publications Verification 20α-Hydroxycholesterol	Smo Endogenous Metabolite	Cardiovascular Disease Metabolic Disease Cancer
20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC₅₀ of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the Raf/MEK/ERK pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis .

HY-P99171

Gevokizumab 2 Publications Verification	Interleukin Related	Inflammation/Immunology Cancer
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .

HY-175750

MOMA-341	DNA/RNA Synthesis	Cancer
MOMA-341 is a selective Werner RecQ like helicase (WRN) inhibitor. MOMA-341 binds to WRN at cysteine 727 through an allosteric and ATP-competitive binding mechanism. MOMA-341 has antitumor activity and can be used for advanced and metastatic solid tumors research .

HY-108708

GeA-69	PARP	Cancer
GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a K_d value of 2.1 μM. GeA-69 involves in DNA damage repair mechanisms and prevents recruitment of PARP14 MD2 to sites of laser-induced DNA damage .

HY-49444

EN450	NF-κB Molecular Glues E1/E2/E3 Enzyme	Cancer
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .

HY-107111

GSK1034702	mAChR	Neurological Disease
GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-161296

TH6342	Bacterial HIV	Infection
TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe .

HY-118967

VUANT1 VU0183254	HCN Channel	Others
VUANT1 (VU0183254) is an allosteric antagonist of insect odorant receptor ion channels, which has the activity of inhibiting insect odorant receptor signaling. VUANT1 can inhibit the activation of insect odorant receptors through allosteric regulation, which is important for the study of the molecular mechanism of insect olfactory signaling. Although it may be of limited use in insect control programs, it can be used as a pharmacological tool to study related mechanisms.

HY-162401

AZ7976	RXFP Receptor	Cardiovascular Disease
AZ7976 (Compound 42) is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1) (pEC₅₀ > 10.5). AZ7976 enhances RXFP1's cAMP signaling through an allosteric mechanism, thereby physiologically increasing heart rate. AZ7976 can be used in the field of cardiovascular disease research .

HY-10250

Triciribine phosphate TCN-P	ATP Synthase	Metabolic Disease Cancer
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-10250A

Triciribine phosphate sodium TCN-P sodium	ATP Synthase	Metabolic Disease Cancer
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-126158

SRI-29574	Dopamine Transporter Serotonin Transporter	Neurological Disease
SRI-29574 is an allosteric modulator of the dopamine transporter (DAT). SRI-29574 partially inhibits the uptake of the DAT (IC₅₀=2.3 nM) and also partially inhibits the uptake of the serotonin transporter (SERT) and norepinephrine transporter (NET). SRI-29574 may serve as a useful probe to study the function and regulatory mechanisms of DAT .

HY-10250S1

Triciribine phosphate-d3 TCN-P-d₃	Isotope-Labeled Compounds ATP Synthase	Metabolic Disease
Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity .

HY-107111A

GSK1034702 hydrochloride	Cholinesterase (ChE) mAChR	Neurological Disease
GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-117106

PNU-107484A	GABA Receptor	Others
PNU-107484A is a GABA_A receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl ^- currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .

HY-182062

NAMPT activator-9	NAMPT E1/E2/E3 Enzyme	Neurological Disease
NAMPT activator-9 (Compound DIPM) is an allosteric, non-competitive NAMPT activator, with an EC₅₀ of 3.366 μM against hNAMPT. NAMPT activator-9 enhances the enzymatic activity of NAMPT via an allosteric, non-competitive mechanism. NAMPT activator-9 increases intracellular NAD ⁺ levels. NAMPT activator-9 restores myotube diameter and reduces the expression of atrophy markers Atrogin-1 and MuRF1. NAMPT activator-9 is applicable to research related to muscle atrophy .

HY-122222

MRL20	PPAR	Others
MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC₅₀ being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC₅₀ values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ .

HY-124253

SMDC818909	p97	Cancer
SMDC818909 is an indole amide-derived uncompetitive inhibitor targeting p97 AAA+ ATPase, with an IC₅₀ of 3.5 μM and a K_a of 9.1 μM. SMDC818909 binds to the D2 ATPase domain of p97, preferentially associates with the ADP-bound conformation of p97, allosterically blocks the ATP hydrolysis cycle of p97, and inhibits its mediated intracellular protein homeostasis regulatory function. SMDC818909 is applied to the research and development of p97-targeted antitumor drugs, as well as studies on cancer-related proteotoxic stress mechanisms .

HY-107111R

GSK1034702 (Standard)	Reference Standards mAChR	Neurological Disease
GSK1034702 (Standard) is the analytical standard of GSK1034702 (HY-107111). This product is intended for research and analytical applications. GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-179634

ASF-006 sodium	SARS-CoV HIV Enterovirus Angiotensin-converting Enzyme (ACE) RSV Filovirus	Infection
ASF-006 sodium, a tetrapodal tryptophan derivative, is a potent viral invasion inhibitor. ASF-006 sodium shows potent antiviral activity against different SARS-CoV-2 Omicron variants but not against the ancestral SARS-CoV.2 strain (Wuhan-Hu-1). ASF-006 sodium competitively inhibits receptor-binding domain (RBD)-ACE2 binding via an allosteric mechanism. ASF-006 sodium inhibits Omicron BA.1, Omicron XBB.1.5, respiratory syncytial virus (RSV) and Ebola virus infection with IC₅₀s of 0.02 μM, 0.3 μM, 1.52 μM and 0.2 μM, respectively. ASF-006 sodium inhibits cell entry of both HIV and enterovirus A71[1].

Cat. No.	Product Name	Target	Research Area	Image

HY-P99171

Gevokizumab 2 Publications Verification	Interleukin Related	Inflammation/Immunology Cancer
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-16940

24(S)-Hydroxycholesterol 24S-OHC; 24S-HC; Cerebrosterol	Classification of Application Fields Disease markers Metabolic Disease Nervous System Disorder Endogenous metabolite Disease Research Fields Steroids Source Classification	LXR iGluR Endogenous Metabolite
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .

HY-12316

20(S)-Hydroxycholesterol 3 Publications Verification 20α-Hydroxycholesterol	Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification Cancer	Smo Endogenous Metabolite
20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC₅₀ of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the Raf/MEK/ERK pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis .

Cat. No.	Product Name	Chemical Structure

HY-10250S1

Triciribine phosphate-d3
Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity .

Triciribine phosphate-d3

Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity .

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