Search Result

Results for "

ligand-binding domain

" in MedChemExpress (MCE) Product Catalog:

By Targets:	FKBP (1) Ligands for Target Protein for PROTAC (1) Androgen Receptor (3) Apoptosis (3) Aryl Hydrocarbon Receptor (1) Cytochrome P450 (1) Endogenous Metabolite (2) Ephrin Receptor (2) Estrogen Receptor/ERR (8) Ferroptosis (5) Glycosidase (2) Histone Methyltransferase (6) IGF-1R (1) iGluR (3) Interleukin Related (1) Isotope-Labeled Compounds (2) LOX-1 (1) nAChR (1) Nuclear Hormone Receptor 4A/NR4A (6) Orphan Receptor (2) Parasite (6) PPAR (10) RAR/RXR (1) ROR (2) Transmembrane Glycoprotein (1) TSH Receptor (1) VD/VDR (1)
By Research Areas:	Cancer (21) Cardiovascular Disease (1) Endocrinology (2) Infection (6) Inflammation/Immunology (10) Metabolic Disease (13) Neurological Disease (11)

By Targets:

FKBP (1)

Ligands for Target Protein for PROTAC (1)

Androgen Receptor (3)

Apoptosis (3)

Aryl Hydrocarbon Receptor (1)

Cytochrome P450 (1)

Endogenous Metabolite (2)

Ephrin Receptor (2)

Estrogen Receptor/ERR (8)

Ferroptosis (5)

Glycosidase (2)

Histone Methyltransferase (6)

IGF-1R (1)

iGluR (3)

Interleukin Related (1)

Isotope-Labeled Compounds (2)

LOX-1 (1)

nAChR (1)

Nuclear Hormone Receptor 4A/NR4A (6)

Orphan Receptor (2)

Parasite (6)

PPAR (10)

RAR/RXR (1)

ROR (2)

Transmembrane Glycoprotein (1)

TSH Receptor (1)

VD/VDR (1)

By Research Areas:

Cancer (21)

Cardiovascular Disease (1)

Endocrinology (2)

Infection (6)

Inflammation/Immunology (10)

Metabolic Disease (13)

Neurological Disease (11)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Targets Recommended:

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13956S

Pioglitazone-d4 U 72107-d₄	PPAR Ferroptosis	Metabolic Disease Cancer
Pioglitazone-d₄ is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].

HY-13956

Pioglitazone Maximum Cited Publications 31 Publications Verification U 72107	PPAR Ferroptosis	Metabolic Disease Cancer
Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .

HY-P10579

123B9	Ephrin Receptor	Cancer
123B9, a tumor-homing agent, is a potent and selective EphA2 agonist with a K_d value of 4.0 μM. 123B9 selectively targets the EphA2 tyrosine kinase receptor ligand-binding domain. 123B9 does not appreciably inhibit the ligand binding domains of the most closely related EphA3 and EphA4 receptors .

HY-108822

Rilonacept Arcalyst; IL 1 Trap; Interleukin 1 Trap	Interleukin Related	Inflammation/Immunology
Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes .

HY-13956S1

Pioglitazone-d4 (alkyl)	Isotope-Labeled Compounds PPAR Ferroptosis	Metabolic Disease Cancer
Pioglitazone-d₄ (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].

HY-13956B

Pioglitazone potassium U 72107 potassium	PPAR Ferroptosis	Metabolic Disease Cancer
Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .

HY-13956C

(R)-Pioglitazone (R)-U 72107	PPAR	Neurological Disease
(R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease .

HY-13956R

Pioglitazone (Standard)	PPAR Ferroptosis	Metabolic Disease Cancer
Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .

HY-116205

UBP684	iGluR	Others
UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.

HY-P10430

Stalk peptide	Transmembrane Glycoprotein	Neurological Disease
Stalk peptide is a GPR110 activator. Stalk peptide is released from GPCR Autoproteolysis INducing domain by autocatalytic process and then Stalk peptide is inserted into the ligand-binding pocket of the receptor to activate the receptor. Stalk peptide can promote nerve growth and synaptic formation. Stalk peptide can be used to study neurodevelopmental and neurodegenerative diseases .

HY-162738

JMV6944	Cytochrome P450 Ligands for Target Protein for PROTAC	Cancer
JMV6944 is a PXR agonist. JMV6944 competitively inhibits hPXR ligand-binding domain (LBD) binding to PXR with an IC₅₀ of 680nM. JMV6944 induces CYP3A4 mRNA expression in freshly isolated human primary human hepatocyte cultures. JMV6944 can be used for the synthesis of PROTAC PXR degrader JMV7048 (HY-162704) .

HY-111254

GQ-16	PPAR	Metabolic Disease
GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a K_i of 160 nM. GQ-16 is an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ. GQ-16 is a partial agonist of PPARγ with reduced adipogenic actions. GQ-16 promotes insulin Sensitization without weight gain .

HY-170874

PPARγ modulator-2	PPAR	Metabolic Disease
PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC₅₀ of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models .

HY-136242

UT-34	Estrogen Receptor/ERR	Endocrinology Cancer
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC₅₀ values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.

HY-121372

Lactandrate	Estrogen Receptor/ERR	Cancer
Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI₅₀ value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .

HY-117182

LG190178	Apoptosis VD/VDR RAR/RXR	Metabolic Disease Inflammation/Immunology Cancer
LG190178 is a non-steroidal vitamin D receptor (VDR) ligand that can induce the formation of heterodimer complexes between VDR and retinoid X receptor (RXR), stabilizing the agonistic conformation of the VDR ligand-binding domain and promoting its interaction with co-activators. LG190178 has functions in regulating calcium homeostasis, bone mineralization, as well as cell proliferation, differentiation, and apoptosis, making it useful for research in psoriasis, osteoporosis, and cancer .

HY-132205

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

HY-122742

HBT1	iGluR	Neurological Disease
HBT1 is a potent α-Amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor (AMPA-R) potentiator. HBT1 bonds with S518 in the ligand-binding domain (LBD) of AMPA-R in a glutamate-dependent manner. HBT1 did not show remarkable bell-shaped response in brain-derived neurotrophic factor (BDNF) production in primary neurons .

HY-P2264

KYL peptide	Ephrin Receptor	Inflammation/Immunology
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor (IC₅₀:4.22 μM, Kd:1.3 μM). KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses .

HY-143201

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

HY-N2025

Oroxin A	PPAR Glycosidase	Metabolic Disease
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .

HY-N2025R

Oroxin A (Standard)	PPAR Glycosidase	Metabolic Disease
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .

HY-156190

NR2F2-IN-1	Orphan Receptor	Cancer
NR2F6 modulator-2 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F6 modulator-2 substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F6 modulator-2 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .

HY-156190A

NR2F2-IN-1 free base	Orphan Receptor	Cancer
NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .

HY-D1398

LtIA-F	nAChR	Neurological Disease
LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.

HY-23999

BI-0115	LOX-1	Cardiovascular Disease
BI-0115 is a selective inhibitor of LOX-1 (IC₅₀=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain .

HY-120210

XY018	ROR	Inflammation/Immunology Cancer
XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC₅₀, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .

HY-110392

CMP8	Estrogen Receptor/ERR	Cancer
CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC₅₀ values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively .

HY-109176

Giredestrant 5 Publications Verification GDC-9545; RG6171	Estrogen Receptor/ERR	Cancer
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity .

HY-135903

Giredestrant tartrate GDC-9545 tartrate; RG6171 tartrate	Estrogen Receptor/ERR	Cancer
Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity .

HY-113646

Shield-2	FKBP	Others
Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .

HY-164552

ZNU-IMB-Z15	Apoptosis Androgen Receptor	Cancer
ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .

HY-159922

AR antagonist 9	Androgen Receptor	Cancer
AR antagonist 9 is an orally bioavailable selective androgen receptor (AR) antagonist that exerts anticancer effects by disrupting the dimerization of AR ligand-binding domains, showing potential for overcoming drug resistance in prostate cancer (PCa). Its AR antagonistic activity has an IC₅₀ value of 0.051 μM, comparable to Enzalutamide (HY-70002) (IC₅₀ = 0.060 μM). AR antagonist 9 demonstrated superior efficacy against AR_F876L/T877A and AR_W741C mutants compared to Enzalutamide (HY-70002). Furthermore, AR antagonist 9 exhibited favorable pharmacokinetic properties, with an oral bioavailability of F = 66.24% in rats. In the LNCaP xenograft mouse model, oral administration of AR antagonist 9 significantly inhibited tumor growth. AR antagonist 9 holds promise for research into overcoming PCa drug resistance .

HY-B1322A

Amodiaquine 5+ Cited Publications Amodiaquin	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-B1322

Amodiaquine dihydrochloride dihydrate 5+ Cited Publications Amodiaquin dihydrochloride dihydrate	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-14422

SR1078 10+ Cited Publications	ROR	Cancer
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .

HY-B1322B

Amodiaquine dihydrochloride 5+ Cited Publications Amodiaquin dihydrochloride	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a K_i of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-B1322AS

Amodiaquine-d10	Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine-d₁₀ is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect[1][2][3][4].

HY-B1322AS1

Amodiaquine-d10 hydrochloride Amodiaquin-d₁₀	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase Isotope-Labeled Compounds	Infection Neurological Disease Inflammation/Immunology
Amodiaquine-d₁₀ hydrochloride is deuterated labeled Amodiaquine (HY-B1322A). Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-164373

SC428	Androgen Receptor Apoptosis	Cancer
SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .

HY-W677684

Nurr1 agonist 2	Nuclear Hormone Receptor 4A/NR4A	Others
Nurr1 agonist 2 (Compound 7) is a Nurr1 agonist (EC₅₀: 0.07 μM). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand binding domain (LBD) with a K_d value of 0.14 μM. Nurr1 agonist 2 increases the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) mRNA expression .

HY-B1322R

Amodiaquine (dihydrochloride dihydrate) (Standard)	Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase	Infection Neurological Disease Inflammation/Immunology
Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect .

HY-P99165

Teprotumumab 1 Publications Verification	IGF-1R TSH Receptor	Endocrinology
Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research .

HY-141551

GNE-274	Estrogen Receptor/ERR	Cancer
GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.

HY-133830

7α,24(S)-Dihydroxycholesterol (3β,7α,24S)-Cholest-5-ene-3,7,24-triol	Endogenous Metabolite	Others
7α,24(S)-Dihydroxycholesterol ((3β,7α,24S)-Cholest-5-ene-3,7,24-triol) serves as a ligand for liver X receptor (LXR), binding specifically to the ligand binding domains of both LXRα and LXRβ. This compound is synthetically produced from E-α,β-enone, utilizing Arsonium ylide and J-tert-butyldimethylsilyloxy-bisnor-5-cholenaldehyde as starting materials, followed by a series of transformations to yield 7α,24(S)-dihydroxycholesterol.

HY-148611

NSC339614 potassium	iGluR	Neurological Disease
NSC339614 potassium is a selective GluN1/GluN2C and GluN1/GluN2D receptor enhancer with the activity of enhancing neuronal responses to specific NMDA receptors. NSC339614 potassium can selectively enhance the signaling of GluN1/GluN2C and GluN1/GluN2D receptors without affecting other NMDA receptors. The mechanism of action of NSC339614 potassium does not compete with agonists of L-glutamate or glycine, nor does it depend on membrane potential. The activity of NSC339614 potassium depends on the specific structure of the agonist ligand binding domain, showing its potential as a novel pharmacological agent for studying the function of NMDA receptor subtypes and providing new lead compounds for a variety of neurological diseases .

HY-W017113

2-Mercaptobenzothiazole	Endogenous Metabolite Aryl Hydrocarbon Receptor	Metabolic Disease
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC₅₀ value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .

Cat. No.	Product Name	Target	Research Area