6

MRS 1523

6 Publications Verification

Cat. No.: HY-121119

CAS No.: 212329-37-8

Purity: 99.97%

Target:

Adenosine Receptor Calcium Channel

Research Areas:

Cardiovascular Disease Neurological Disease Inflammation/Immunology

MRS 1523 is a potent and selective adenosine A₃ receptor antagonist with K_i values of 18.9 nM and 113 nM for human and rat A₃ receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A₁ and A_2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons .

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4

Lazertinib

4 Cited Publications

Cat. No.: HY-109061

CAS No.: 1903008-80-9

Purity: 99.87%

Synonyms: YH25448; GNS-1480

Target:

Apoptosis Akt TRP Channel EGFR ERK

Research Areas:

Infection Neurological Disease Metabolic Disease Cancer

Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .

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4

KT5720

4 Cited Publications

Cat. No.: HY-N6789

CAS No.: 108068-98-0

Target:

PKA

Research Areas:

Neurological Disease Cancer

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

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4

Olodanrigan

4 Cited Publications

Cat. No.: HY-13106

CAS No.: 1316755-16-4

Purity: 98.89%

Synonyms: EMA401; PD-126055; (S)-EMA400

Target:

Angiotensin Receptor

Research Areas:

Cardiovascular Disease Neurological Disease Endocrinology

Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .

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4

Lazertinib mesylate

4 Cited Publications

Cat. No.: HY-109061B

CAS No.: 2247995-37-3

Synonyms: YH25448 mesylate; GNS-1480 mesylate

Target:

TRP Channel EGFR Akt ERK Apoptosis

Research Areas:

Cancer

Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .

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1

H-20

1 Cited Publications

Cat. No.: HY-P10908

CAS No.: 3020015-02-2

Target:

PD-1/PD-L1 Opioid Receptor

Research Areas:

Neurological Disease

H-20 is a PD-1 agonist peptide. H-20 increases μOR mRNA in DRG neurons and modulates μOR-mediated analgesia. H-20 produces synergistic analgesic effects in inflammatory pain models and can reduce analgesic-induced tolerance, hyperalgesia, constipation, and motor impairment. H-20 can be used in pain-related research .

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1

PTPσ Inhibitor, ISP

1 Cited Publications

Cat. No.: HY-P5982

Target:

Phosphatase Transmembrane Glycoprotein MMP ERK Akt Cathepsin

Research Areas:

Neurological Disease Cancer

PTPσ Inhibitor, ISP is a PTPσ intracellular wedge domain mimetic peptide containing a TAT cell-penetrating domain, which acts as a PTPσ inhibitor. PTPσ Inhibitor, ISP binds to and inhibits PTPσ, thereby relieving CSPG-mediated axonal growth inhibition. PTPσ Inhibitor, ISP enhances CSPG degradation by promoting the secretion of Cathepsin B or MMP-2, and promotes DRG axonal growth, OPC migration and remyelination. PTPσ Inhibitor, ISP promotes nerve regeneration and improves sensory, motor and urinary functions in animal models of spinal cord injury, dorsal root injury and multiple sclerosis. PTPσ Inhibitor, ISP also increases the phosphorylation of ERK and AKT in colorectal cancer cells. PTPσ Inhibitor, ISP can be used in studies related to PTPσ/CSPG signaling, nerve regeneration, demyelinating diseases and RAS/ERK signaling .

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SG2057

Cat. No.: HY-101160

CAS No.: 260417-62-7

Purity: 99.93%

Synonyms: DRG16

Target:

DNA Alkylator/Crosslinker ADC Payloads

Research Areas:

Cancer

SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent .

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