154

Erlotinib Hydrochloride

154 Publications Verification

Cat. No.: HY-12008

CAS No.: 183319-69-9

Purity: 99.94%

Synonyms: CP-358774 hydrochloride; NSC 718781 hydrochloride; OSI-774 hydrochloride

Target:

EGFR OAT ERK GSK-3 β-catenin

Research Areas:

Endocrinology Cancer

Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis .

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154

Erlotinib

154 Publications Verification

Cat. No.: HY-50896

CAS No.: 183321-74-6

Synonyms: CP-358774; NSC 718781; OSI-774

Target:

EGFR OAT ERK GSK-3 β-catenin

Research Areas:

Endocrinology Cancer

Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions .

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6

K145 hydrochloride

6 Cited Publications

Cat. No.: HY-15779A

CAS No.: 1449240-68-9

Purity: 99.62%

Target:

SphK Apoptosis

Research Areas:

Cancer

K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC₅₀ of 4.3 μM and a K_i of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity .

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5

Kinase, Natto fermentation

5 Cited Publications

Cat. No.: HY-P2373

CAS No.: 133876-92-3

Target:

PAI-1

Research Areas:

Cardiovascular Disease

Kinase, Natto fermentation is a potent fibrinolytic enzyme. Kinase, Natto fermentation can break down blood clots by directly hydrolyzing fibrin and plasmin substrate. Kinase, Natto fermentation can be used for the research of cardiovascular diseases .

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4

ATP-polyamine-biotin

4 Cited Publications

Cat. No.: HY-D0183

CAS No.: 1800401-93-7

ATP-polyamine-biotin, the first cell-permeable ATP analogue, is an efficient kinase cosubstrate. ATP-polyamine-biotin promotes biotin labeling of kinase substrates in live cells .

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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

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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3

SAMS

3 Cited Publications

Cat. No.: HY-P0136

CAS No.: 125911-68-4

Target:

AMPK

Research Areas:

Metabolic Disease

SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).

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3

BIO-11006 acetate

3 Cited Publications

Cat. No.: HY-106377A

Purity: 99.94%

Target:

MARCKS

Research Areas:

Inflammation/Immunology Cancer

BIO-11006 acetate, an analog of the MANS peptide, is a MARCKS (myristoylated alanine-rich C kinase substrate) inhibitor .

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3

Sodium creatine phosphate dibasic tetrahydrate

3 Cited Publications

Cat. No.: HY-D0885A

CAS No.: 71519-72-7

Synonyms: Creatine phosphate disodium tetrahydrate; Creatinephosphoric acid disodium tetrahydrate

Category:

Metabolic Disease Amino acids Endogenous metabolite Disease Research Fields

Target:

Endogenous Metabolite

Phosphocreatine disodium tetrahydrate, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives, is a substrate for the determination of creatine kinase and used to regenerate ATP during skeletal muscle contraction .

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3

BDP9066

3 Cited Publications

Cat. No.: HY-111424

CAS No.: 2226507-04-4

Purity: 98.18%

Target:

Cdc42-binding kinase

Research Areas:

Cancer

BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinase MRCK inhibitor with an IC₅₀ of 64 nM for MRCKβ in SCC12 cells, K_i values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.

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2

Kemptide

2 Cited Publications

Cat. No.: HY-P0248

CAS No.: 65189-71-1

Target:

PKA

Research Areas:

Metabolic Disease

Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).

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2

Casein Kinase 2 Substrate Peptide

2 Cited Publications

Cat. No.: HY-P3815

CAS No.: 132176-35-3

Target:

Casein Kinase

Research Areas:

Others

Casein Kinase 2 Substrate Peptide is a common CK2 substrate peptide. Casein Kinase 2 Substrate Peptide is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). Casein Kinase 2 Substrate Peptide can be used for protein kinase CK2 activity determination .

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2

Crosstide

2 Cited Publications

Cat. No.: HY-P0315

CAS No.: 171783-05-4

Target:

Akt

Research Areas:

Others

Crosstide is a peptide analog of glycogen synthase kinase α/β fusion protein sequence which is a substrate for Akt.

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2

Myelin basic protein (4-14)

2 Cited Publications

Cat. No.: HY-P1821

CAS No.: 126768-94-3

Synonyms: MHP4-14

Target:

PKC

Research Areas:

Neurological Disease Inflammation/Immunology

Myelin basic protein 4-14 (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (K_m=7 μM). Myelin Basic Protein is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca ²⁺/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .

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2

Myelin basic protein (4-14) TFA

2 Cited Publications

Cat. No.: HY-P1821A

Synonyms: MHP4-14 TFA

Target:

PKC

Research Areas:

Neurological Disease

Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (K_m=7 μM). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca ²⁺/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts .

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2

Syntide 2 TFA

2 Cited Publications

Cat. No.: HY-P0271A

Target:

CaMK

Research Areas:

Neurological Disease

Syntide 2 (TFA), a Ca ²⁺- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected .

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2

Halicin

2 Cited Publications

Cat. No.: HY-107597

CAS No.: 40045-50-9

Purity: 98.92%

Synonyms: SU3327

Target:

JNK

Research Areas:

Metabolic Disease Inflammation/Immunology

Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC₅₀ of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC₅₀ of 239 nM. Halicin shows less active against p38α and Akt kinase .

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