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Results for "

Cys242

" in MedChemExpress (MCE) Product Catalog:

119

Inhibitors & Agonists

122

Peptides

4

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P0036
    Octreotide
    Maximum Cited Publications
    16 Publications Verification

    SMS 201-995

    Somatostatin Receptor Apoptosis Cardiovascular Disease Inflammation/Immunology Endocrinology Cancer
    Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
    Octreotide
  • HY-P1932

    Somatostatin Receptor Neurological Disease Inflammation/Immunology Endocrinology
    Cortistatin-14 is a neuropeptide that shares structural similarities with somatostatin, working by binding to somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) has anticonvulsant, neuroprotective effects, and significant anti-inflammatory properties .
    Cortistatin-14
  • HY-159852

    PI3K Ras Akt Cancer
    BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
    BBO-10203
  • HY-P1464

    Amylin (rat)

    Amylin Receptor Metabolic Disease
    Amylin, amide, rat is a potent and high affinity ligand of Amylin receptor AMY1 and AMY3 receptors and variably of AMY2 receptors; binding studies are generally used for the latter receptor.
    Amylin, amide, rat
  • HY-P1548
    β-CGRP, human
    1 Publications Verification

    Human β-CGRP; CGRP-II (Human)

    CGRP Receptor Cardiovascular Disease Inflammation/Immunology
    β-CGRP, human (Human β-CGRP) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells .
    β-CGRP, human
  • HY-P0173A
    Chlorotoxin
    2 Publications Verification

    Chloride Channel Cancer
    Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.
    Chlorotoxin
  • HY-P1036
    Compstatin
    3 Publications Verification

    Complement System Others
    Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
    Compstatin
  • HY-P10033

    Ser/Thr Protease Others
    SFTI-1 is a cyclic peptide trypsin inhibitor consisting of 14 amino acid residues. SFTI-1 belongs to the Bowman-Birk class of inhibitors. Characterized by its small size, high stability, and potent activity, SFTI-1 can be used for research on peptide drug design platforms .
    SFTI-1
  • HY-P1070A

    DAP amide, human TFA

    Amylin Receptor Metabolic Disease
    Amylin, amide, human TFA, a 37-amino acid polypeptide, is a pancreatic hormone cosecreted with insulin that exerts unique roles in metabolism and glucose homeostasis. Amylin, amide, human TFA inhibits glucagon secretion, delays gastric emptying, and acts as a satiety agent .
    Amylin, amide, human TFA
  • HY-176812

    Ras PI3K Akt Cancer
    VVD-849 is a RAS ligand. VVD-849 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT (S473) in HER2-overexpressing tumors. VVD-849 can be used for the research of cancers such as breast cancer .
    VVD-849
  • HY-176811

    Ras PI3K Akt Cancer
    VVD-442 is an inhibitor targeting PI3Kα. VVD-442 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α, induces conformational changes, and disrupts the interaction between PI3K p110α and RAS proteins. VVD-442 also blocks RAS-mediated PI3K activation. VVD-442 can be used in research related to RAS-mutant cancers and HER2-overexpressing cancers .
    VVD-442
  • HY-P1070

    DAP amide, human

    Amylin Receptor Metabolic Disease
    Amylin, amide, human, a 37-amino acid polypeptide, is a pancreatic hormone cosecreted with insulin that exerts unique roles in metabolism and glucose homeostasis. Amylin, amide, human inhibits glucagon secretion, delays gastric emptying, and acts as a satiety agent .
    Amylin, amide, human
  • HY-P10920

    Drug Derivative Cancer
    DOTAMTATE is a somatostatin analogue. DOTAMTATE marked 212Pb is promising for research of somatostatin receptor positive neuroendocrine tumors .
    DOTAMTATE
  • HY-P4058

    CGRP free acid

    CGRP Receptor Neurological Disease
    Calcitonin gene-related peptide (CGRP) free acid is a 37-amino acid neuropeptide, which represents the deamidated form of α-CGRP (human) (HY-P1071). Calcitonin gene-related peptide free acid is produced in the central and peripheral nervous systems of rats, and localizes to specific sensory, integrative and motor neuron systems, including those involved in nociception/thermoreception, feeding behavior, olfaction and visceral motor functions .
    Calcitonin gene-related peptide free acid
  • HY-P3732

    Integrin Cancer
    RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models .
    RGD-4C
  • HY-P1959

    BIM 23014

    Somatostatin Receptor Endocrinology Cancer
    Lanreotide (BIM 23014) is a somatostatin analogue with antineoplastic activity. Lanreotide can be used for the research of carcinoid syndrome .
    Lanreotide
  • HY-P1959A

    BIM 23014 acetate

    Somatostatin Receptor Endocrinology Cancer
    Lanreotide (BIM 23014) acetate is a somatostatin analogue with antineoplastic activity. Lanreotide acetate can be used for the research of carcinoid syndrome .
    Lanreotide acetate
  • HY-P0061A
    Vapreotide acetate
    1 Publications Verification

    RC-160 acetate; BMY-41606 acetate

    Neurokinin Receptor Cancer
    Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide acetate
  • HY-P1212

    CST-14 (mouse, rat)

    Somatostatin Receptor Neurological Disease
    Cortistatin 14, mouse, rat (CST-14, human, rat), a neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus .
    Cortistatin 14 (mouse, rat)
  • HY-P1913A

    CGRP II (rat) TFA

    CGRP Receptor Cardiovascular Disease
    Calcitonin Gene Related Peptide II rat TFA, a CGRP receptor activator, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide II rat TFA can be used in the research of cardiovascular diseases .
    Calcitonin Gene Related Peptide II (rat) TFA
  • HY-P1548A
    β-CGRP, human TFA
    1 Publications Verification

    Human β-CGRP TFA; CGRP-II (Human) TFA

    CGRP Receptor Cardiovascular Disease Inflammation/Immunology
    β-CGRP, human TFA (Human β-CGRP TFA) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells .
    β-CGRP, human TFA
  • HY-P0173B
    Chlorotoxin TFA
    2 Publications Verification

    Chloride Channel Cancer
    Chlorotoxin TFA is a peptide isolated from the venom of the scorpion Leiurus quinquestriatus, acts as a chloride channel blocker . Anti-cancer activity .
    Chlorotoxin TFA
  • HY-P10239

    Somatostatin Receptor Radionuclide-Drug Conjugates (RDCs) Cancer
    Tyr3-Octreotate is a ligand for somatostatin receptor subtype 2 (sst2), with an IC50 value of 1.3 nM against sst2 when labeled with [ 111In-DTPA], and an IC50 value of 1.6 nM against sst2 when labeled with [ 90Y-DOTA]. Radiolabeled Tyr3-Octreotate generates cell-associated radioactivity, and acts as both a tumor growth inhibitor and a tumor cytotoxic agent. When radiolabeled with 177Lu or 90Y, Tyr3-Octreotate serves as a peptide receptor radionuclide therapy (PRRT) analog. Tyr3-Octreotate can be used in studies related to pancreatic tumors .
    Tyr3-Octreotate
  • HY-P0061
    Vapreotide
    1 Publications Verification

    RC160; BMY 41606

    Neurokinin Receptor Cancer
    Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC50 of 330 nM.
    Vapreotide
  • HY-P2026

    Natriuretic Peptide Receptor (NPR) Cardiovascular Disease
    A 71915 is a highly potent and competitive natriuretic peptide receptor A (ANP, NPRA) antagonist (pKi= 9.18). A 71915 displaces [ 125I]ANP dose dependently, with a Ki of 0.65 nM. A71915( pA2= 9.48) against rat ANP-induced cGMP production in NB-OK-1 cells .
    A 71915
  • HY-P1565A

    TD 1 Disulfide(peptide) TFA

    Na+/K+ ATPase Others
    Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA) is a 11-amino acid peptide, binds to Na +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide TFA can enhance the transdermal delivery of many macromolecules .
    Transdermal Peptide Disulfide TFA
  • HY-P4767

    Amylin Receptor Metabolic Disease
    Amylin (1-13) (human) is a fragment and a residues within amyloid cores of Amylin (human IAPP). Amylin is a glucose-regulating hormone, deposits as amyloid fibrils in condition of type II diabetes (T2D). Amylin (1-13) (human) has no effect on firbl formation, as it cannot form fibrils by itself .
    Amylin (1-13) (human)
  • HY-P1036A
    Compstatin TFA
    3 Publications Verification

    Complement System Others
    Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
    Compstatin TFA
  • HY-P4928

    Amylin Receptor Metabolic Disease
    Biotinyl-Amylin (mouse, rat) is a biotinylated Amylin (mouse, rat). Amylin (mouse, rat) is a 37-aminoacid pancreatic protein that exerts control over several metabolic events such as glycemia and lacticemia .
    Biotinyl-Amylin (mouse, rat)
  • HY-108814A
    Ecallantide TFA
    2 Publications Verification

    DX-88 TFA

    Kallikrein Cardiovascular Disease
    Ecallantide (DX-88) TFA is a specific recombinant plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide may be used to prevent acute attacks of angioedema .
    Ecallantide TFA
  • HY-P3282

    Guanylate Cyclase Metabolic Disease
    MM 419447, a linaclotide metabolite, is a guanylate cyclase-C agonist. MM 419447 has the potential for the research of the irritable bowel syndrome with constipation (IBS-C) .
    MM 419447
  • HY-17584A
    Linaclotide acetate
    2 Publications Verification

    Guanylate Cyclase Cancer
    Linaclotide acetate is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
    Linaclotide acetate
  • HY-P1139

    PCFWKTCK

    GHSR Metabolic Disease
    Cortistatin-8 (CST-8; PCFWKTCK), a neuropeptide, is a GHS-R1a antagonist by counteracting the response of ghrelin on gastric acid secretion. Cortistatin-8 can modulate GH release from somatotroph cells. Cortistatin-8 is a synthetic CST-analogue devoid of any binding affinity to SST-R but capable to bind the GHS-R1a. Cortistatin-8 can exert antagonistic effects on ghrelin actions either in vitro or in vivo in animals .
    Cortistatin-8
  • HY-P10273A

    Radionuclide-Drug Conjugates (RDCs) Biochemical Assay Reagents Cancer
    DOTA-Octreotide TFA is composed of chelator DOTA and Octreotide (HY-P0036). DOTA-Octreotide TFA is used for research of cancer through combination with radioactive elements. DOTA-Octreotide TFA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
    DOTA-Octreotide TFA
  • HY-P4764

    Melanocortin Receptor Cardiovascular Disease
    Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 is a cyclic octapeptide with MC4R agonism. Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 significantly increases heart rate and blood pressure .
    Ac-(d-Arg)-CEH-(d-Phe)-RWC-NH2
  • HY-P1932A

    Somatostatin Receptor Neurological Disease Inflammation/Immunology Endocrinology
    Cortistatin-14 (TFA), a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties .
    Cortistatin-14 TFA
  • HY-P5183

    Sodium Channel Neurological Disease
    Hm1a is a venom peptide and a selective hNaV1.1 activator with an EC50 of 7.5 nM. Hm1a enhances hNaV1.1 and hNaV1.3 channel currents via delayed inactivation. Hm1a restores action potential firing in Dravet syndrome GABAergic inhibitory interneurons, reduces interictal epileptiform discharges and whole-brain hyperexcitability, lowers seizure frequency, and rescues premature death in Dravet syndrome mice. Hm1a can be used for the research of neurological disease, such as Dravet syndrome .
    Hm1a
  • HY-P0036A

    SMS 201-995 dihydrochloride

    Somatostatin Receptor Apoptosis Inflammation/Immunology Endocrinology Cancer
    Octreotide (SMS 201-995) hydrochloride is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide hydrochloride can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide hydrochloride increases Gi activity and reduces intracellular cAMP production. Octreotide hydrochloride has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly .
    Octreotide dihydrochloride
  • HY-P1913

    CGRP II (rat)

    CGRP Receptor Cardiovascular Disease
    Calcitonin Gene Related Peptide II rat, a CGRP receptor activator, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide II rat can be used in the research of cardiovascular diseases .
    Calcitonin Gene Related Peptide II (rat)
  • HY-P5925A

    SsTx Toxin TFA

    Potassium Channel Neurological Disease Inflammation/Immunology
    Ssm Spooky Toxin TFA is found in Scolopendra mutilans that potently inhibits KCNQ (voltage-gated potassium channel family 7) channels, with IC50s of 2.8 μM, 5.26 μM and 0.1-0.3 M for Kv7.4, Kv1.3, and Shal channel, respectivily. Ssm Spooky Toxin TFA inhibits cytokine generation by specifically acting on the KV1.3 channel in T cells. Ssm Spooky Toxin TFA plays an essential role in the centipede’s circulatory system .
    Ssm spooky toxin TFA
  • HY-P5809

    μ-TrTx-Pe1b

    Sodium Channel Neurological Disease
    Pe1b (μ-TrTx-Pe1b) is a selective Nav1.7 inhibitor with an IC50 of 167 nM .
    Pe1b
  • HY-P10851

    Apoptosis Inflammation/Immunology Cancer
    HVEM(14-39) is a B- and T-lymphocyte attenuator (BTLA) peptide inhibitor. HVEM (14-39) can be combined with BTLA with a KD of 0.102 μM. HVEM(14-39) enhances the activation and proliferation of T cells by regulating the expression of BTLA and HVEM in T cells, and promotes the transformation of cells into effector memory T cells. HVEM(14-39) inhibits tumor cell proliferation and promotes late apoptosis. HVEM(14-39) has immunomodulatory effects and can be used in the study of cancer .
    HVEM(14-39)
  • HY-108814

    DX-88

    Kallikrein Cardiovascular Disease
    Ecallantide (DX-88) is a specific plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide can be used to prevent acute attacks of angioedema .
    Ecallantide
  • HY-P1719

    IW-9179

    Biochemical Assay Reagents Others
    Recanaclotide can be studied in research on gastroparesis, functional dyspepsia and gastrointestical disorders.
    Recanaclotide
  • HY-P5160A

    PhlTx1 TFA

    Sodium Channel Neurological Disease
    Phlotoxin-1 (PhlTx1) is a 34-amino acid and 3-disulfide bridge peptide. Phlotoxin-1 can be isolated from Phlogiellus genus spider. Phlotoxin-1 is an antinociceptive agent by inhibiting NaV1.7 channel .
    Phlotoxin-1 TFA
  • HY-P2786A

    Potassium Channel Neurological Disease
    Phrixotoxin 2 is a highly selective KV4.2 and KV4.3-channels blocker .
    Phrixotoxin 2
  • HY-P2569

    Apoptosis Cancer
    Malformin A1, a cyclic pentapeptide isolated from Aspergillus niger, possess a range of bioactive properties including antibacterial activity. Malformin A1 shows potent cytotoxic activities on human colorectal cancer cells. Malformin A1 induces apoptosis by activating PARP, caspase 3, -7, and -9 .
    Malformin A1
  • HY-P5659

    Bacterial Antibiotic Infection
    Brevinin-1 is an antimicrobial peptide derived from the skin secretions of Rana esculenta .
    Brevinin-1
  • HY-P10833

    VEGFR PI3K Akt mTOR ERK Apoptosis Cardiovascular Disease Cancer
    C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer .
    C-VGB3
  • HY-P10793

    EGFR Apoptosis Cancer
    Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
    Cyclic(YCDGFYACYMDV)

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