Search Result
Results for "
Cys909
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-102046
-
FM-381
1 Publications Verification
|
JAK
|
Inflammation/Immunology
|
FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
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-
-
- HY-19544
-
|
JAK
|
Cancer
|
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM) .
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-
-
- HY-P0122
-
c(CRGDKGPDC)
|
Integrin
|
Cancer
|
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
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-
-
- HY-12554A
-
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Terlipressin diacetate is a vasopressin analogue with potent vasoactive properties. Terlipressin diacetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin diacetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin diacetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
-
-
- HY-P2271
-
|
Apelin Receptor (APJ)
|
Cancer
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
|
-
-
- HY-161912
-
|
JAK
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Others
|
5TTU is a covalent JAK3 inhibitor. 5TTU not only forms a covalent bond with CYS909 but also establishes a hydrogen bond with the NH group of CYS909 .
|
-
-
- HY-131014
-
|
JAK
|
Inflammation/Immunology
|
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases . FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
|
-
-
- HY-P5188A
-
-
-
- HY-12554
-
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
-
-
- HY-P1766
-
|
CGRP Receptor
|
Cardiovascular Disease
|
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. Rat adrenomedullin induces a selective arterial vasodilation via CGRP1 receptors .
|
-
-
- HY-P5907
-
|
Opioid Receptor
|
Neurological Disease
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
-
-
- HY-12554B
-
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
-
-
- HY-P3448
-
CEND-1; iRGD; LSTA1
|
Integrin
Complement System
|
Cancer
|
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors .
|
-
-
- HY-P5914
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WaTx
|
TRP Channel
|
Neurological Disease
|
Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
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-
-
- HY-P5914A
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WaTx TFA
|
TRP Channel
|
Neurological Disease
|
Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
-
- HY-P5160
-
PhlTx1
|
Sodium Channel
|
Inflammation/Immunology
|
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 .
|
-
-
- HY-P5183
-
|
Sodium Channel
|
Neurological Disease
|
Hm1a is a disulfide-rich spider-venom peptide, and a NaV1.1 activator. Hm1a restores the function of inhibitory interneurons in Dravet syndrome (DS) mouse model .
|
-
-
- HY-P1410A
-
GsMTx4 TFA
Maximum Cited Publications
44 Publications Verification
|
TRP Channel
Piezo Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
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-
-
- HY-P1410
-
GsMTx4
Maximum Cited Publications
44 Publications Verification
|
TRP Channel
Piezo Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
|
-
-
- HY-P5164
-
|
Sodium Channel
|
Neurological Disease
|
GrTx1 is a peptide toxin originally isolated from the venom of the spider Grammostola rosea. GrTx1 blocks sodium channel, with IC50s of 0.63 µM, 0.23 µM, 0.77 µM, 1.29 µM, 0.63 µM and 0.37 µM for Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6 and Nav1.7, repectively .GrTx1 can be used for neurological disease research .
|
-
-
- HY-P5153
-
μ-TRTX-Tp1a
|
Sodium Channel
|
Neurological Disease
|
ProTx-III is a selective and potent inhibitor of voltage-gated sodium channel Nav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia .
|
-
-
- HY-P5179
-
HWTX-I
|
Calcium Channel
Sodium Channel
|
Neurological Disease
|
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively .
|
-
-
- HY-P5177
-
-
-
- HY-P5155
-
|
Potassium Channel
|
Neurological Disease
|
Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats .
|
-
-
- HY-P5184
-
HNTX-IV
|
Sodium Channel
|
Neurological Disease
|
Hainantoxin-IV is a specific antagonist of Sodium Channel, targeting to tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels. His28 and Lys32 are the key resiudes of Hainantoxin-IV for binding with target, while Hainantoxin-IV adopts an inhibitor cystine knot motif .
|
-
-
- HY-P1410B
-
-
-
- HY-P2785
-
-
-
- HY-P5180
-
|
Sodium Channel
|
Neurological Disease
|
Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, respectively .
|
-
-
- HY-P2786A
-
-
-
- HY-P1410C
-
-
-
- HY-P2785A
-
-
-
- HY-P1215
-
|
Melanocortin Receptor
|
Metabolic Disease
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
-
-
- HY-P1215A
-
|
Melanocortin Receptor
|
Metabolic Disease
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
-
-
- HY-P5165
-
|
Potassium Channel
|
Inflammation/Immunology
|
Maurotoxin is a 34-residue and four disulde-bridged toxin that can be isolated from the chactoid scorpion (Scorpio maurus). Maurotoxin inhibits the Shaker potassium channels (ShB) K + current with an IC50 of 2 nM .
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-
-
- HY-P5931
-
Potassium channel toxin alpha-KTx 6.13; SPX; α-KTx6.13
|
Potassium Channel
|
Inflammation/Immunology
|
Spinoxin isolated from the venom of scorpion Heterometrus spinifer, is a 34-residue peptide neurotoxin cross-linked by four disulfide bridges. Spinoxin is a potent inhibitor of Kv1.3 potassium channel (IC50 = 63 nM), considering to be valid molecular targets in the diagnostics and therapy of various autoimmune disorders and cancers .
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-
-
- HY-P5182
-
|
Potassium Channel
|
Inflammation/Immunology
|
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
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-
-
- HY-P5182A
-
|
Potassium Channel
|
Inflammation/Immunology
|
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
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-
-
- HY-P1682A
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POL6326 TFA
|
CXCR
Arrestin
|
Cancer
|
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
-
- HY-P1682
-
POL6326
|
CXCR
Arrestin
|
Cancer
|
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
|
-
-
- HY-P4745
-
|
MCHR1 (GPR24)
|
Metabolic Disease
|
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0122
-
c(CRGDKGPDC)
|
Integrin
|
Cancer
|
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
|
-
- HY-P2526A
-
|
Peptides
|
Cancer
|
LyP-1 TFA is a cyclic 9 amino acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
|
-
- HY-P5217
-
|
Peptides
|
Others
|
CSTSMLKAC (peptide 2) is a cyclic 9 amino acid sequence that mimics endogenous peptide sequences. CSTSMLKAC homes to cardiomyocytes in the ischemic myocardium .
|
-
- HY-P1457
-
|
Peptides
|
Cardiovascular Disease
|
Adrenomedullin (AM) (13-52), human is a 40 amino acid peptide, which acts as an endothelium-dependent vasodilator agent.
|
-
- HY-12554A
-
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Terlipressin diacetate is a vasopressin analogue with potent vasoactive properties. Terlipressin diacetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin diacetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin diacetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
-
- HY-P2526
-
|
Peptides
|
Cancer
|
LyP-1 is a cyclic 9‐amino‐acids tumor homing peptide and selectively bind to p32 receptors overexpressed in various tumor-associated cells .
|
-
- HY-P3825
-
CCAP
|
Peptides
|
Cardiovascular Disease
|
Crustacean cardioactive peptide (CCAP) is a insect cardioregulatory peptides that contmns 9 amino acid, first isolated from the tobacco hawkmoth, Manduca sexta. There are two cystemes at pnsttons 3 and 9 forming a disulfide bridge and the carboxyl-terminns is amldated .
|
-
- HY-P5188A
-
-
- HY-P10557
-
|
Peptides
|
Neurological Disease
|
DAG peptide is a cyclic peptide. DAG peptide selectively recognizes a subset of astrocytes that are activated in Alzheimer's disease (AD) starting at an early stage of the disease. DAG peptide can be used as a tool to enhance the delivery of therapeutics and imaging agents to sites of vascular changes and astrogliosis in diseases associated with neuroinflammation .
|
-
- HY-P1766
-
|
CGRP Receptor
|
Cardiovascular Disease
|
Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. Rat adrenomedullin induces a selective arterial vasodilation via CGRP1 receptors .
|
-
- HY-P2271
-
|
Apelin Receptor (APJ)
|
Cancer
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation .
|
-
- HY-P3525
-
|
Peptides
|
Others
|
G-Pen-GRGDSPCA is a polypeptide. G-Pen-GRGDSPCA can be used for the research of various biochemical studies .
|
-
- HY-P5907
-
|
Opioid Receptor
|
Neurological Disease
|
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a Ki of 21 nM and an EC50 of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .
|
-
- HY-12554B
-
|
Vasopressin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
|
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
|
-
- HY-P3448
-
CEND-1; iRGD; LSTA1
|
Integrin
Complement System
|
Cancer
|
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors .
|
-
- HY-P5914
-
WaTx
|
TRP Channel
|
Neurological Disease
|
Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-P5914A
-
WaTx TFA
|
TRP Channel
|
Neurological Disease
|
Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-P5160
-
PhlTx1
|
Sodium Channel
|
Inflammation/Immunology
|
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 .
|
-
- HY-P5167
-
|
Peptides
|
Inflammation/Immunology
|
GsAF-1 is a peptide toxin containing three disulfide bonds. GsAF-1 can be isolated from the venom of the Chilean pink tarantula. GsAF-1 can be used for research of moderate-to-severe pain .
|
-
- HY-P5183
-
|
Sodium Channel
|
Neurological Disease
|
Hm1a is a disulfide-rich spider-venom peptide, and a NaV1.1 activator. Hm1a restores the function of inhibitory interneurons in Dravet syndrome (DS) mouse model .
|
-
- HY-P1410A
-
GsMTx4 TFA
Maximum Cited Publications
44 Publications Verification
|
TRP Channel
Piezo Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
|
-
- HY-P1410
-
GsMTx4
Maximum Cited Publications
44 Publications Verification
|
TRP Channel
Piezo Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
|
-
- HY-P5164
-
|
Sodium Channel
|
Neurological Disease
|
GrTx1 is a peptide toxin originally isolated from the venom of the spider Grammostola rosea. GrTx1 blocks sodium channel, with IC50s of 0.63 µM, 0.23 µM, 0.77 µM, 1.29 µM, 0.63 µM and 0.37 µM for Nav1.1, Nav1.2, Nav1.3, Nav1.4, Nav1.6 and Nav1.7, repectively .GrTx1 can be used for neurological disease research .
|
-
- HY-P5153
-
μ-TRTX-Tp1a
|
Sodium Channel
|
Neurological Disease
|
ProTx-III is a selective and potent inhibitor of voltage-gated sodium channel Nav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia .
|
-
- HY-P5916
-
κ-Theraphotoxin-Gr4a; Kappa-TRTX-Gr4a; Voltage sensor toxin 3; Peptide F
|
Peptides
|
Neurological Disease
|
VSTx-3 is a KV channel blocker. VSTx-3 is demonstrated to be a potent, TTX-sensitive sodium channel blocker and especially, a potent blocker of NaV1.8 channels (IC50 0.19 μM for hNaV1.3, 0.43 μM for hNaV1.7 and 0.77 μM for hNaV1.8 channels).
|
-
- HY-P5179
-
HWTX-I
|
Calcium Channel
Sodium Channel
|
Neurological Disease
|
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively .
|
-
- HY-P5177
-
-
- HY-P5155
-
|
Potassium Channel
|
Neurological Disease
|
Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats .
|
-
- HY-P5184
-
HNTX-IV
|
Sodium Channel
|
Neurological Disease
|
Hainantoxin-IV is a specific antagonist of Sodium Channel, targeting to tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels. His28 and Lys32 are the key resiudes of Hainantoxin-IV for binding with target, while Hainantoxin-IV adopts an inhibitor cystine knot motif .
|
-
- HY-P1410B
-
-
- HY-P2785
-
-
- HY-P5180
-
|
Sodium Channel
|
Neurological Disease
|
Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, respectively .
|
-
- HY-P2786A
-
-
- HY-P1410C
-
-
- HY-P2785A
-
-
- HY-P5151
-
|
Peptides
|
Others
|
LiTx3 is a lethal and cysteine-rich peptide. LiTx3 can be isolated from L. intermedia crude venom. LiTx3 induces flaccid paralysis in Spodoptera frugiperda larvae .
|
-
- HY-P1215
-
|
Melanocortin Receptor
|
Metabolic Disease
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
|
-
- HY-P1215A
-
|
Melanocortin Receptor
|
Metabolic Disease
|
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake .
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- HY-P5176
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LtTx-1a
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Peptides
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Neurological Disease
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Latartoxin-1a (LtTx-1a) is a peptide toxin can be isolated from L. tarabaevi. Latartoxin-1a is paralytic and lethal to insects and has membrane-bound activity .
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- HY-P5165
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Potassium Channel
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Inflammation/Immunology
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Maurotoxin is a 34-residue and four disulde-bridged toxin that can be isolated from the chactoid scorpion (Scorpio maurus). Maurotoxin inhibits the Shaker potassium channels (ShB) K + current with an IC50 of 2 nM .
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- HY-P5931
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Potassium channel toxin alpha-KTx 6.13; SPX; α-KTx6.13
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Potassium Channel
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Inflammation/Immunology
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Spinoxin isolated from the venom of scorpion Heterometrus spinifer, is a 34-residue peptide neurotoxin cross-linked by four disulfide bridges. Spinoxin is a potent inhibitor of Kv1.3 potassium channel (IC50 = 63 nM), considering to be valid molecular targets in the diagnostics and therapy of various autoimmune disorders and cancers .
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- HY-P5182
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Potassium Channel
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Inflammation/Immunology
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HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
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- HY-P5182A
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Potassium Channel
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Inflammation/Immunology
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HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
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- HY-P1682A
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POL6326 TFA
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CXCR
Arrestin
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Cancer
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Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
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- HY-P1682
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POL6326
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CXCR
Arrestin
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Cancer
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Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
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- HY-P4745
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MCHR1 (GPR24)
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Metabolic Disease
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hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research .
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