NFAT Inhibitor (VIVIT peptide) is a cell-permeable peptide inhibitor of nuclear factor of activated Tcells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT[1][2].
IC50 Target
Nuclear factor of activated Tcells (NFAT)[1][2]
体外研究 (In Vitro)
NFAT Inhibitor treatment significantly inhibits nuclear translocation of NFATc1 for 24 hours. Long-term treatment with VIVIT significantly inhibits the cytoplasmic levels of cathepsin K, TRAP, and MMP-9[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[2]
Cell Line:
Human peripheral blood CD14+ monocytes
Concentration:
10 μM
Incubation Time:
24 hours or 21 days
Result:
Short-term treatment with 10 μM, significantly inhibited nuclear translocation of NFATc1. Long-term treatment, significantly inhibited the cytoplasmic levels of cathepsin K, TRAP, and MMP-9.
[1]. Aramburu J, et al. Affinity-driven peptide selection of an NFAT inhibitor more selective than cyclosporin A. Science. 1999 Sep 24;285(5436):2129-33.
[2]. Ma JD, et al. Activation of the Peroxisome Proliferator-Activated Receptor γ Coactivator 1β/NFATc1 Pathway in Circulating Osteoclast Precursors Associated With Bone Destruction in Rheumatoid Arthritis. Arthritis Rheumatol. 2019 Aug;71(8):1252-1264.
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 是一种衍生自 LAP-TGFβ 的四肽，是一种竞争性的 TGF-β1 拮抗剂。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 抑制 TSP-1 与 LAP 的结合并减轻肾间质纤维化和肝纤维化。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 通过抑制 TSP-1 介导的 TGF-β1 活性来抑制蛛网膜下纤维化，防止慢性脑积水的发生并改善蛛网膜下腔出血后的长期神经认知缺陷。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 可以轻松穿越血脑屏障。
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) Chemical Structure
规格
价格
是否有货
数量
10;mM;*;1 mL in DMSO
￥1134
In-stock
5 mg
￥900
In-stock
10 mg
￥1300
In-stock
25 mg
￥2600
In-stock
50 mg
;
询价
;
100 mg
;
询价
;
* Please select Quantity before adding items.
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) 相关产品
bull;相关化合物库:
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Kinase Inhibitor Library
TGF-beta/Smad Compound Library
Anti-Cancer Compound Library
CNS-Penetrant Compound Library
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Angiogenesis Related Compound Library
Targeted Diversity Library
Anti-Colorectal Cancer Compound Library
Peptide Library
生物活性
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier[1][2].
IC50 Target
TGF-β1[1]
体外研究 (In Vitro)
The KTFR sequence from ADAMTS1 is responsible for the interaction with the LSKL, Inhibitor of Thrombospondin (TSP-1) (LSKL peptide) from the latent form of TGF-β, leading to its activation. There is a stable binding mode between LSKL, Inhibitor of Thrombospondin (TSP-1) and ADAMTS1 KTFR sequence, characterized by 3 salt bridges and 2 hydrogen bonds[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
LSKL, Inhibitor of Thrombospondin (TSP-1) (1 mg/kg; intraperitoneal injection; male Sprague-Dawley rats) is protective against subarachnoid fibrosis, attenuates ventriculomegaly and effectively suppresses hydrocephalus. LSKL, Inhibitor of Thrombospondin (TSP-1) treatment inhibits TGF-β1 activity and subsequent Smad2/3 signaling[1]. LSKL, Inhibitor of Thrombospondin (TSP-1) (30 mg/kg, i.p.) successfully inhibits transforming growth factor (TGF) β-Smad signal activation induced by partial hepatectomy. LSKL, Inhibitor of Thrombospondin (TSP-1) successfully attenuates TGF-β-Smad signal activation by antagonizing TSP-1, but not by reducing TSP-1 protein expression. LSKL, Inhibitor of Thrombospondin (TSP-1) accelerates hepatocyte proliferation after hepatectomy[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
103 male Sprague-Dawley rats (6 weeks of age; 160-180 g) with subarachnoid hemorrhage (SAH)[1]
Dosage:
1 mg/kg
Administration:
Intraperitoneal injection
Result:
Was protective against subarachnoid fibrosis, attenuated ventriculomegaly and effectively suppressed hydrocephalus.
分子量
572.62
Formula
C23H43F3N6O7
Sequence
Leu-Ser-Lys-Leu
Sequence Shortening
LSKL
中文名称
LSKL, 血小板反应蛋白抑制剂 (TSP-1) 三氟醋酸盐
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Liao F, et al. LSKL peptide alleviates subarachnoid fibrosis and hydrocephalus by inhibiting TSP1-mediated TGF-β1 signaling activity following subarachnoid hemorrhage in rats. Exp Ther Med. 2016 Oct;12(4):2537-2543. Epub 2016 Aug 31.
[2]. Laurent MA, et al. In silico characterization of the interaction between LSKL peptide, a LAP-TGF-beta derived peptide, and ADAMTS1. Comput Biol Chem. 2016 Apr;61:155-61.
[3]. Kuroki H, et al. Effect of LSKL peptide on thrombospondin 1-mediated transforming growth factor β signal activation and liver regeneration after hepatectomy in an experimental model. Br J Surg. 2015 Jun;102(7):813-25.
Fibrinogen Binding Inhibitor Peptide Chemical Structure
CAS No. : 89105-94-2
规格
价格
是否有货
数量
1 mg
￥800
In-stock
5 mg
￥1900
In-stock
10 mg
￥3200
In-stock
50 mg
;
询价
;
100 mg
;
询价
;
* Please select Quantity before adding items.
Fibrinogen Binding Inhibitor Peptide 相关产品
bull;相关化合物库:
Bioactive Compound Library Plus
Anti-Cardiovascular Disease Compound Library
Peptide Library
生物活性
Fibrinogen Binding Inhibitor Peptide is a dodecapeptide (HHLGGAKQAGDV, H12), which is a fibrinogen γ-chain carboxy-terminal sequence (γ400-411). Fibrinogen Binding Inhibitor Peptide is a specific binding site of the ligand for activated glycoprotein (GP) IIb/IIIa.
体外研究 (In Vitro)
Glycoprotein (GP) IIb/IIIa, which exists on the membrane of platelets, changes its form from inactive to active when platelets adhere to collagen exposed on sites of vascular injury. In the circulation, platelet aggregation is mediated by fibrinogen by bridging adjacent platelets through GPIIb/IIIa in an activation-dependent manner. A dodecapeptide HHLGGAKQAGDV (H12), corresponding to the fibrinogen γ-chain carboxy-terminal sequence (γ400-411), is a specific binding site of the ligand for activated GPIIb/IIIa[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1189.28
Formula
C50H80N18O16
CAS 号
89105-94-2
Sequence
His-His-Leu-Gly-Gly-Ala-Lys-Gln-Ala-Gly-Asp-Val
Sequence Shortening
HHLGGAKQAGDV
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-80deg;C
2 years
-20deg;C
1 year
In solvent
-80deg;C
6 months
-20deg;C
1 month
Solvent Solubility
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Okamura Y, et al. Release abilities of adenosine diphosphate from phospholipid vesicles with different membraneproperties and their hemostatic effects as a platelet substitute. J Control Release. 2010 Dec 20;148(3):373-9.
[1]. Gao Y, Xing J, et al. Trp(56) of rac1 specifies interaction with a subset of guanine nucleotide exchange factors [published correction appears in J Biol Chem. 2005 Jan 14;280(2):1704]. J Biol Chem. 2001;276(50):47530-47541.
PKG inhibitor peptide is an ATP-competitive inhibitor of cGMP-dependent protein kinase (PKG), with a Ki of 86 μM[1].
IC50 Target
Ki: 86 μM (PKG)[1]
体外研究 (In Vitro)
Summary of experiments showing that intracellular dialysis of postsynaptic cells with PKG inhibitor PKG inhibitor peptide (1 mM) failed to alter the induction of long-term depression (CCh-LTD)[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
943.11
Formula
C38H74N18O10
CAS 号
82801-73-8
Sequence Shortening
RKRARKE
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Bhatnagar D, et al. Synthetic peptide analogues differentially alter the binding affinities of cyclic nucleotide dependent protein kinases for nucleotide substrates. Biochemistry. 1988 Mar 22;27(6):1988-94.
[2]. Chiung-Chun Huang, et al. Activation of muscarinic acetylcholine receptors induces a nitric oxide-dependent long-term depression in rat medial prefrontal cortex. Cereb Cortex. 2010 Apr;20(4):982-96.
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein[1][2].
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Peterson, et al. A chemical inhibitor of N-WASP reveals a new mechanism for targeting protein interactions. Proc Natl Acad Sci U S A. 2001 Sep 11;98(19):10624-9.
[2]. S Suetsugu, et al. Identification of another actin-related protein (Arp) 2/3 complex binding site in neural Wiskott-Aldrich syndrome protein (N-WASP) that complements actin polymerization induced by the Arp2/3 complex activating (VCA) domain of N-WASP. J Biol Chem. 2001 Aug 31;276(35):33175-80.
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Honglin Li, et al. Pd-1 targeting polypeptide and use thereof. WO2017162208A1
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders[1].
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. T Adachi, et al. The mapping of the Lyn kinase binding site of the common beta subunit of IL-3/granulocyte-macrophage colony-stimulating factor/IL-5 receptor. J Immunol. 1999 Feb 1;162(3):1496-501.
[2]. T Adachi, et al. A novel Lyn-binding peptide inhibitor blocks eosinophil differentiation, survival, and airway eosinophilic inflammation. J Immunol. 1999 Jul 15;163(2):939-46.
PDZ1 Domain inhibitor peptide TFA Chemical Structure
规格
是否有货
100 mg
;
询价
;
250 mg
;
询价
;
500 mg
;
询价
;
* Please select Quantity before adding items.
生物活性
PDZ1 Domain inhibitor peptide TFA, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95). PDZ1 Domain inhibitor peptide TFA disrupts the GluR6/PSD-95 interaction and is very efficient in competing against the C terminus of GluR6 for the PDZ1 domain[1].
分子量
933.97
Formula
C40H62F3N9O13
Sequence Shortening
YKKTEAV (Lactam bridge:Lys3-Glu5)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献
[1]. Andrea Piserchio, et al. Targeting specific PDZ domains of PSD-95; structural basis for enhanced affinity and enzymatic stability of a cyclic peptide. Chem Biol. 2004 Apr;11(4):469-73.
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gao Y, Xing J, et al. Trp(56) of rac1 specifies interaction with a subset of guanine nucleotide exchange factors [published correction appears in J Biol Chem. 2005 Jan 14;280(2):1704]. J Biol Chem. 2001;276(50):47530-47541.
