标签归档：inhibitor

187-1, N-WASP inhibitor TFA

发表于由
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187-1, N-WASP inhibitor TFA;

187-1, N-WASP inhibitor TFA 是一种14-aa 环肽，也是一种变构神经 Wiskott Aldrich 综合征蛋白 (N-WASP) 抑制剂。187-1, N-WASP inhibitor TFA 有效抑制由磷脂酰肌醇 4,5-二磷酸酯 (PIP2) 诱导的肌动蛋白装配，IC50 为 2 μM。187-1, N-WASP inhibitor TFA 通过稳定蛋白质的自抑制状态，阻止了 N-WASP 激活 Arp2/3。

187-1, N-WASP inhibitor TFAamp;;

187-1, N-WASP inhibitor TFA Chemical Structure

规格 是否有货
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生物活性

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].

分子量

1898.13

Formula

C98H123F3N18O18
Sequence

Cyclo[Gln-Lys-{d-Phe}-{d-Pro}-{d-Phe}-Phe-{d-Pro}-Gln-Lys-{d-Phe}-{d-Pro}-{d-Phe}-Phe-{d-Pro}]
Sequence Shortening

Cyclo[QK-{d-Phe}-{d-Pro}-{d-Phe}-F-{d-Pro}-QK-{d-Phe}-{d-Pro}-{d-Phe}-F-{d-Pro}]
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.
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.

Human PD-L1 inhibitor II

发表于由

Human PD-L1 inhibitor II;

Human PD-L1 inhibitor II 是有效 PD-L1 抑制剂，具有抗癌活性。

Human PD-L1 inhibitor IIamp;;

Human PD-L1 inhibitor II Chemical Structure

CAS No. : 2135542-85-5

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity[1].

分子量

2219.45

Formula

C103H151N25O30
CAS 号

2135542-85-5
Sequence

Phe-Asn-Trp-Asp-Tyr-Ser-Leu-Glu-Glu-Leu-Arg-Glu-Lys-Ala-Lys-Tyr-Lys
Sequence Shortening

FNWDYSLEELREKAKYK
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]. Honglin Li, et al. Pd-1 targeting polypeptide and use thereof. WO2017162208A1

Lyn peptide inhibitor TFA

发表于由

Lyn peptide inhibitor TFA;

Lyn peptide inhibitor TFA 是一种有效的，可以细胞渗透的抑制剂，抑制 Lyn 偶联的 IL-5 受体相关信号通路，同时保持其他信号的完整。Lyn peptide inhibitor TFA 可以阻断 Lyn 的激活，抑制 Lyn 酪氨酸激酶与 IL-3/GM-CSF/IL-5 受体的 βc 亚基结合。Lyn peptide inhibitor TFA可用于哮喘、过敏等嗜酸性疾病的研究。

Lyn peptide inhibitor TFAamp;;

Lyn peptide inhibitor TFA Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

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].

IC50 Target[1][2]

IL-5

;

IL-3

;

分子量

2484.90

Formula

C116H186F3N30O26
Sequence

Stearoyl-Tyr-Gly-Tyr-Arg-Leu-Arg-Arg-Lys-Trp-Glu-Glu-Lys-Ile-Pro-Asn-Pro-NH2
Sequence Shortening

Stearoyl-YGYRLRRKWEEKIPNP-NH2
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.
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

发表于由

PDZ1 Domain inhibitor peptide TFA;

PDZ1 Domain inhibitor peptide TFA 是一种环状肽，结合 β-Ala 内酰胺侧链接头，并靶向 PSD-95 的 PDZ1 域。PDZ1 Domain inhibitor peptide TFA 破坏 GluR6/PSD-95 的相互作用，可以与 GluR6 的 C 末端竞争在 PDZ1 域的结合。

PDZ1 Domain inhibitor peptide TFAamp;;

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 ;

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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.

Rac1 Inhibitor W56

发表于由

Rac1 Inhibitor W56;

Rac1 Inhibitor W56 是 Rac1 中的残基 45-60。Rac1 Inhibitor W56 抑制 Rac1 与鸟嘌呤核苷酸交换因子 TrioN、GEF-H1 和 Tiam 的相互作用。

Rac1 Inhibitor W56amp;;

Rac1 Inhibitor W56 Chemical Structure

CAS No. : 1095179-01-3

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
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Rac1 Inhibitor W56 的其他形式现货产品:

Rac1 Inhibitor W56 TFA

生物活性

Rac1 Inhibitor W56 is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam[1].

分子量

1671.93

Formula

C74H117N19O23S
CAS 号

1095179-01-3
Sequence

Met-Val-Asp-Gly-Lys-Pro-Val-Asn-Leu-Gly-Leu-Trp-Asp-Thr-Ala-Gly
Sequence Shortening

MVDGKPVNLGLWDTAG
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.
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.

PSI(Synonyms: Proteasome Inhibitor 1)

发表于由

PSI;(Synonyms: Proteasome Inhibitor 1)

PSI (Proteasome Inhibitor 1) 是一种有效的蛋白酶体 proteasome 抑制剂。PSI 抑制原发性渗出性淋巴瘤 (PEL) 细胞的增殖。PSI具有研究卡波济氏肉瘤相关疱疹病毒 (KSHV) 感染和 KSHV 相关淋巴瘤的潜力。

PSIamp;;(Synonyms: Proteasome Inhibitor 1)

PSI Chemical Structure

CAS No. : 158442-41-2

规格 是否有货
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250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas[1].

体外研究
(In Vitro)

PSI (24 h) inhibits the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively)[1].
PSI (50 nM; 6 h) increases caspase-3/7 activity by 8-fold compared with control[1].
PSI (50 nM; 6 h) decreases the transcriptional activity of NF-κB by 52%[1].
PSI (1, 5 nM; 3 days) inhibits the growth of BC3 cells at a high concentration (5 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: BC3, BCBL1, Ramos, BJAB cells
Concentration:
Incubation Time: 24 h
Result: Inhibited the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively).

Western Blot Analysis[1]

Cell Line: HBL6 cells
Concentration: 50 nM
Incubation Time: 6 h
Result: Decreased the NF-κB activity by 52%.

分子量

618.76

Formula

C32H50N4O8
CAS 号

158442-41-2
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.
参考文献

  • [1]. Saji C, et al. Proteasome inhibitors induce apoptosis and reduce viral replication in primary effusion lymphoma cells. Biochem Biophys Res Commun. 2011; 415(4):573-8.

Rac1 Inhibitor F56, control peptide TFA

发表于由

Rac1 Inhibitor F56, control peptide TFA;

Rac1 Inhibitor F56, control peptide TFA 是一种含有 Rac1 残基 45-60 的肽。Rac1 Inhibitor F56, control peptide TFA 含有 Trp56 到 Phe56 突变。Rac1 Inhibitor F56, control peptide TFA 对 Rac1与鸟嘌呤核苷酸交换因子 (GEFs) 的相互作用没有影响。

Rac1 Inhibitor F56, control peptide TFAamp;;

Rac1 Inhibitor F56, control peptide TFA Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

Rac1 Inhibitor F56, control peptide TFA is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor F56, control peptide TFA contains a Trp56 to Phe56 mutation. Rac1 Inhibitor F56, control peptide TFA has no effect on Rac1 interaction with its guanine nucleotide exchange factors (GEFs)[1].

分子量

1746.91

Formula

C74H117F3N18O25S
Sequence

Met-Val-Asp-Gly-Lys-Pro-Val-Asn-Leu-Gly-Leu-Phe-Asp-Thr-Ala-Gly
Sequence Shortening

MVDGKPVNLGLFDTAG
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.
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.

PKG inhibitor peptide TFA

发表于由

PKG inhibitor peptide TFA;

PKG inhibitor peptide TFA 是一种 ATP 竞争性的 PKG 抑制剂，Ki 值为 86 μM。

PKG inhibitor peptide TFAamp;;

PKG inhibitor peptide TFA Chemical Structure

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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PKG inhibitor peptide TFA 的其他形式现货产品:

PKG inhibitor peptide

生物活性

PKG inhibitor peptide TFA 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 TFA (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

1057.13

Formula

C40H75F3N18O12
Sequence

Arg-Lys-Arg-Ala-Arg-Lys-Glu
Sequence Shortening

RKRARKE
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.
参考文献

  • [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.

Rac1 Inhibitor F56, control peptide

发表于由

Rac1 Inhibitor F56, control peptide;

Rac1 Inhibitor F56, control peptide 是一种含有Rac1残基45-60的肽。Rac1 Inhibitor F56, control peptide 含有 Trp56 到 Phe56 突变。Rac1 Inhibitor F56, control peptide 对Rac1与鸟嘌呤核苷酸交换因子 (GEFs) 的相互作用没有影响。

Rac1 Inhibitor F56, control peptideamp;;

Rac1 Inhibitor F56, control peptide Chemical Structure

CAS No. : 1315378-77-8

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

Rac1 Inhibitor F56, control peptide is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor F56, control peptide contains a Trp56 to Phe56 mutation. Rac1 Inhibitor F56, control peptide has no effect on Rac1 interaction with its guanine nucleotide exchange factors (GEFs)[1].

分子量

1632.89

Formula

C72H116N18O23S
CAS 号

1315378-77-8
Sequence

Met-Val-Asp-Gly-Lys-Pro-Val-Asn-Leu-Gly-Leu-Phe-Asp-Thr-Ala-Gly
Sequence Shortening

MVDGKPVNLGLFDTAG
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]. 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.

PDZ1 Domain inhibitor peptide

发表于由

PDZ1 Domain inhibitor peptide;

PDZ1 Domain inhibitor peptide 是一种环状肽，结合 β-Ala 内酰胺侧链接头，并靶向 PSD-95 的 PDZ1 域。PDZ1 Domain inhibitor peptide 破坏 GluR6/PSD-95 的相互作用，可以与 GluR6 的 C 末端竞争在 PDZ1 域的结合。

PDZ1 Domain inhibitor peptideamp;;

PDZ1 Domain inhibitor peptide Chemical Structure

CAS No. : 1315378-73-4

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, 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 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

819.94

Formula

C38H61N9O11
CAS 号

1315378-73-4
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.