YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM)[1].
IC50 Target
IC50: 25 nM (YAP–TEAD interaction)[1]
体外研究 (In Vitro)
YAP-TEAD-IN-1 (peptide 17)(2 μM) is against endogenous YAP binding to GST-TEAD (1209-426) in a GST pull-down assay, the Kd of His-YAP1209-426 is determined to be 40 nM[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Zhang Z, et al. Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction.ACS Med Chem Lett. 2014 Jul 14;5(9):993-8.
Tutuilamide A 是一种有效的猪胰弹性蛋白酶 (PPE) 抑制剂，IC50 值为 1.2 nM。Tutuilamide A 还抑制人中性粒细胞弹性蛋白酶 (HNE; IC50=0.73 nM) 和激肽释放酶 7 (KLK7; IC50=5.0 nM)。
Tutuilamide A Chemical Structure
CAS No. : 2756129-42-5
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
Tutuilamide A is a potent porcine pancreatic elastase (PPE) inhibitor, with an IC50 of 1.2 nM. Tutuilamide A also inhibits human neutrophil elastase (HNE; IC50=0.73 nM) and kallikrein 7 (KLK7; IC50=5.0 nM)[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]. Chen QY, et, al. Ahp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7. Bioorg Med Chem. 2020 Dec 1;28(23):115756.
HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively[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]. Yu W, et al. Discovery of Chromane Containing Hepatitis C Virus (HCV) NS5A Inhibitors with Improved Potency against Resistance-Associated Variants. J Med Chem. 2016 Nov 23;59(22):10228-10243. Epub 2016 Nov 9.
OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive drug[1].
OSK1 has no effect on KCa2.1, KCa2.2, KCa2.3 and KCa1.1 channels when in the micromolar concentration range, whereas it shows a moderate activity on KCa3.1 channel (also referred to as IK1 or SK4) with an IC50 value of 225 nM[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
OSK1 is lethal in mice by intracerebroventricular injection, with a LD50 (50% lethal dose) value of 2 μg/kg[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
4205.17
Formula
C28H40N4O6
CAS 号
183815-75-0
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]. Stéphanie Mouhat, et al. K+ channel types targeted by synthetic OSK1, a toxin from Orthochirus scrobiculosus scorpion venom. Biochem J. 2005 Jan 1;385(Pt 1):95-104.
Oxazine 1 perchlorate is a symmetric cationic dye (λex=653 nm, λem=666 nm).
体外研究 (In Vitro)
Oxazine 1 perchlorate (OX1) absorbs and emits light at about 653 and 666 nm in dilute aqueous solutions, respectively. It is soluble over a very wide range of polar solvents. The optical spectrum of Oxazine 1 perchlorate typically possesses an intense absorption band (λmax), which is neighbored by a shoulder at shorter wavelengths. Oxazine 1 perchlorate appears to exist almost in its monomeric form at concentrations below about 1×10-4 M in aqueous solutions. As it is expected, similar to polar ordinary liquid solvents, Oxazine 1 perchlorate shows only single fluorescence band in polar anisotropic media[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
423.89
Formula
C20H26ClN3O5
CAS 号
24796-94-9
中文名称
噁嗪高氯酸盐
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Gilani AG, et al. Estimation of ground- and excited-state dipole moments of oxazine 1 in liquid and liquid crystalline media. Spectrochim Acta A Mol Biomol Spectrosc. 2011 Jun;79(1):148-55.
Kinase Assay [1]
Oxazine 1 perchlorate doped liquid crystal samples are prepared from a pair of quartz sheets sandwiched exactly at known gap and sealed. The introduction of the dissolved Oxazine 1 perchlorate in nematic solvents is achieved by capillary action. Oxazine 1 perchlorate concentrations are chosen to be 1×10−5 M for all the liquid samples. Oxazine 1 perchlorate is studied in the nematic media up to a concentration of about 0.1%, w/w. The absorption spectra of Oxazine 1 perchlorate are recorded on a double beam spectrophotometer over a wavelength range 300 to 800 nm combined with a cell temperature controller[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Gilani AG, et al. Estimation of ground- and excited-state dipole moments of oxazine 1 in liquid and liquid crystalline media. Spectrochim Acta A Mol Biomol Spectrosc. 2011 Jun;79(1):148-55.
Pepstatin (Pepstatin A) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
Pepstatin (Pepstatin A) is a specific acid protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively[1]. Pepstatin (Pepstatin A) inhibits the recombinant HIV protease with an IC50 of 250 μM. Pepstatin shows no effect on cellular protein synthesis and probably does not exert severe cell toxicity[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Pepstatin (Pepstatin A) has a very low toxicity, with LD50s of 1090 mg/kg, 875 mg/kg, 820 mg/kg and 450 mg/kg for mice, rats, rabbits, and dogs by i.p. route, and > 2000 mg/kg for all species by oral route. Pepstatin (0.5-50 mg/kg, p.o.) suppresses stomach ulceration of the pylorus in ligated Shay rats[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
685.89
Formula
C34H63N5O9
CAS 号
26305-03-3
Sequence
IsoValeryl-Val-Val-Sta-Ala-Sta-OH
Sequence Shortening
IsoVeryl-VV-Sta-A-Sta-OH
中文名称
胃酶抑素；抑肽素；胃蛋白酶抑制剂；胃酶抑素A
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62.
[2]. Seelmeier S, et al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6.
Cell Assay [2]
Pepstatin A is freshly dissolved in DMSO at 7 mM. It is very slowly diluted (1:100) into the medium of HIV-infected H9 suspension cultures so that no pepstatin A precipitated (final concentration, 70 μM pepstatin A and 1% DMSO), and the cultures are incubated without change of culture medium for 48 hr. As control, uninfected H9 cells are also incubated with pepstatin and in addition HIV infected and uninfected cells are incubated with 1% DMSO but without pepstatin[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Umezawa H, et al. Pepstatin, a new pepsin inhibitor produced by Actinomycetes. J Antibiot (Tokyo). 1970 May;23(5):259-62.
[2]. Seelmeier S, et al. Human immunodeficiency virus has an aspartic-type protease that can be inhibited by pepstatin A. Proc Natl Acad Sci U S A. 1988 Sep;85(18):6612-6.
Oxazine 1 perchlorate is a symmetric cationic dye (λex=653 nm, λem=666 nm).
体外研究 (In Vitro)
Oxazine 1 perchlorate (OX1) absorbs and emits light at about 653 and 666 nm in dilute aqueous solutions, respectively. It is soluble over a very wide range of polar solvents. The optical spectrum of Oxazine 1 perchlorate typically possesses an intense absorption band (λmax), which is neighbored by a shoulder at shorter wavelengths. Oxazine 1 perchlorate appears to exist almost in its monomeric form at concentrations below about 1×10-4 M in aqueous solutions. As it is expected, similar to polar ordinary liquid solvents, Oxazine 1 perchlorate shows only single fluorescence band in polar anisotropic media[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
423.89
Formula
C20H26ClN3O5
CAS 号
24796-94-9
中文名称
噁嗪高氯酸盐
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Gilani AG, et al. Estimation of ground- and excited-state dipole moments of oxazine 1 in liquid and liquid crystalline media. Spectrochim Acta A Mol Biomol Spectrosc. 2011 Jun;79(1):148-55.
Kinase Assay [1]
Oxazine 1 perchlorate doped liquid crystal samples are prepared from a pair of quartz sheets sandwiched exactly at known gap and sealed. The introduction of the dissolved Oxazine 1 perchlorate in nematic solvents is achieved by capillary action. Oxazine 1 perchlorate concentrations are chosen to be 1×10−5 M for all the liquid samples. Oxazine 1 perchlorate is studied in the nematic media up to a concentration of about 0.1%, w/w. The absorption spectra of Oxazine 1 perchlorate are recorded on a double beam spectrophotometer over a wavelength range 300 to 800 nm combined with a cell temperature controller[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Gilani AG, et al. Estimation of ground- and excited-state dipole moments of oxazine 1 in liquid and liquid crystalline media. Spectrochim Acta A Mol Biomol Spectrosc. 2011 Jun;79(1):148-55.
Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
IC50 & Target[1]
ERK2
16.5 nM (IC50)
ERK1
87 nM (IC50)
体外研究 (In Vitro)
Magnolin is a natural compound abundantly found in Magnolia flos, which has been traditionally used in oriental medicine to treat headaches, nasal congestion and anti-inflammatory reactions. Magnolin targets the active pockets of ERK1 and ERK2, which are important signaling molecules in cancer cell metastasis. Magnolin inhibits NF-κB transactivation activity by suppressing the ERKs/RSK2 signaling pathway. Magnolin inhibits the production of tumor necrosis factor-α (TNF-α) and prostaglandin E2 (PGE2) by inhibiting extracellular signal-regulated kinases (ERKs), which are key signaling molecules in the regulation of cell proliferation, transformation and cancer cell metastasis. JB6 Cl41 cell migration enhanced by EGF treatment is dramatically suppressed by Magnolin treatment in a dose-dependent manner. Magnolin inhibits ERK1/2/RSK2 signaling-mediated IκBα phosphorylation at Ser32, resulting in the inhibition of NF-κB activation and cell migration[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
416.46
Formula
C23H28O7
CAS 号
31008-18-1
中文名称
木兰苷
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Lee CJ, et al. Magnolin inhibits cell migration and invasion by targeting the ERKs/RSK2 signaling pathway. BMC Cancer. 2015 Aug 8;15:576.
Cell Assay [1]
JB6 Cl41 (7×104), A549 (7×104) and NCI-H1975 (7×104) cells, and RSK2+/+ (7×104) and RSK2-/- (7×104) MEFs are seeded into culture-inserts and cultured overnight. The cells are treated with mitomycin-C (10 μg/mL) for 2 h, and the culture-inserts are removed to offer a cell-free gap. The cells are treated with the indicated doses of Magnolin (15, 30, and 60 μM) either in the presence or absence of EGF for 12 or 24 h, and cell migration is observed under a light microscope. The migrated area is measured using the Image J computer software program. To measure the Magnolin effect on cancer cell invasion, a matrigel-coated invasion chamber is used. Briefly, A549 or NCI-H1975 (2.5×104) cells are seeded into an insert chamber with FBS-free media supplemented with the indicated doses of Magnolin(15, 30, and 60 μM), and cultured in 24-well plates supplemented with complete media for the appropriate time period. The cells are fixed with 4 % formaldehyde, permeabilized with methanol and stained with crystal violet. The stained cells are observed under a light microscope and those that have migrated are counted[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Lee CJ, et al. Magnolin inhibits cell migration and invasion by targeting the ERKs/RSK2 signaling pathway. BMC Cancer. 2015 Aug 8;15:576.
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans[1][2][3][4].
IC50 & Target
IC50: 46 nM (p56 lck autophosphorylation) and 220 nM (phosphorylation of exogenous substrates by p56 lck)[1]; Apoptosis[2]; Candida albicans[2]
体外研究 (In Vitro)
Damnacanthal has > 100-fold selectivity for p56lck over the serine/threonine kinases, protein kinase A and protein kinase C, and > 40-fold selectivity for p56lck over four receptor tyrosine kinases. Damnacanthal also demonstrates modest (7-20-fold), but highly statistically significant, selectivity for p56lck over the homologous enzymes p60src and p59fyn[1]. Damnacanthal (0.1-100 μM; 1-4 days; HCT-116 and SW480 cells) treatment results in a significant reduction of cell proliferation in a concentration- and time-dependent manner[2]. Damnacanthal (1-50 μM; 72 hours; HCT-116 cells) treatment results in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM[2]. Damnacanthal (10 μM; 24 hours; HCT-116 cells) treatment significantly increases caspase 3/7 activity. Damnacanthal-induced apoptosis[2]. Damnacanthal (0.1-10 μM; 24 hours; HCT-116 cells) treatment induces NAG-1 expression in HCT-116 cells. Cyclin D1 expression is reduced at 10 μM of Damnacanthal, whereas p21 and p53 does not alter their expression. PARP cleavage is seen at 10 μM Damnacanthal treatment only in HCT-116 cells, where NAG-1 is induced[2]. Damnacanthal treatment for 2 weeks shows significant decreasing colony number in HCT-116 cells in a concentration-dependent manner. Damnacanthal-treated cells show a dramatic inhibition of clonogenic capacity. Damnacanthal-treated (1-50 μM; 48 hours) cells significantly inhibits the migration of HCT-116 cells in a concentration-dependent manner[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[2]
Cell Line:
HCT-116 and SW480 cells
Concentration:
0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time:
1, 2, and 4 days
Result:
Resulted in a significant reduction of cell proliferation in a concentration- and time-dependent manner.
Cell Cycle Analysis[2]
Cell Line:
HCT-116 cells
Concentration:
1 μM, 10 μM and 50 μM
Incubation Time:
72 hours
Result:
Resulted in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM.
Apoptosis Analysis[2]
Cell Line:
HCT-116 cells
Concentration:
10 μM
Incubation Time:
24 hours
Result:
Significantly increased caspase 3/7 activity.
Western Blot Analysis[2]
Cell Line:
HCT-116 cells
Concentration:
0.1 μM, 1 μM and 10 μM
Incubation Time:
24 hours
Result:
NAG-1 was induced in HCT-116 cells in a dose- and time-dependent manner. Cyclin D1 expression was reduced at 10 μM.
体内研究 (In Vivo)
Damnacanthal (10-100 mg/kg; oral administration; for 10-300 minutes; male ddY mice) treatment exhibits a significant antinociceptive effect in a dose-dependent manner in the formalin test. Administration of damnacanthal (100 mg/kg) shows significant inhibition of histamine-induced paw edema[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male ddY mice (5-6 weeks) injected with formalin or Histamine[4]
Dosage:
10 mg/kg, 30 mg/kg and 100 mg/kg
Administration:
Oral administration; for 10 minutes, 30 minutes, 60 minutes or 300 minutes
Result:
Significantly reduced the growth of human lung tumor without acute toxicity.
分子量
282.25
Formula
C16H10O5
CAS 号
477-84-9
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Faltynek CR, et al. Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity. Biochemistry. 1995 Sep 26;34(38):12404-10.
[2]. Nualsanit T, et al. Damnacanthal, a noni component, exhibits antitumorigenic activity in human colorectal cancer cells. J Nutr Biochem. 2012 Aug;23(8):915-23.
[3]. Aziz MY, et al. Damnacanthal is a potent inducer of apoptosis with anticancer activity by stimulating p53 and p21 genes in MCF-7 breast cancer cells. Oncol Lett. 2014 May;7(5):1479-1484.
[4]. Okusada K, et al. The antinociceptive and anti-inflammatory action of the CHCl3-soluble phase and its main active component, damnacanthal, isolated from the root of Morinda citrifolia. Biol Pharm Bull. 2011;34(1):103-7.
