A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Ki values of 4 and 264 nM, respectively[1].
A2A receptor antagonist 1 (CPI-444 analog) is a potent adenosine A2A receptor antagonist, selective over the A1 receptor and demonstrates its binding activity with Ki values of 4 and 264 nM, respectively[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
309.30
Formula
C16H12FN5O
CAS 号
443103-97-7
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Gillespie RJ, et al. Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines. Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9.
AA92593 is a selective and competitive OPN4 (melanopsin) antagonist[1][2].
体外研究 (In Vitro)
AA92593 is a competitive melanopsin antagonist, its presence in the retinal-binding pocket of melanopsin leads to the displacement of retinal, which could trigger a downstream signaling that would ultimately result in Per1 increased expression[1]. AA92593 is shown to be specific because it competes with retinaldehyde for the melanopsin retinal binding site which is very distinct from other opsins[1]. Inhibition of melanopsin activity with AA92593 increases a-MSH expression and induces melanin dispersion in the melanophores, which darkens the embryo[3]. AA92593 exhibits an IC50 of 665 nM in CHOOpn4 cells[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
Melan-a melanocytes and B16-F10 melanoma cells[1].
Concentration:
10 μM.
Incubation Time:
1 hour (heat 39.5 °C).
Result:
Pharmacologically inhibited melanopsin.
体内研究 (In Vivo)
AA92593 is able to decrease IOP in rabbits living under normal light condition[2]. AA92593 produces an increment in melatonin levels resulting in a drop of IOP[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Wild type (WT) mice[4].
Dosage:
30 mg/kg.
Administration:
IP 20 min prior to PLR measurement.
Result:
Attenuated pupil constriction in response to light (1013 ph.cm−2.s−1) by ~50%.
分子量
269.36
Formula
C13H19NO3S
CAS 号
457961-34-1
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Maria Nathália Moraes, et al. Melanopsin, a Canonical Light Receptor, Mediates Thermal Activation of Clock Genes. Sci Rep. 2017 Oct 25;7(1):13977.
[2]. Victoria Eugenia Lledó, et al. Yellow Filter Effect on Melatonin Secretion in the Eye: Role in IOP Regulation. Curr Eye Res. 2019 Jun;44(6):614-618.
[3]. Gabriel E Bertolesi, et al. Melanopsin photoreception in the eye regulates light-induced skin colour changes through the production of α-MSH in the pituitary gland. Pigment Cell Melanoma Res. 2015 Sep;28(5):559-71.
[4]. Kenneth A Jones, et al. Small-molecule antagonists of melanopsin-mediated phototransduction. Nat Chem Biol. 2013 Oct;9(10):630-5.
PINT-87aa, an 87-amino acid (aa) peptide, is encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT). PINT-87aa directly interacts with polymerase associated factor complex (PAF1c) and inhibits the transcriptional elongation of multiple oncogenes. PINT-87aa suppresses glioblastoma cell proliferation in vitro and in vivo[1].
体外研究 (In Vitro)
Both 456 and 4121 cells overexpressing PINT-87aa exhibits G1 arrest and reduces cell proliferation without obvious cellular toxicity, whereas PINT-87aa K.O. SW1783 and Hs683 cells shows increased cell cycle and cell proliferation rates[1]. The mRNA of PAF1 downstream genes (CPEB1, SOX-2, c-Myc, etc.) is inhibited transcriptionally in PIN87aa-overexpressing 456 and 4121 cells compared with that in control cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
456 and 4121 cells stably overexpressing PINT-87aa exhibits decreased in situ tumorigenic potential compared with control cells, as assessed by tumor growth and animal survival in mice[1]. PINT-87aa K.O. cells results in significantly increased xenograft tumor volumes of nude mice[1].
Shanghai Jinpan Biotech Co Ltd 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.
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 (<0)
1. Try to dissolve the peptide in water first. 2. If water fails, add NH4OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>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]. Zhang M, et, al. A peptide encoded by circular form of LINC-PINT suppresses oncogenic transcriptional elongation in glioblastoma. Nat Commun. 2018 Oct 26;9(1):4475.
PINT-87aa, an 87-amino acid (aa) peptide, is encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT). PINT-87aa directly interacts with polymerase associated factor complex (PAF1c) and inhibits the transcriptional elongation of multiple oncogenes. PINT-87aa suppresses glioblastoma cell proliferation in vitro and in vivo[1].
体外研究 (In Vitro)
Both 456 and 4121 cells overexpressing PINT-87aa exhibits G1 arrest and reduces cell proliferation without obvious cellular toxicity, whereas PINT-87aa K.O. SW1783 and Hs683 cells shows increased cell cycle and cell proliferation rates[1]. The mRNA of PAF1 downstream genes (CPEB1, SOX-2, c-Myc, etc.) is inhibited transcriptionally in PIN87aa-overexpressing 456 and 4121 cells compared with that in control cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
456 and 4121 cells stably overexpressing PINT-87aa exhibits decreased in situ tumorigenic potential compared with control cells, as assessed by tumor growth and animal survival in mice[1]. PINT-87aa K.O. cells results in significantly increased xenograft tumor volumes of nude mice[1].
上海金畔生物科技有限公司 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.
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 (<0)
1. Try to dissolve the peptide in water first. 2. If water fails, add NH4OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>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]. Zhang M, et, al. A peptide encoded by circular form of LINC-PINT suppresses oncogenic transcriptional elongation in glioblastoma. Nat Commun. 2018 Oct 26;9(1):4475.
PINT-87aa, an 87-amino acid (aa) peptide, is encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT). PINT-87aa directly interacts with polymerase associated factor complex (PAF1c) and inhibits the transcriptional elongation of multiple oncogenes. PINT-87aa suppresses glioblastoma cell proliferation in vitro and in vivo[1].
体外研究 (In Vitro)
Both 456 and 4121 cells overexpressing PINT-87aa exhibits G1 arrest and reduces cell proliferation without obvious cellular toxicity, whereas PINT-87aa K.O. SW1783 and Hs683 cells shows increased cell cycle and cell proliferation rates[1]. The mRNA of PAF1 downstream genes (CPEB1, SOX-2, c-Myc, etc.) is inhibited transcriptionally in PIN87aa-overexpressing 456 and 4121 cells compared with that in control cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
456 and 4121 cells stably overexpressing PINT-87aa exhibits decreased in situ tumorigenic potential compared with control cells, as assessed by tumor growth and animal survival in mice[1]. PINT-87aa K.O. cells results in significantly increased xenograft tumor volumes of nude mice[1].
Shanghai Jinpan Biotech Co Ltd 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.
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 (<0)
1. Try to dissolve the peptide in water first. 2. If water fails, add NH4OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>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]. Zhang M, et, al. A peptide encoded by circular form of LINC-PINT suppresses oncogenic transcriptional elongation in glioblastoma. Nat Commun. 2018 Oct 26;9(1):4475.
