Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3)[1].
分子量
489.55
Formula
C26H31F4N5
CAS 号
2735803-90-2
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]. Gu Peng, et al. Pyrrolidine compounds and their applications. Patent WO2021228210A1.
AHR antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, extracted from patent WO2019101641A1, compound example 1, with IC50s of 0.885 and 2.03 nM for human and mouse AhR[1].
分子量
418.37
Formula
C20H17F3N4O3
CAS 号
2338747-54-7
运输条件
Room temperature in continental US; may vary elsewhere.
RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities[1][2].
体外研究 (In Vitro)
RAGE antagonist peptide TFA (RAP) reduces the ability of the ligands to stimulate RAGE activation of NFκB in cancer cells in vitro[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)
RAGE antagonist peptide TFA (RAP, 100 µg) inhibits RAGE-mediated Basal NFκB Activity in PDAC cells in vivo[1]. RAGE antagonist peptide TFA (RAP) reduces the growth and metastasis of pancreatic tumors and also inhibited glioma tumor growth[1]. In mice bearing asthma, RAGE antagonist peptide TFA (RAP; 4 mg/kg; i.p.) blunts airway reactivity, airway inflammation and goblet cell metaplasia, and decreases release of Th2 cytokines. RAGE antagonist peptide TFA also reduces total, cytoplasmic and nuclear levels of β-catenin, enhances β-catenin phosphorylation at Ser33/37/Thr41, which triggers ubiquitination, down-regulated expression of β-catenin targeted genes, and tends to keep β-catenin at the cytomembrane, shifting β-catenin from a signalling active pattern to an adhesive function[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:
Cancer cells expressing the NFκB-luc reporter implanted into immune-deficient mice[1].
Dosage:
100 µg
Administration:
Intratumoral delivery (or intraperitoneally).
Result:
Systemic administration caused a substantial reduction (p<0.05) in the NFκB signal 5 h after injection.
分子量
1386.58
Formula
C59H102F3N13O19S
Sequence Shortening
Ac-ELKVLMEKEL-NH2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Thiruvengadam Arumugam, et al. S100P-derived RAGE antagonistic peptide reduces tumor growth and metastasis. Clin Cancer Res. 2012 Aug 15;18(16):4356-64.
[2]. Lihong Yao, et al. The receptor for advanced glycation end products is required for β-catenin stabilization in a chemical-induced asthma model. Br J Pharmacol. 2016 Sep;173(17):2600-13.
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.
LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM)[1].
IC50 & Target
IC50: 28.3 nM (LPA2); 13.85 μM (LPA3)[1]
体外研究 (In Vitro)
Lysophosphatidic acid (LPA) is a phospholipid mediator that elicits a host of biological effects including cell proliferation, survival, motility and differentiation. LPA has been shown to regulate cancer cell invasion, metastasis, and resistance to both chemotherapeutics and radiation. LPA2 antagonist 2 (H2L 5226501) inhibits LPA1 with an Imax of 59.0% at 30 µM[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
380.35
Formula
C20H16N2O6
CAS 号
36840-10-5
运输条件
Room temperature in continental US; may vary elsewhere.
CXCR7 antagonist-1 is an inhibitor of the binding of the SDF-1 chemokine (CXCL12 chemokine) or I-TAC (CXCL11) to the chemokine receptor CXCR. CXCR7 antagonist-1 prevents tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128)[1].
IC50 & Target
CXCR7
分子量
390.41
Formula
C21H19FN6O
CAS 号
1613021-99-0
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.
参考文献
[1]. Junfa Fan, et al. Cxcr7 antagonists. Patent WO2014085490A1.
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2].
IC50 & Target
IC50: 59 nM (androgen receptor)[1]
体外研究 (In Vitro)
Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNCaP and LNAR cells but not DU145 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.
Cell Proliferation Assay[1]
Cell Line:
Prostate cancer (CaP) cells (LNCAP, LNAR, and DU145)
Concentration:
1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM
Incubation Time:
7 days
Result:
Antiproliferative effects of in LNCAP and LNAR cells.
体内研究 (In Vivo)
Androgen receptor antagonist 1 (Compound 26; 100 mg/kg once a day for 5 weeks) demonstrates excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model[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.
Animal Model:
Male athymic nude mice with LNCaP xenograft model of CRPC[1]
Dosage:
100 mg/kg
Administration:
Orally once a day for 5 weeks
Result:
Demonstrated outstanding efficacy in inhibiting tumor growth. At the given doses (100 mg/kg once a day) nearly completely suppressed tumor growth (by 90 %) and the PSA levels (78%) after 5 weeks, with no detectable body weight loss for the period of time when animals were treated.
分子量
416.90
Formula
C21H25ClN4O3
CAS 号
1338812-36-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Guo C, et al. Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem. 2011 Nov 10;54(21):7693-704.
[2]. Han X, et al. Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. J Med Chem. 2019 Jan 24;62(2):941-964.
Useful FRET substrate for a continuous fluorescence-based assay of the malaria aspartyl protease (plasmepsin). The peptide sequence ERNleFLSFP is derived from the cleavage site present in hemoglobin, with Nle as a substitution for Met to avoid potential oxidation related problems.
溶解度
分子量
2629.08
化学式
C115H194N34O34S1
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
G.F.Seelig et al., J. Biol. Chem., 270, 9241 (1995)
Antagonist G TFA 是有效的后叶加压素 (vasopressin) 的拮抗剂。Antagonist G 也是弱的GRP 和缓激肽的弱拮抗剂。Antagonist G 可诱导 AG-1 的转录，是癌细胞对化疗增敏。
Antagonist G 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.
Antagonist G TFA 的其他形式现货产品:
Antagonist G
生物活性
Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy[1][2].
体外研究 (In Vitro)
Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells[2]. Antagonist G activates JNK1 in SCLC cells[2]. Antagonist G is not intrinsically a free radical oxygen donor but stimulates free radical generation specifically within SCLC cells (6.2-fold) and increases the activity of the redox-sensitive transcription factor AP-1 by 61%[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells.
Concentration:
0-100 μM.
Incubation Time:
24 h.
Result:
Inhibited cell growh.
分子量
1065.21
Formula
C51H67F3N12O8S
Sequence Shortening
RW-{Me-Phe}-WLM-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.
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]. P J Woll, et al. A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 1990 Jul 1;50(13):3968-73.
[2]. A C MacKinnon, et al. [Arg6, D-Trp7,9, NmePhe8]-substance P (6–11) (antagonist G) inducesP-1 transcription and sensitizes cells to chemotherapy. Br J Cancer. 2000 Oct; 83(7): 941–948.
Antagonist G TFA 是有效的后叶加压素 (vasopressin) 的拮抗剂。Antagonist G 也是弱的GRP 和缓激肽的弱拮抗剂。Antagonist G 可诱导 AG-1 的转录，是癌细胞对化疗增敏。
Antagonist G 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.
Antagonist G TFA 的其他形式现货产品:
Antagonist G
生物活性
Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy[1][2].
体外研究 (In Vitro)
Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells[2]. Antagonist G activates JNK1 in SCLC cells[2]. Antagonist G is not intrinsically a free radical oxygen donor but stimulates free radical generation specifically within SCLC cells (6.2-fold) and increases the activity of the redox-sensitive transcription factor AP-1 by 61%[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.
Cell Viability Assay[2]
Cell Line:
SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells.
Concentration:
0-100 μM.
Incubation Time:
24 h.
Result:
Inhibited cell growh.
分子量
1065.21
Formula
C51H67F3N12O8S
Sequence Shortening
RW-{Me-Phe}-WLM-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.
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]. P J Woll, et al. A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 1990 Jul 1;50(13):3968-73.
[2]. A C MacKinnon, et al. [Arg6, D-Trp7,9, NmePhe8]-substance P (6–11) (antagonist G) inducesP-1 transcription and sensitizes cells to chemotherapy. Br J Cancer. 2000 Oct; 83(7): 941–948.
Antagonist G TFA 是有效的后叶加压素 (vasopressin) 的拮抗剂。Antagonist G 也是弱的GRP 和缓激肽的弱拮抗剂。Antagonist G 可诱导 AG-1 的转录，是癌细胞对化疗增敏。
Antagonist G 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.
Antagonist G TFA 的其他形式现货产品:
Antagonist G
生物活性
Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy[1][2].
体外研究 (In Vitro)
Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells[2]. Antagonist G activates JNK1 in SCLC cells[2]. Antagonist G is not intrinsically a free radical oxygen donor but stimulates free radical generation specifically within SCLC cells (6.2-fold) and increases the activity of the redox-sensitive transcription factor AP-1 by 61%[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells.
Concentration:
0-100 μM.
Incubation Time:
24 h.
Result:
Inhibited cell growh.
分子量
1065.21
Formula
C51H67F3N12O8S
Sequence Shortening
RW-{Me-Phe}-WLM-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.
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]. P J Woll, et al. A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 1990 Jul 1;50(13):3968-73.
[2]. A C MacKinnon, et al. [Arg6, D-Trp7,9, NmePhe8]-substance P (6–11) (antagonist G) inducesP-1 transcription and sensitizes cells to chemotherapy. Br J Cancer. 2000 Oct; 83(7): 941–948.
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities[1][2].
体外研究 (In Vitro)
RAGE antagonist peptide (RAP) reduces the ability of the ligands to stimulate RAGE activation of NFκB in cancer cells in vitro[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)
RAGE antagonist peptide (RAP, 100 µg) inhibits RAGE-mediated Basal NFκB Activity in PDAC cells in vivo[1]. RAGE antagonist peptide (RAP) reduces the growth and metastasis of pancreatic tumors and also inhibited glioma tumor growth[1]. In mice bearing asthma, RAGE antagonist peptide (RAP; 4 mg/kg; i.p.) blunts airway reactivity, airway inflammation and goblet cell metaplasia, and decreases release of Th2 cytokines. RAGE antagonist peptide also reduces total, cytoplasmic and nuclear levels of β-catenin, enhanced β-catenin phosphorylation at Ser33/37/Thr41, which triggers ubiquitination, down-regulated expression of β-catenin targeted genes, and tends to keep β-catenin at the cytomembrane, shifting β-catenin from a signalling active pattern to an adhesive function[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Cancer cells expressing the NFκB-luc reporter implanted into immune-deficient mice[1].
Dosage:
100 µg.
Administration:
Intratumoral delivery (or intraperitoneally).
Result:
Systemic administration caused a substantial reduction (p<0.05) in the NFκB signal 5 h after injection.
分子量
1272.56
Formula
C57H101N13O17S
CAS 号
1092460-91-7
Sequence Shortening
Ac-ELKVLMEKEL-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]. Thiruvengadam Arumugam, et al. S100P-derived RAGE antagonistic peptide reduces tumor growth and metastasis. Clin Cancer Res. 2012 Aug 15;18(16):4356-64.
[2]. Lihong Yao, et al. The receptor for advanced glycation end products is required for β-catenin stabilization in a chemical-induced asthma model. Br J Pharmacol. 2016 Sep;173(17):2600-13.
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities[1][2].
体外研究 (In Vitro)
RAGE antagonist peptide (RAP) reduces the ability of the ligands to stimulate RAGE activation of NFκB in cancer cells in vitro[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)
RAGE antagonist peptide (RAP, 100 µg) inhibits RAGE-mediated Basal NFκB Activity in PDAC cells in vivo[1]. RAGE antagonist peptide (RAP) reduces the growth and metastasis of pancreatic tumors and also inhibited glioma tumor growth[1]. In mice bearing asthma, RAGE antagonist peptide (RAP; 4 mg/kg; i.p.) blunts airway reactivity, airway inflammation and goblet cell metaplasia, and decreases release of Th2 cytokines. RAGE antagonist peptide also reduces total, cytoplasmic and nuclear levels of β-catenin, enhanced β-catenin phosphorylation at Ser33/37/Thr41, which triggers ubiquitination, down-regulated expression of β-catenin targeted genes, and tends to keep β-catenin at the cytomembrane, shifting β-catenin from a signalling active pattern to an adhesive function[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:
Cancer cells expressing the NFκB-luc reporter implanted into immune-deficient mice[1].
Dosage:
100 µg.
Administration:
Intratumoral delivery (or intraperitoneally).
Result:
Systemic administration caused a substantial reduction (p<0.05) in the NFκB signal 5 h after injection.
分子量
1272.56
Formula
C57H101N13O17S
CAS 号
1092460-91-7
Sequence Shortening
Ac-ELKVLMEKEL-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]. Thiruvengadam Arumugam, et al. S100P-derived RAGE antagonistic peptide reduces tumor growth and metastasis. Clin Cancer Res. 2012 Aug 15;18(16):4356-64.
[2]. Lihong Yao, et al. The receptor for advanced glycation end products is required for β-catenin stabilization in a chemical-induced asthma model. Br J Pharmacol. 2016 Sep;173(17):2600-13.
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities[1][2].
体外研究 (In Vitro)
RAGE antagonist peptide (RAP) reduces the ability of the ligands to stimulate RAGE activation of NFκB in cancer cells in vitro[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)
RAGE antagonist peptide (RAP, 100 µg) inhibits RAGE-mediated Basal NFκB Activity in PDAC cells in vivo[1]. RAGE antagonist peptide (RAP) reduces the growth and metastasis of pancreatic tumors and also inhibited glioma tumor growth[1]. In mice bearing asthma, RAGE antagonist peptide (RAP; 4 mg/kg; i.p.) blunts airway reactivity, airway inflammation and goblet cell metaplasia, and decreases release of Th2 cytokines. RAGE antagonist peptide also reduces total, cytoplasmic and nuclear levels of β-catenin, enhanced β-catenin phosphorylation at Ser33/37/Thr41, which triggers ubiquitination, down-regulated expression of β-catenin targeted genes, and tends to keep β-catenin at the cytomembrane, shifting β-catenin from a signalling active pattern to an adhesive function[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Cancer cells expressing the NFκB-luc reporter implanted into immune-deficient mice[1].
Dosage:
100 µg.
Administration:
Intratumoral delivery (or intraperitoneally).
Result:
Systemic administration caused a substantial reduction (p<0.05) in the NFκB signal 5 h after injection.
分子量
1272.56
Formula
C57H101N13O17S
CAS 号
1092460-91-7
Sequence Shortening
Ac-ELKVLMEKEL-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]. Thiruvengadam Arumugam, et al. S100P-derived RAGE antagonistic peptide reduces tumor growth and metastasis. Clin Cancer Res. 2012 Aug 15;18(16):4356-64.
[2]. Lihong Yao, et al. The receptor for advanced glycation end products is required for β-catenin stabilization in a chemical-induced asthma model. Br J Pharmacol. 2016 Sep;173(17):2600-13.
AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC50 of 82.2 nM. AHR antagonist 4 has anti-cancer effects[1].
AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC50 of 82.2 nM. AHR antagonist 4 has anti-cancer effects[1].
AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC50 of 82.2 nM. AHR antagonist 4 has anti-cancer effects[1].
EP4 receptor antagonist 3 is a potent EP4 receptor antagonist, example 3,extracted from patent WO2010019796 A1. EP4 receptor antagonist 3 can be used for the reseacrh of EP4 receptor-mediated diseases, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer[1].
IC50 & Target[1]
EP4
分子量
498.52
Formula
C26H21F3N2O3S
CAS 号
1207954-34-4
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]. Wei W. Yuan, et al. Heterocyclic amide derivatives as ep4 receptor antagonists. Patent WO2010019796A1.
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