(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury[1][2][3].
体外研究 (In Vitro)
(S)-Coriolic acid (25μM) causes mitochondrial structural alterations and injury in bronchial epithelium[2]. (S)-Coriolic acid (30 nM; 6 hours; E-FABP-/- keratinocytes) induces K1 expression through NF-κB activation. (S)-Coriolic acid increases the phosphorylation of IκBαat serine 32, which induces IκB degradation and thereby activates NF-κB. (S)-Coriolic acid also increases the phosphorylation of Ikkinase-bat tyrosine 199, which promotes IκBα phosphorylation and subsequent NF-kB activation[3].
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)
(S)-Coriolic acid (0-0.6 mg per mouse; Intranasally once a day for 3 consecutive days) causes severe airway dysfunction, airway neutrophilia, mitochondrial dysfunction and epithelial injury[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
BALB/c mice (6-8 weeks)[2]
Dosage:
0-0.6 mg per mouse
Administration:
Intranasally once a day for 3 consecutive days
Result:
BALB/c mice developed features of mitochondrial dysfunction such as reduction in mitochondrial membrane potential, reduction in complex IV activity in lung mitochondria, and increase in the levels of cytochrome c in lung cytosol.
分子量
296.44
Formula
C18H32O3
CAS 号
29623-28-7
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]. Yuan H, et al. 15-Lipoxygenases and its metabolites 15(S)-HETE and 13(S)-HODE in the development of non-small cell lung cancer. Thorax. 2010;65(4):321-326.
[2]. Mabalirajan U, et al. Linoleic acid metabolite drives severe asthma by causing airway epithelial injury. Sci Rep. 2013;3:1349.
[3]. Ogawa E, et al. Epidermal FABP (FABP5) regulates keratinocyte differentiation by 13(S)-HODE-mediated activation of the NF-κB signaling pathway. J Invest Dermatol. 2011;131(3):604-612.
[4]. Yuan H, et al. 15-Lipoxygenases and its metabolites 15(S)-HETE and 13(S)-HODE in the development of non-small cell lung cancer. Thorax. 2010;65(4):321-326.
CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity[1][2][3].
IC50 & Target
IC50: 0.75 μM (HA22T)[1]
体外研究 (In Vitro)
CHM-1 (0-100μM; 24 hours) induces significant concentration-dependent growth inhibition in HA22T, Hep3B, and HepG2 cells, with the most potent effects observed in HA22T cells (IC50 = 0.75 μM)[1]. CHM-1 (0-10 μM; 24 hours) significantly increases the binding of cyclin B1 to Cdc2 in HA22T 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 Viability Assay[1]
Cell Line:
HA22T, Hep3B, and HepG2 cells
Concentration:
0-100 μM
Incubation Time:
24 hours
Result:
Induced G2-M arrest of the cell cycle followed by apoptosis.
Western Blot Analysis[1]
Cell Line:
HA22T cells
Concentration:
0-10 μM
Incubation Time:
24 hours
Result:
Induced change in expressed and phosphorylated status of G2-M regulators in human hepatocellular carcinoma cells.
体内研究 (In Vivo)
CHM-1 (10 mg/kg; I.p.) induces a dose-dependent inhibition of HA22T tumor growth[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 severe combined immunodeficient mice (HA22T)[1]
Dosage:
10 mg/kg
Administration:
I.p.
Result:
Induced a dose-dependent inhibition of HA22T tumor growth.
分子量
283.25
Formula
C16H10FNO3
CAS 号
154554-41-3
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]. Wang SW, et al. CHM-1, a novel synthetic quinolone with potent and selective antimitotic antitumor activity against human hepatocellular carcinoma in vitro and in vivo. Mol Cancer Ther. 2008 Feb;7(2):350-60.
[2]. Liu CW, et al. CHM-1, a novel microtubule-destabilizing agent exhibits antitumor activity via inducing the expression of SIRT2 in human breast cancer cells. Chem Biol Interact. 2018 Jun 1;289:98-108.
[3]. Tsai AC, et al. CHM-1, a new vascular targeting agent, induces apoptosis of human umbilical vein endothelial cells via p53-mediated death receptor 5 up-regulation. J Biol Chem. 2010 Feb 19;285(8):5497-506.
MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].
IC50 & Target[1]
KRas G12C
体外研究 (In Vitro)
LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC50s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via a bona fide PROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h[1]. LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
662.15
Formula
C34H37ClFN7O4
CAS 号
2561529-96-0
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]. Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375.
Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
184.23
Formula
C12H8D2N2
中文名称
哈尔满碱 d2
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Louis ED, et, al. Blood harmane concentrations and dietary protein consumption in essential tremor. Neurology. 2005 Aug 9;65(3):391-6.
[3]. Musgrave IF, et, al. Harmane produces hypotension following microinjection into the RVLM: possible role of I(1)-imidazoline receptors. Br J Pharmacol. 2000 Mar;129(6):1057-9.
[4]. Glover V, et, al. β-Carbolines as selective monoamine oxidase inhibitors:In vivo implications
[5]. Umezawa K, et, al. Comutagenic effect of norharman and harman with 2-acetylaminofluorene derivatives. Proc Natl Acad Sci U S A. 1978 Feb;75(2):928-30.
Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM)[1].
IC50 & Target
IC50: 3 μM (P2X1 receptor)
体外研究 (In Vitro)
Ro 0437626 reduces PMA-evoked Ca2+entry with 6.8 ± 4.7% of control[2].
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)
Ro 0437626 (1 and 10 μmol/kg; i.v.) causes a reduction in postinfusion isovolumetric contractions[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Female rat (urethane-anaesthetized)[3]
Dosage:
1 and 10 μmol/kg
Administration:
I.v.
Result:
Caused a reduction in postinfusion isovolumetric contractions.
分子量
525.66
Formula
C27H35N5O4S
CAS 号
134362-79-1
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]. Jaime-Figueroa S, et al. Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist. Bioorg Med Chem Lett. 2005;15(13):3292-3295.
[2]. Harper MT, et al. Phorbol ester-evoked Ca2+ signaling in human platelets is via autocrine activation of P(2X1) receptors, not a novel non-capacitative Ca2+ entry. J Thromb Haemost. 2010;8(7):1604-1613.
[3]. King BF, et al. Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats. Br J Pharmacol. 2004;142(3):519-530.
C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects[1][2].
分子量
397.63
Formula
C24H47NO3
CAS 号
124753-97-5
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]. Zhu Q, et, al. C6-ceramide synergistically potentiates the anti-tumor effects of histone deacetylase inhibitors via AKT dephosphorylation and α-tubulin hyperacetylation both in vitro and in vivo. Cell Death Dis. 2011 Jan 27;2(1):e117.
[2]. Liu L, et, al. C6-ceramide treatment inhibits the proangiogenic activity of multiple myeloma exosomes via the miR-29b/Akt pathway. J Transl Med. 2020 Aug 3;18(1):298.
Intoplicine dimesylate(Synonyms: RP 60475 dimesylate) 纯度: 98.28%
Intoplicine (RP 60475) dimesylate，一种 7H 苯并 [e] 吡啶并 [4,3-b] 吲哚系列的抗肿瘤衍生物，是一种 DNA 拓扑异构酶 I 和 II 抑制剂。Intoplicine dimesylate 与 DNA (KA = 2 x 105 /M) 强烈结合，从而增加线性 DNA 的长度。
Intoplicine dimesylate Chemical Structure
CAS No. : 133711-99-6
规格
价格
是否有货
数量
5 mg
￥8000
In-stock
10 mg
￥13000
In-stock
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
Intoplicine dimesylate 相关产品
•相关化合物库:
Clinical Compound Library Plus
Bioactive Compound Library Plus
生物活性
Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2].
IC50 & Target
Topoisomerase I
Topoisomerase II
体外研究 (In Vitro)
With 1-hour exposure to Intoplicine dimesylate at final concentrations of 2.5 micrograms/mL and 10.0 micrograms/mL, 26% and 54% of the assessable specimens shows positive in vitro responses, respectively[2]. With continuous exposure to Intoplicine dimesylate at concentrations of 0.25 micrograms/mL and 2.5 micrograms/mL, 16% and 71% of the assessable specimens showed positive responses, respectively[2]. Activity is seen against breast (71%), non-small-cell lung (69%), and ovarian (45%) cancer colony-forming units at a Intoplicine dimesylate concentration of 10.0 micrograms/mL after 1-hour exposure[2].
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)
At the highest non-toxic dose (HNTD) (6 mg/kg/injection, total dose, 36 mg/kg), intoplicine dimesylate shows highly active with a T/C of 0% and a corresponding total log cell kill of 3[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
540.65
Formula
C23H32N4O7S2
CAS 号
133711-99-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : 115 mg/mL (212.71 mM; Need ultrasonic)
H2O : 100 mg/mL (184.96 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.8496 mL
9.2481 mL
18.4963 mL
5 mM
0.3699 mL
1.8496 mL
3.6993 mL
10 mM
0.1850 mL
0.9248 mL
1.8496 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
[1]. Riou JF, et al. Intoplicine (RP 60475) and its derivatives, a new class of antitumor agents inhibiting both topoisomerase I and II activities. Cancer Res. 1993;53(24):5987-5993.
[2]. Eckardt JR, et al. Activity of intoplicine (RP60475), a new DNA topoisomerase I and II inhibitor, against human tumor colony-forming units in vitro. J Natl Cancer Inst. 1994;86(1):30-33.
[3]. Bissery MC, et al. Antitumor activity of intoplicine (RP 60475, NSC 645008), a new benzo-pyrido-indole: evaluation against solid tumors and leukemias in mice. Invest New Drugs. 1993;11(4):263-277.
BM-1244 is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively. BM-1244 inhibits senescent fibroblasts (SnCs) with an EC50 of 5 nM. (From patent WO2019033119A1)[1].
分子量
1159.79
Formula
C54H59ClF4N6O8S4
CAS 号
1619923-32-8
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Jill Hopkins, et al. Treatment of ophthalmic conditions such as macular degeneration, glaucoma, and diabetic retinopathy using pharmaceutical agents that eliminate senescent cells. WO2019033119A1.
[2]. Kim R. Unknotting the roles of Bcl-2 and Bcl-xL in cell death. Biochem Biophys Res Commun. 2005;333(2):336-343.
CDK4/6-IN-6 (example A94) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively[1].
IC50 & Target[1]
Cdk4/cyclin D1
0.6 nM (Ki)
cdk6/cyclin D3
13.9 nM (Ki)
体外研究 (In Vitro)
CDK4/6-IN-6 (example A94) has IC50s of 38.5 nM and 144.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3 using phospho-Rb S795 ELISA assays in JEKO-1 and MV4-1 1 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
463.93
Formula
C22H27ClFN5O3
CAS 号
2380321-51-5
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]. Ping Chen, et al. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors. WO2019207463A1.
MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].
IC50 & Target[1]
KRas G12C
体外研究 (In Vitro)
LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC50s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via a bona fide PROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h[1]. LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
662.15
Formula
C34H37ClFN7O4
CAS 号
2561529-96-0
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]. Bond MJ, et al. Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs. ACS Cent Sci. 2020;6(8):1367-1375.
5-Iminodaunorubicin 是一种醌改性蒽环类药物，具有抗肿瘤活性。5-Iminodaunorubicin 在癌细胞中可诱导 DNA 链断裂。
5-Iminodaunorubicin Chemical Structure
CAS No. : 72983-78-9
规格
价格
是否有货
数量
10 mM * 1 mL in DMSO
￥4050
In-stock
5 mg
￥3500
In-stock
10 mg
￥5800
In-stock
25 mg
￥11000
In-stock
50 mg
￥17000
In-stock
100 mg
询价
200 mg
询价
* Please select Quantity before adding items.
5-Iminodaunorubicin 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Anti-Blood Cancer Compound Library
生物活性
5-Iminodaunorubicin is a quinone-modified anthracycline that retains antitumor activity[1]. 5-Iminodaunorubicin produces protein-concealed DNA strand breaks in cancer cells[2].
体外研究 (In Vitro)
In mouse leukemia L1210 cells, 5-Iminodaunorubicin produces protein-concealed DNA strand breaks. Many of the 5-iminodaunorubicin breaks may arise from apposed single-strand breaks (i.e., double-strand breaks)[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.
体内研究 (In Vivo)
In rat, 5-Iminodaunorubicin (5-ID; 1-16 mg/kg) treatment produces widening of the QRS complex, increased R- and S-wave voltage, and prolonged the Q alpha T interval. And the quinone redox cycling is suppressed in 5-Iminodaunorubicin. 5-Iminodaunorubicin shows lower cardiotoxic[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
526.54
Formula
C27H30N2O9
CAS 号
72983-78-9
中文名称
5-亚氨基柔红霉素
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. R A Jensen, et al. Electrocardiographic and transmembrane potential effects of 5-iminodaunorubicin in the rat. Cancer Res. 1984 Sep;44(9):4030-9.
[2]. L A Zwelling, et al. Cytotoxicity and DNA strand breaks by 5-iminodaunorubicin in mouse leukemia L1210 cells: comparison with adriamycin and 4′-(9-acridinylamino)methanesulfon-m-anisidide. Cancer Res. 1982 Jul;42(7):2687-91.
PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function[1].
体外研究 (In Vitro)
Biphenyl acid PCSK9 degrader 1 (compound 9) binds to and thermally stabilizes PCSK9 in a complex environment such as Huh7 lysate[1]. PCSK9 degrader 1 (compound 9), with high affinity for recombinant PCSK9 and target engagement in cell lysate, could be used as a recruiting element to promote the selective degradation of PCSK9[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
631.71
Formula
C34H34FN3O6S
CAS 号
2215931-60-3
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]. Whitney L Petrilli, et al. From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9. Cell Chem Biol. 2020 Jan 16;27(1):32-40.e3.
Ro 0437626 is a selective purinergic (P2X1) receptor antagonist (IC50 = 3 μM), but shows low affinity for P2X2, P2X3 and P2X2/3 receptors (IC50 > 100 μM)[1].
IC50 & Target
IC50: 3 μM (P2X1 receptor)
体外研究 (In Vitro)
Ro 0437626 reduces PMA-evoked Ca2+entry with 6.8 ± 4.7% of control[2].
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)
Ro 0437626 (1 and 10 μmol/kg; i.v.) causes a reduction in postinfusion isovolumetric contractions[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Female rat (urethane-anaesthetized)[3]
Dosage:
1 and 10 μmol/kg
Administration:
I.v.
Result:
Caused a reduction in postinfusion isovolumetric contractions.
分子量
525.66
Formula
C27H35N5O4S
CAS 号
134362-79-1
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]. Jaime-Figueroa S, et al. Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist. Bioorg Med Chem Lett. 2005;15(13):3292-3295.
[2]. Harper MT, et al. Phorbol ester-evoked Ca2+ signaling in human platelets is via autocrine activation of P(2X1) receptors, not a novel non-capacitative Ca2+ entry. J Thromb Haemost. 2010;8(7):1604-1613.
[3]. King BF, et al. Investigation of the effects of P2 purinoceptor ligands on the micturition reflex in female urethane-anaesthetized rats. Br J Pharmacol. 2004;142(3):519-530.
JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM[1]. JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth[1].
IC50 & Target
IC50: 1.17μM (Wnt signaling)[1]
体外研究 (In Vitro)
JW67 (1 μM; 24 hours) increases concentration of AXIN2 and decreases the active form of β-catenin[1]. JW67 affects the expression of Wnt target genes and reduces cell growth of colon cancer cell lines[1]. JW67 shows a concentrationdependent reduction in proliferation with a GI50 value of 7.8 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.
Western Blot Analysis[1]
Cell Line:
SW480 cells
Concentration:
1 μM
Incubation Time:
24 hours
Result:
Increased the AXIN2 expression.
RT-PCR[1]
Cell Line:
SW480 cells
Concentration:
10 or 25μM
Incubation Time:
72 hours
Result:
Reduced growth of SW480 CRC cells in vitro by inhibiting cell-cycle progression at the G1/S.
分子量
394.38
Formula
C21H18N2O6
CAS 号
442644-28-2
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]. Waaler J, et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011;71(1):197-205.
Cl-4AS-1 是一种有效的类固醇雄激素受体 (AR) 激动剂 (IC50 为 12 nM)，也是 5α- 还原酶 I 型和 II 型的抑制剂 (IC50 分别为 6 和 10 nM)。
Cl-4AS-1 Chemical Structure
CAS No. : 188589-66-4
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
Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively)[1][2].
Cl-4AS-1 suppresses MMP-1 promoter activity in 22Rv1 human prostate cancer cells[1]. Cl-4AS-1 (10 μM) effectively promotes the AR N/C interaction, with an average maximal activity of 35.3%[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)
Cl-4AS-1 produces no significant reduction in prostate weight in intact animals and in castrates rats caused a significant increase of ventral prostate weight[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
ORX rats[1]
Dosage:
10 mg/kg
Administration:
I.s.; 7 days
Result:
Effect of Cl-4AS-1 on prostate and seminal vesicle growth.
分子量
441.01
Formula
C26H33ClN2O2
CAS 号
188589-66-4
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]. Schmidt A, et al. Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands. J Biol Chem. 2009 Dec 25;284(52):36367-36376.
[2]. Tolman RL, et al. 4-Methyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-N-aryl-carboxamides: an approach to combined androgen blockade [5alpha-reductase inhibition with androgen receptor binding in vitro]. J Steroid Biochem Mol Biol. 1997 Mar;60(5-6):303-9.
SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity[1].
IC50 & Target
IC50: 42 nM (TAO3), 237 nM (MEKK3)[1]
体外研究 (In Vitro)
SBI-581 shows moderate selectivity (> 5-10x) against the majority of a broad panel of kinases[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
383.44
Formula
C24H21N3O2
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]. Iizuka S, et al. Serine-Threonine Kinase TAO3-Mediated Trafficking of Endosomes Containing the Invadopodia Scaffold TKS5α Promotes Cancer Invasion and Tumor Growth. Cancer Res. 2021 Mar 15;81(6):1472-1485.
CDK4/6-IN-6 (example A94) is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively[1].
IC50 & Target[1]
Cdk4/cyclin D1
0.6 nM (Ki)
cdk6/cyclin D3
13.9 nM (Ki)
体外研究 (In Vitro)
CDK4/6-IN-6 (example A94) has IC50s of 38.5 nM and 144.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3 using phospho-Rb S795 ELISA assays in JEKO-1 and MV4-1 1 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
463.93
Formula
C22H27ClFN5O3
CAS 号
2380321-51-5
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]. Ping Chen, et al. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors. WO2019207463A1.
LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
LP-184 inhibits the growth of HT29, OVCAR-3, AsPC-1 and PC-3, with GI50s of 0.68, 0.6, 16 and 0.14 μM, respectively[1]. LP-184 displays IC50s of 800nM and 210 nM for anti-cancer activitie in the thymidine incorporation into cellular DNA (2 hour) and Trypan blue (48 hour) assay[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)
LP-184 (7.5 and 10 mg/kg; i.p.; 21 day) has potent 15 anti-tumor activity against MV522 tumors, producing 4/6 and 5/5 partial responses, 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.
Animal Model:
Mice (MV522 tumors) [1]
Dosage:
7.5 and 10 mg/kg
Administration:
I.p; 21day
Result:
Effective agent for human anti-tumor therapy.
分子量
304.34
Formula
C16H20N2O4
CAS 号
924835-67-6
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]. Trevor C. Mcmorris, et al. Illudin analogs useful as anticancer agents. WO2007019308A2.
SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases[1][2].
IC50 & Target[1]
5-HT7 Receptor
7.5 (pKi)
体外研究 (In Vitro)
SB-258719 (1, 3 and 10 μM; HEK 293 cells) hydrochloride produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no signifcant alteration in the maximal response to 5-CT[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)
SB-258719 (5~20 mg/kg; i.p.) hydrochloride significantly attenuates the 5-CT-induced hypothermia[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Swiss Webster mice (20~25 g)[2].
Dosage:
5~20 mg/kg
Administration:
I.p.
Result:
Significantly attenuated the 5-CT-induced hypothermia.
分子量
374.97
Formula
C18H31ClN2O2S
CAS 号
1217674-10-6
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]. Thomas DR, et al. Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br J Pharmacol. 1998;124(6):1300-1306.
[2]. Guscott MR, et al. The hypothermic effect of 5-CT in mice is mediated through the 5-HT7 receptor. Neuropharmacology. 2003;44(8):1031-1037.
[3]. Fatima S, et al. 5-Hydroxytryptamine promotes hepatocellular carcinoma proliferation by influencing β-catenin. Mol Oncol. 2016;10(2):195-212.
