分类目录归档：试剂耗材

FGTI-2734

发表于由

FGTI-2734CAS号： 1247018-19-4分子式： C26H31FN6O2S分子量： 510.63描述储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors. FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively.
储存/保存方法
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:50 mg/mL (97.92 mM)
生物活性
靶点
Farnesyl transferase (FTase):250 nM, GGTase I:520 nM
In vitro(体外研究)
FGTI-2734 (3-30 μM;?72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.?FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells.?FGTI-2734 (1-30 μM;?72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.
In vivo(体内研究)
FGTI-2734 (intraperitoneally;?100 mg/kg/daily for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors.

GSK2879552

发表于由

GSK2879552CAS号： 1401966-69-5分子式： C23H28N2O2分子量： 364.48描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
纯度
>98%
储存/保存方法
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
别名
GSK-2879552,GSK 2879552
外观
Powder
可溶性/溶解性
Water 44 mg/mL (100.59 mM)

DMSO 29 mg/mL (66.3 mM)
生物活性
靶点
Histone Demethylase
In vitro(体外研究)
GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 derepresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells. GSK2879552 is 280-fold selective over D-amino acid oxidase, allowing for direct comparison of inactivation efficiency (KIapp=520 ± 170 μM, kinact=0.12 ± 0.01 min−1, kinact/KIapp=2.3×10-4 ± 1.31×10-5 min-1 μM-1). GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines, with EC50 of 2-240 nM.
In vivo(体内研究)
GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice. There is 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrate partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI is observed for SHP77 bearing mice.

分子结构图

GSK2879552

PD0166285

发表于由

PD0166285CAS号： 185039-89-8分子式： C26H27Cl2N5O2分子量： 512.43描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.
纯度
＞98%
储存/保存方法
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
别名
PD 0166285; PD-0166285
可溶性/溶解性
DMSO : 65 mg/mL (126.85 mM; Need ultrasonic)
生物活性
靶点
Wee1；Myt1；Chk1
In vitro(体外研究)
PD0166285 is identified to inhibit Wee1 activity at nanomolar concentrations. The inhibitor abrogates G2/M checkpoint inducing early cell division. At the cellular level, 0.5 μM PD0166285 dramatically inhibits irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in seven of seven cancer cell lines tested. This G2 checkpoint abrogation by PD0166285 is demonstrated to kill cancer cells.PD0166285 does not inhibit Cdc2/cyclin B but inhibits Chk1 kinase at a much higher concentration (3433 nM). the treatment of cells with the inhibitor is related to microtubule stabilization and decrease in cyclin D transcription. Thus, PD0166285 may be a potentially useful anti-cancer therapy.
In vivo(体内研究)
PD0166285 at 0.5 μM concentration can inhibit Cdc2Y15 /T14 phosphorylation in all cell lines tested, regardless of their p53 status and pharmacological targeting of WEE1 by PD0166285 sensitizes U251-FM GBM tumors to IR in vivo.

分子结构图

PD0166285

11β,16α,17α,21-Tetrahydroxypregna-1,4-diene-3,20-dione-d5 See T296078.

发表于由

11β,16α,17α,21-Tetrahydroxypregna-1,4-diene-3,20-dione-d5 See T296078.分子式： C21H23D5O6分子量： 381.47描述储存/保存方法别名外观可溶性/溶解性参考文献

产品描述
描述
A labelled metabolite of Budesonide (B689490), an antiinflammatory agent.
储存/保存方法
-20°C Freezer
基本信息
别名
(11β,16α)-11,16,17,21-Tetrahydroxypregna-1,4-diene-3,20-dione-d5; 16α-Hydroxyprednisolone-d5;
外观
White to Off-White Solid
可溶性/溶解性
DMSO, Methanol
参考文献
参考文献
Cserhati, T., et al.: J. Pharm. Biomed. Anal., 22, 25 (2000), Dilger, K., et al.: J. Clin. Pharmacol., 47, 1532 (2007), Buchwald, P., et al.: Steroids, 73, 193 (2008),

Wnt agonist 1

发表于由

Wnt agonist 1CAS号： 853220-52-7分子式： C19H18N4O3分子量： 350.37描述应用纯度储存/保存方法别名外观可溶性/溶解性靶点

产品描述
描述

Wnt Agonist is a cell-permeable pyrimidine compound that acts as, at an IC50 > 60 μM, a potent and selective activator of Wnt signaling. In addition to mimicking the effect of Wnt, Wnt Agonist has also induced β-catenin and T-cell fate-dependent transcriptional activity in HEK-293T cells at an EC50 = 700 nM. When applied to Xenopous embryos Wnt Agonist caused substantial head defects development. Wnt Agonist has also been observed to enhance beta cell expansion in vitro. The compound is beneficial for studying the effects of Wnt pathway due to the activation of Wnt without inhibiting the activity of GSK-3β.
应用
A potent and selective activator of Wnt signaling
纯度
≥98%
储存/保存方法
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
别名
BML-284
外观
Yellowish sticky solid
可溶性/溶解性
DMSO : ≥ 100 mg/mL (285.41 mM)
生物活性
靶点
Wnt/β-catenin

分子结构图

Wnt agonist 1

Anti-CD98 Reference Antibody(KHK2898)

发表于由

Anti-CD98 Reference Antibody(KHK2898)描述宿主反应种属应用分子量纯化方法类型同种型储存/保存方法背景说明

概述
描述
内毒素：<1 eu>纯度：>95%
宿主
CHO
反应种属
Human
应用
ELISA, Kinetics (BLI), Kinetics (SPR), Flow Cyt, Functional assay
分子量
145.5 kDa
性能
纯化方法
Protein A purified
类型
Monoclonal Antibody
同种型
IgG
储存/保存方法
Store at -80℃ for one year.
靶标
背景说明
Anti-CD98 Reference Antibody(KHK2898) is expressed from CHO. The heavy chain type is huIgG1, and the light chain type is hukappa. It has a predicted MW of 145.5 kDa.

Rabbit anti-ZNF287 Polyclonal Antibody

发表于由

Rabbit anti-ZNF287 Polyclonal Antibody描述别名宿主特异性反应种属应用分子量免疫原纯化方法类型储存/保存方法UniProt

概述
描述
Rabbit polyclonal antibody to ZNF287
别名
ZNF287抗体;ZKSCAN13; Zinc finger protein 287; Zinc finger protein with KRAB and SCAN domains 13
宿主
Rabbit
特异性
Recognizes endogenous levels of ZNF287 protein.
反应种属
Human, Mouse
应用
WB 1:500 – 1:1000, IHC 1:50 – 1:100
分子量
Detects a band of approximately 80kD
Disclaimer note: The observed molecular weight of the protein may vary from the listed predicted molecular weight due to post translational modifications, post translation cleavages, relative charges, and other experimental factors.
免疫原
KLH-conjugated synthetic peptide encompassing a sequence within the center region of human ZNF287. The exact sequence is proprietary.
性能
纯化方法
The antibody was purified by immunogen affinity chromatography.
类型
Polyclonal Antibody
储存/保存方法
Shipped at 4°C. Upon delivery aliquot and store at -20°C for one year. Avoid freeze/thaw cycles.
靶标
UniProt
Q9HBT7

实验结果图

Rabbit anti-ZNF287 Polyclonal Antibody

Western blot analysis of ZNF287 expression in HEK293T (A), A549 (B), mouse brain (C) whole cell lysates.

Rabbit anti-ZNF287 Polyclonal Antibody

Immunohistochemical analysis of ZNF287 staining in human brain formalin fixed paraffin embedded tissue section. The section was pre-treated using heat mediated antigen retrieval with sodium citrate buffer (pH 6.0). The section was then incubated with the antibody at room temperature and detected using an HRP conjugated compact polymer system. DAB was used as the chromogen. The section was then counterstained with haematoxylin and mounted with DPX.

CCT128930

发表于由

CCT128930CAS号： 885499-61-6分子式： C18H20ClN5分子量： 341.84描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

产品描述
描述
CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.
纯度
98%
储存/保存方法
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO ：68 mg/mL (198.92 mM)
生物活性
靶点
Akt2 ,p70 S6K ,PKA
In vitro(体外研究)
CCT128930 exhibits marked antiproliferative activity against PTEN-deficient human tumor cell lines including U87MG human glioblastoma cells, LNCaP human prostate cancer cells and PC3 human prostate cancer cells with GI50 of 6.3 μM, 0.35 μM and 1.9 μM, respectively. Furthermore, CCT128930 causes a G1 arrest in PTEN-null U87MG human glioblastoma cells and Akt pathway blockade.
In vivo(体内研究)
CCT128930 at 25 mg/kg i.p. shows a marked antitumor effect in established PTEN-null U87MG human glioblastoma xenografts with a treated:control (T/C) ratio of 48% on day 12. In HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, CCT128930 at 40 mg/kg also produces a profound antitumor effect with complete growth arrest and a T/C ratio of 29% on day 22. CCT128930 administrated via i.v. reaches a peak concentration of 6.4 μM in plasma and is eliminated with a relatively short half-life, high volume of distribution, and rapid clearance, giving an area under the curve AUC0-∞ of 4.6 μM h. CCT128930 administrated via i.p. leads to the peak plasma drug concentration of 1.3 μM and the corresponding AUC0-∞ of 1.3 μM·h. Oral CCT128930 administration leads to the peak plasma concentration of only 0.43 μM and a correspondingly low AUC0-∞ of 0.4 μM·h.
参考文献
参考文献
  • 1. Yap TA, et al. Mol Cancer Ther. 2011, 10(2), 360-371.
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    分子结构图

    CCT128930

    GGTI-287

    发表于由

    GGTI-287分子式： C22H29N3O3S分子量： 415.6描述应用储存/保存方法形态别名可溶性/溶解性PubChem CID

    产品描述
    描述
    GGTI-287 is a highly potent and selective peptidomimetic inhibitor of GGTase I in vitro.
    应用
    A potent, selective, peptidomimetic inhibitor of GGTase I
    储存/保存方法
    Store at -20° C
    形态
    Solid
    基本信息
    别名
    N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine
    可溶性/溶解性
    Soluble in DMSO
    PubChem CID
    16760465

    UBP 296

    发表于由

    UBP 296CAS号： 745055-86-1分子式： C15H15N3O6分子量： 333.30描述应用储存/保存方法形态可溶性/溶解性PubChem CID

    产品描述
    描述
    UBP 296 is a potent and selective GluR5-subunit containing kainate receptor antagonist (apparent KD = 1.09 mM). It displays ~ 90-fold selectivity over both AMPA receptors and recombinant human GluR6- and KA2-containing kainate receptors and shows little to no action at NMDA or group I mGlu receptors. UBP 296 selectively blocks kainate receptor-mediated LTP induction in rat hippocampal mossy fibers.
    应用
    A selective GluR5-subunit containing kainate receptor antagonist
    储存/保存方法
    Store at room temperature
    形态
    Solid
    基本信息
    可溶性/溶解性
    Soluble to 10 mM in 1eq. NaOH and to 10 mM in DMSO
    PubChem CID
    11674376