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11

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9831 MKC-1

Ro-31-7453

Apoptosis; Akt; Microtubule Associated; mTOR Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
MKC-1 (Ro-31-7453) 是一种口服生物可利用的小分子双吲哚基马来酰亚胺细胞周期抑制剂,具有潜在的抗肿瘤活性。
T2145 Temsirolimus

NSC 683864,CCI-779,西罗莫司脂化物

Apoptosis; mTOR; Autophagy Apoptosis; Autophagy; PI3K/Akt/mTOR signaling
Temsirolimus (CCI-779) 是一种mTOR 抑制剂,IC50值为 1.76 μM。它能激活自噬,可防止心脏功能恶化。
T76828 Sonepcizumab

LT 1009

LPL Receptor GPCR/G Protein
Sonepcizumab (LT 1009) 是一种完全人源化的抗 S1P 单克隆抗体。Sonepcizumab 具有抗癌活性,可用于研究转移性肾细胞癌 (mRCC) ,可预防青光眼滤过手术后的眼部瘢痕形成。
T1916 Apitolisib

RG 7422,GNE 390,GDC-0980

Apoptosis; PI3K; mTOR Apoptosis; PI3K/Akt/mTOR signaling
Apitolisib (RG 7422) 是一种口服有效的 PI3K 和 mTOR(TORC1/2) 激酶抑制剂,抑制 PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ的活性,IC50值为 5 nM/27 nM/7 nM/14 nM,抑制 mTOR,Ki 为 17 nM。它用于乳腺癌、前列腺癌、肾细胞癌和子宫内膜癌等实体癌的试验研究 。
T69877 SPOP-IN-6lc

Apoptosis Apoptosis
SPOP-IN-6lc 是一种有效的 SPOP 抑制剂,在癌症中有多种作用,在多种肿瘤中有抑癌作用,在肾癌中却发挥着癌基因功能。SPOP-IN-6lc 可用于研究细胞信号传送和细胞凋亡。
T31058 CP-461 free base

CEL031,CP461,UNII-824ZMS3BGL,CP-461,OSI-461

CP-461 (OSI-461) is a pde2a / 5A inhibitor, which may be used in the treatment of renal cell carcinoma, prostate cancer, and Crohn's disease.
T60802 Tubulin polymerization-IN-2

Tubulin polymerization-IN-2 为针对β-微管蛋白的强效抗癌分子,IC50 值为0.92 μM。该分子在多种细胞系中,包括白血病、非小细胞肺癌、肾癌、前列腺癌及乳腺癌细胞中展现出显著的抑制效果。
T70928 CB-1158-analog

CB-1158-analog, also known as Numidargistat-analog and INCB01158-analog, is a potent and orally active arginase inhibitor with IC50=89 nM) . CB-1158 blocked myeloid cell-mediated suppression of T cell proliferation in vitro and reduced tumor growth in multiple mouse models of cancer, as a single agent and in combination with checkpoint blockade, adoptive T cell therapy, adoptive NK cell therapy, and the chemotherapy agent gemcitabine. CB-1158 increased tumor-infiltrating CD8+ T cells and NK cell...
T76723 Tilvestamab

Tilvestamab (BGB149) 是一种人源化抗AXL 抗体,阻断AXL 介导的细胞信号传导。Tilvestamab 在体外能显著抑制Gas6刺激诱导的AXL 激活,并抑制 786-0-Luc RCC 细胞中下游AXL 的磷酸化。Tilvestamab 可用于癌症,尤其是AXL 过度表达肾细胞癌的研究。
T35855 AAA

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension...
T36673 CC 401 dihydrochloride

High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 |Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J...

化合物

MKC-1
Cat.No: T9831
Synonym: Ro-31-7453
Target: Apoptosis, Akt, Microtubule Associated, mTOR
Temsirolimus
Cat.No: T2145
Synonym: NSC 683864,CCI-779,西罗莫司脂化物
Target: Apoptosis, mTOR, Autophagy
Sonepcizumab
Cat.No: T76828
Synonym: LT 1009
Target: LPL Receptor
Apitolisib
Cat.No: T1916
Synonym: RG 7422,GNE 390,GDC-0980
Target: Apoptosis, PI3K, mTOR
SPOP-IN-6lc
Cat.No: T69877
Synonym:
Target: Apoptosis
CP-461 free base
Cat.No: T31058
Synonym: CEL031,CP461,UNII-824ZMS3BGL,CP-461,OSI-461
Target:
Tubulin polymerization-IN-2
Cat.No: T60802
Synonym:
Target:
CB-1158-analog
Cat.No: T70928
Synonym:
Target:
Tilvestamab
Cat.No: T76723
Synonym:
Target:
AAA
Cat.No: T35855
Synonym:
Target:
CC 401 dihydrochloride
Cat.No: T36673
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2S2043 Dracorhodin perchlorate

Dracorhodin perochlorate,血竭素高氯酸盐,Dracohodin perochlorate

Apoptosis; Others Apoptosis; Others
Dracorhodin perchlorate 是来源于中药血竭的一种天然产物。它抑制细胞生长,并以剂量和时间依赖性方式诱导成纤维细胞凋亡,将细胞周期阻滞在 G1 期,可作为抗乳腺癌的候选药物。
TMA1743 Ergosterol peroxide

ERK; VEGFR; p38 MAPK; Wnt/beta-catenin; Akt; JAK; CDK; JNK; STAT; Antifection Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Foxo3a activity by inhibiting pAKT and c-Myc and activating pro-apoptotic protein Puma and Bax to

天然产物

Dracorhodin perchlorate
Cat.No: T2S2043
Synonym: Dracorhodin perochlorate,血竭素高氯酸盐,Dracohodin perochlorate
Target: Apoptosis, Others
Ergosterol peroxide
Cat.No: TMA1743
Synonym:
Target: ERK, VEGFR, p38 MAPK, Wnt/beta-catenin, Akt, JAK, CDK, JNK, STAT, Antifection
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