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Cat. No. | Product Name | Target | Signaling Pathways |
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T9205 |
NCGC00378430
|
Phosphatase; Others | Metabolism; Others |
NCGC00378430 是一种 SIX1/EYA2 相互作用抑制剂。它部分逆转 SIX1 过表达介导的转录和代谢谱,并逆转 SIX1 诱导的 TGF-β 信号传导和上皮-间质转化。在小鼠模型中,它能够抑制 SIX1 介导的乳腺癌转移。 | |||
T4459 |
PK11000
|
DNA Alkylator/Crosslinker | DNA Damage/DNA Repair |
PK11000 是一种烷化剂,可通过共价半胱氨酸修饰来稳定野生型和突变型p53的 DNA 结合结构域。 | |||
T8334 |
CADD522
MFCD00167693,3-{[(3,4-二氯苯基)氨基]羰基}二环[2.2.1]庚-5-烯-2-羧酸 |
Others | Others |
CADD522 (MFCD00167693) 是 runt 相关转录因子-2 (RUNX2)-DNA 结合的抑制剂(IC50:10 nM),具有抗肿瘤作用。 | |||
T5858 |
Sertindole
Lu 23-174,舍吲哚 |
Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; Autophagy | Autophagy; GPCR/G Protein; Neuroscience |
Sertindole (Lu 23-174) 是一种非典型抗精神病药,可与多巴胺 D2 受体和血清素受体亚型 5-HT1D、5-HT2A 和 5-HT2C 结合,Kd 值分别为 2.7、20、0.14 和 6 nM。 | |||
T41233 |
Cis-22a
|
Calcium Channel; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
Cis-22a 是一种TRPV6抑制剂(IC50 = 0.32 μM),对相关TRPV 通道和钙通道具有选择性。cis-22a 对T47D 人乳腺癌细胞有抗增殖作用。 | |||
T7311 |
Oxyphenisatin acetate
|
Autophagy | Autophagy |
Oxyphenisatin acetate 是oxyphenisatin 的前体药物,可抑制乳腺癌细胞系 MCF7、T47D、HS578T 和 MDA-MB-468 的生长。 | |||
T63744 | Autophagy inducer 4 | ||
Autophagy inducer 4 是基于 Magnolol 的曼尼希碱衍生物,能够用作抗癌剂。Autophagy inducer 4 能够诱导自噬 (autophagy) 进而抑制癌细胞。Autophagy inducer 4 对 T47D 细胞的毒性是 Magnolol 的 76 倍。Autophagy inducer 4 也能够抑制 T47D 和 Hela 癌细胞的迁移。 | |||
T13685 |
ERD-308
|
Others | Others |
ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).ERD-308 is a highly potent PROTAC degrade | |||
T79383 |
ER degrader 7
|
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ER degrader 7 (Compound 35t) 是一种既能降解ERα又能降解ERβ的化合物。该化合物具有抑制微管蛋白聚合的功能,并能有效降低多种细胞系(包括MCF-7、T47D、MCF-10A、LCC2、T47D D538G与T47D Y537S)的细胞活性,相应IC50s值分别为0.06、2.56、15.84、1.59、1.67、1.37 μM。此外,ER degrader 7 对乳腺癌肿瘤生长同样有抑制作用。 | |||
T36427 |
PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt)
|
PACAP | GPCR/G Protein |
Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, ... | |||
T36195 |
CAY10744
|
||
CAY10744 is a topoisomerase II-α poison.1 It inhibits topoisomerase II-α by 78.9% when used at a concentration of 20 μM. CAY10744 is selective for topoisomerase II-α over topoisomerase I providing 100 and 0% inhibition, respectively, at 100 μM. It inhibits proliferation of HCT15 colon, T47D breast, DU145 prostate, and HeLa cervical cancer cells (IC50s = 0.014, 0.00267, 0.072, and 2.46 μM, respectively). CAY10744 induces apoptosis in T47D cells when used at concentrations of 10 and 30 μM. CAY1074... | |||
T79397 |
Neutrophil elastase inhibitor 4
|
||
Neutrophilelastase inhibitor4 (compound 4f) 是竞争性抑制HNE的化合物,具有较低的半抑制浓度(IC50: 42.30 nM)和解离常数(Ki: 8.04 nM)。此外,该化合物能够诱导T47D细胞的apoptosis,并在多种细胞系中展现出抗增殖作用,分别在T47D、RPMI 8226、A549、HSF细胞系的IC50值为21.25、34.17、29.93、99.11 nM。 | |||
T36462 |
CAY10770
CAY10770 |
||
CAY10770 is an inhibitor of the cytochrome P450 (CYP) isoform CYP4Z1 (IC50= 5.9 μM).1It is selective for CYP4Z1 over CYP4A11, CYP4F2, CYP4F3a, CYP4F3b (IC50s = 187-282 μM) but does inhibit CYP4F8 and CYP4F12 (IC50s = 167 and 91 μM, respectively). CAY10770 (3 μM) inhibits the production of 14(15)-EET, 19-HETE, and 14(15)-DiHET by 83, 86, and 80%, respectively, in T47D breast cancer cells expressing CYP4Z1. 1.Kowalski, J.P., McDonald, M.G., Pelletier, R.D., et al.Design and characterization of the... | |||
T36539 |
Nocardamine
|
||
Nocardamine is a ferrioxamine siderophore that has been found inStreptomycesand has diverse biological activities.1,2,3,4It chelates iron in a chrome azurol S assay (IC50= 9.9 μM).1Nocardamine inhibitsM. smegmatisandM. bovisbiofilm formation (MIC = 10 μM for both), an effect that can be reversed by iron.2It is cytotoxic to T47D, SK-MEL-5, SK-MEL-28, and RPMI-7951 cancer cells (IC50s = 6, 18, 12, and 14 μM, respectively).3Nocardamine also induces morphological changes in BM-N4 insect cells.4 1.Lo... | |||
T35676 |
17β-hydroxy Exemestane
|
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17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = ... | |||
T36308 |
PF-06843195
|
||
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy[1]. PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively[1].PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells w... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5755 |
Aloesin
|
Tyrosinase | Proteases/Proteasome |
Aloesin 是芦荟的活性成分之一,能够通过 MAPK 信号通路发挥抗癌作用,并具有抗炎、紫外线保护和抗菌作用。 | |||
T36857 |
Estrone sulfate sodium
雌酮3-硫酸钠,Estrone 3-sulfate (sodium salt),17β-Estrone 3-sulfate |
Endogenous Metabolite | Metabolism |
Estrone sulfate sodium (17β-Estrone 3-sulfate) 是一种主要的循环血浆雌激素,无生物活性,通过类固醇硫酸酯酶(STS) 转化为生物活性雌激素雌酮。 | |||
T10390 |
Asperphenamate
|
Others; Antifungal | Microbiology/Virology; Others |
Asperphenamate 是 Aspergillus flatiipes 的真菌代谢产物。 T47D 细胞、MDA-MB-231 细胞和 HL-60 细胞的 IC50 分别为 92.3 μM、96.5 μM 和 97.9 μM。 Asperphenamate 具有抗癌作用。 | |||
TN5164 |
trans-Hinokiresinol
|
IL Receptor; TNF; NOS; LTR | Apoptosis; Immunology/Inflammation |
Hinokiresinol is a novel inhibitor of LTB4 binding to the human neutrophils, it has antiallergic effect, it inhibits IgE-induced mouse passive cutaneous anaphylaxis reaction. Hinokiresinol (trans-hinokiresinol) and nyasol (cis-hinokiresinol) are estrogen |