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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T63211 AKT-IN-10

AKT-IN-10 是有效的 AKT 抑制剂,对乳腺癌和前列腺癌表现出研究潜力。其中蛋白激酶 B (PKB,也称为 AKT) 是细胞中 PI3K/AKT/mTOR 信号传导的核心,其功能对细胞生长、存活、分化和代谢很重要。
T4496 LM22B-10

LM22B10

ERK; Trk receptor; Akt Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
LM22B-10 是TrkB/TrkC 神经营养因子受体激活剂,诱导体内外TrkB、TrkC、AKT 和ERK 的活化。
T4444 A-674563 HCl (552325-73-2(free base))

ERK; Akt; PKA; CDK; PKC Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
A-674563 HCl (552325-73-2(free base)) 是一种口服的、ATP 竞争性的、可逆的 Akt 抑制剂(Akt1 的 Ki:11 nM)。它对 PKA 和 Cdk2 具有抑制活性(IC50:16/46 nM),但对 Akt1 的选择性比 CMGC、CAMK 和 TK 家族中的其他激酶高 10 至 >1800 倍。
T21493 Cyclosporin H

Others Others
Cyclosporin H 是一种 FPR-1(甲酰肽受体 1) 的选择性强效抑制剂。它缺乏 Cyclosporin A 具有的免疫抑制活性。它是一种病毒转导增强剂,可使人脐带血来源的造血干细胞和祖细胞中慢病毒转导增强 10 倍。它与雷帕霉素或前列腺素 E2 联合使用时表现出累加效应。
T10804 CHMFL-PI3KD-317

PI3K; PI4K PI3K/Akt/mTOR signaling
CHMFL-PI3KD-317 是一种高效、选择性、可口服的 PI3Kδ 抑制剂,IC50 值为 6 nM,对其选择性是对其他 PIKK 家族的 10-1500 倍,例如 PI3Kα (IC50,62.6 nM),PI3Kβ (IC50,284 nM),PI3Kγ (IC50,202.7 nM),PIK3C2A (IC50,>10000 nM),PIK3C2B (IC50,882.3 nM),VPS34 (IC50,1801.7 nM),PI4KIIIA (IC50,574.1 nM) 和 PI4KIIIB (IC50,300.2 nM)。在 Raji 细胞中,CHMFL-PI3KD-317 抑制 PI3Kδ 介导的 Akt T308 磷酸化,EC50 值为 4.3 nM。CHMFL-PI3KD-317 对癌细胞具有抗增殖作用。
T62013 PI3Kδ-IN-10

PI3Kδ-IN-10 是高效的、具有口服活性的PI3Kδ抑制剂(IC50= 2 nM)。在肝细胞癌模型中,PI3Kδ-IN-10 强烈抑制下游AKT 通路,并诱导细胞凋亡(apoptosis)。
T69589 PX-316

PX-316 is a AKT inhibior. PX-316, when administered intraperitoneally to mice at 150 mg/kg, inhibits Akt activation in HT-29 human tumor xenografts up to 78% at 10 h with recovery to 34% at 48 h. PX-316 has antitumor activity against early human MCF-7 breast cancer and HT-29 colon cancer xenografts in mice. PX-316 formulated in 20% hydroxypropyl-beta-cyclodextrin for intravenous administration is well tolerated in mice and rats with no hemolysis and no hematological toxicity. Thus, PX-316 is the...
T64219 PI3K/mTOR Inhibitor-6

PI3K/mTOR Inhibitor-6 (Compound 19c) 是一种有效的 PI3K/mTOR 双重抑制剂,在人工胃液中的稳定性比 gedatolisib 更高。10 μM 的 PI3K/mTOR Inhibitor-6 能够明显抑制 PI3K/Akt/mTOR 信号通路。PI3K/mTOR Inhibitor-6 对癌症疾病表现出研究潜力。
T64041 PI3K/mTOR Inhibitor-7

PI3K/mTOR Inhibitor-7 是有效的 PI3K/mTOR 双重抑制剂。PI3K/mTOR Inhibitor-7 的作用比 gedatolisib 高 4.7 倍,他们的 IC50 值分别为 1.4 μM 和 0.3 μM。10 μM 的 PI3K/mTOR Inhibitor-7 能够明显抑制 PI3K/Akt/mTOR 信号通路。PI3K/mTOR Inhibitor-7 对癌症疾病表现出研究潜力。
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...
T79449 Antileishmanial agent-19

Parasite Microbiology/Virology
Antileishmanial agent-19 (Compound F27)是一种有效的抗利什曼病试剂,其对L. donovani promastigotes的IC50值为3.39 μM。该化合物能够抑制L. donovani promastigotes中的脯氨酰-tRNA合成酶,并干预宿主PI3K/Akt/CREB轴,从而抑制IL-10的分泌。此外,Antileishmanial agent-19能诱导L. donovani promastigotes自噬介导的细胞凋亡(apoptosis)过程,并在感染的动物体内显著减少寄生虫负担。
T37561 BX-320

BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50= 30 nM).1It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 μM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 μM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 μM). BX-3...
T35897 ASK120067

ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT...
T35527 PI3Kα-IN-4

PI3Kα-IN-4

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t...
T35874 CC260

CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1]. In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosph...

化合物

AKT-IN-10
Cat.No: T63211
Synonym:
Target:
LM22B-10
Cat.No: T4496
Synonym: LM22B10
Target: ERK, Trk receptor, Akt
A-674563 HCl (552325-73-2(free base))
Cat.No: T4444
Synonym:
Target: ERK, Akt, PKA, CDK, PKC
Cyclosporin H
Cat.No: T21493
Synonym:
Target: Others
CHMFL-PI3KD-317
Cat.No: T10804
Synonym:
Target: PI3K, PI4K
PI3Kδ-IN-10
Cat.No: T62013
Synonym:
Target:
PX-316
Cat.No: T69589
Synonym:
Target:
PI3K/mTOR Inhibitor-6
Cat.No: T64219
Synonym:
Target:
PI3K/mTOR Inhibitor-7
Cat.No: T64041
Synonym:
Target:
AAA
Cat.No: T35855
Synonym:
Target:
Antileishmanial agent-19
Cat.No: T79449
Synonym:
Target: Parasite
BX-320
Cat.No: T37561
Synonym:
Target:
ASK120067
Cat.No: T35897
Synonym:
Target:
PI3Kα-IN-4
Cat.No: T35527
Synonym: PI3Kα-IN-4
Target:
CC260
Cat.No: T35874
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T2163 Dihydrocapsaicin

CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide

Others; TRP/TRPV Channel Membrane transporter/Ion channel; Others
Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素,是TRPV1的选择性激动剂,同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。

天然产物

Dihydrocapsaicin
Cat.No: T2163
Synonym: CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide
Target: Others, TRP/TRPV Channel
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