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34

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T22422 S6K-18

S6 Kinase MAPK; PI3K/Akt/mTOR signaling
S6K-18 是一种高度选择性的 S6K1 抑制剂,抑制 S6K1,IC50 为 52nM。
T6877 LJH685

Apoptosis; S6 Kinase Apoptosis; MAPK; PI3K/Akt/mTOR signaling
LJH685 是一种选择性,ATP-竞争性的RSK 抑制剂, 抑制 RSK1/2/3 生物活性,IC50为 6、5、4 nM。
T5428 BIX 02565

LRRK2; S6 Kinase Autophagy; MAPK; PI3K/Akt/mTOR signaling
BIX 02565 是核糖体 S6 激酶 2 (RSK2) 抑制剂,IC50为 1.1 nM。
T2002 PF-4708671

PF4708671

S6 Kinase; Autophagy Autophagy; MAPK; PI3K/Akt/mTOR signaling
PF-4708671 是一种可渗透细胞的 p70 核糖体 S6 激酶抑制剂,对 S6K1的Ki 为 20 nM,IC50为 160 nM。
T4301 AD80

Raf; c-RET; Src; S6 Kinase Angiogenesis; Apoptosis; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
AD80 是多激酶抑制剂,可抑制 RET、RAF、SRC 和 S6K,并大大降低 mTOR 活性。
T16670 PS210

PDK PI3K/Akt/mTOR signaling
PS210 是针对 PDK1的 PIF 结合口袋的、选择性的、有效的 PDK1激活剂,对其他蛋白激酶无活性。在细胞中,它的前药 PS423 可作为 PDK1的底物选择性抑制剂,抑制 S6K 的磷酸化和活化。
T6878 LJI308

S6 Kinase MAPK; PI3K/Akt/mTOR signaling
LJI308 是泛RSK 抑制剂,对 RSK1、RSK2 和 RSK3 的IC50分别为 6、4 和 13 nM。它抑制辐照、EGF 处理和表达 KRAS 突变的细胞中 RSK (T359/S363) 和 YB-1 (S102) 的磷酸化。
T6171 BI-D1870

S6 Kinase; Autophagy Autophagy; MAPK; PI3K/Akt/mTOR signaling
BI-D1870 是一种可渗透细胞和透过血脑屏障的的 ATP 竞争性核糖体 S6 激酶抑制剂,抑制 RSK1、RSK2、RSK3和 RSK4 的 IC50值分别为 31 nM、24 nM、18 nM 和15 nM。
T6948 Pluripotin

SC1

ERK; Raf; S6 Kinase MAPK; PI3K/Akt/mTOR signaling
Pluripotin (SC1) 是ERK1和RasGAP 的双重抑制剂,KD 分别为 98 和 212 nM。它还抑制RSK1、RSK2、RSK3和RSK4,IC50分别为 0.5、2.5、3.3 和 10.0 μM。
T6304 AT7867

Akt; PKA; S6 Kinase Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
AT7867 是 ATP 竞争性的Akt1/Akt2/Akt3和p70S6K/PKA 抑制剂,IC50分别为 32、17、47 和 85、20 nM。
T14779 BRD7389

SGK; FLT; Pim; CDK; S6 Kinase; DAPK Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
BRD7389 是一种 RSK 家族激酶抑制剂,对 RSK1、RSK2 和 RSK3 的 IC50 分别为 1.5 μM、2.4 μM 和 1.2 μM。
T6159 LY-2584702 free base

S6 Kinase; mTOR MAPK; PI3K/Akt/mTOR signaling
LY-2584702 free base 是一种选择性的 ATP 竞争性 p70S6K 抑制剂,IC50为 4 nM,对S6K1的IC50为 2 nM,用于研究癌症治疗的试验。
T7790 Bisindolylmaleimide V

双吲哚马来酰亚胺 V,双吲哚马来酰亚胺

PKC; S6 Kinase Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling
Bisindolylmaleimide V 是一种弱蛋白激酶 C (PKC) 抑制剂( IC50 >100 µM)。
T1746 LY-2584702 tosylate salt

LY2584702 tosylate

S6 Kinase MAPK; PI3K/Akt/mTOR signaling
LY-2584702 tosylate salt 是一种选择性的 ATP 竞争性 p70S6K 抑制剂,IC50为 4 nM,对S6K1的IC50为 2 nM,用于研究癌症治疗的试验。
T4488 GSK-25

GSK25

ROCK; S6 Kinase; mTOR Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
GSK-25 是一种选择性的,具有口服活性的 ROCK1抑制剂。它对 31 种激酶以及 RSK1 和 p70S6K 保持良好的选择性,RSK1的 IC50 为 398 nM,p70S6K 的 IC50 为 1000nM。它可抑制 P450,对 CYP2C9、CYP2D6和 CYP3A4的 IC50分别为2.5、5.2和2.5 μM。
T2482 AT13148

ROCK; SGK; Akt; PKA; S6 Kinase Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
AT13148 是一种 ATP 竞争性 AGC 激酶口服抑制剂,能够抑制 Akt1/Akt2/Akt3、p70S6K、PKA 和 ROCKI/ROCKII 的活性,IC50值分别为 38/402/50、8、3 和 6 nM/4 nM。
T8978 DD1

3,3'-Diamino-4'-methoxyflavone,HUN85111

Proteasome Proteases/Proteasome; Ubiquitination
DD1 (HUN85111) 是一种蛋白酶体抑制剂,可诱导人髓系肿瘤选择性凋亡。
T19913 CKI-7

CKI 7 2HCl,CKI-7 dihydrochloride,N-(2-氨基乙基)-5-氯异喹啉-8-磺酰胺二盐酸盐,CKI7 2HCl,CKI 7 dihydrochloride,CKI7 dihydrochloride,CKI-7 2HCl

ROCK; SGK; Casein Kinase; CDK; S6 Kinase Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells
CKI-7 是一种有效且 ATP 竞争性的酪蛋白激酶 1 抑制剂,IC50为 6 μM,Ki 为 8.5 μM。它选择性抑制 Cdc7激酶,还抑制 SGK,S6K1以及 MSK1。
T28652 S6K1-IN-DG2

S6K1 Inhibitor DG2,S6K1-Inhibitor-DG2,S6K1 IN DG2,S6K1INDG2,S6K1InhibitorDG2

mTOR PI3K/Akt/mTOR signaling
S6K1-IN-DG2(S6K1InhibitorDG2) 是一种有效的 p70S6K 抑制剂 ,IC50 值小于 100 nM。
T79871 S6K2-IN-1

FGFR Angiogenesis; Tyrosine Kinase/Adaptors
S6K2-IN-1(化合物2)为S6K2抑制剂(IC50:22 nM),并对FGFR4亦有抑制作用(IC50:216 nM)。该化合物在小鼠肝微粒体中展现出良好的稳定性。
T6730 WAY-600

6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶,WAY600

VEGFR; PI3K; Src; mTOR Angiogenesis; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
WAY-600 是一种有效的,选择性的,ATP 竞争型的mTOR 抑制剂,抑制重组 mTOR 酶,其 IC50=9 nM。它能够阻断 mTOR 复合物 1/2 (mTORC1/2) 组装和激活。
T6731 WYE-354

4-[6-[4-[(甲氧羰基)氨基]苯基]-4-(4-吗啉基)-1H-吡唑并[3,4-D]嘧啶-1-基]-1-哌啶羧酸甲酯

Apoptosis; PI3K; mTOR; Autophagy Apoptosis; Autophagy; PI3K/Akt/mTOR signaling
WYE-354 是一种 ATP 竞争性的mTOR 抑制剂,IC50为 5 nM。它抑制PI3Kα和PI3Kγ,IC50分别为 1.89 μM 和 7.37 μM,也抑制mTORC1和mTORC2。它在体外能诱导自噬激活。
T23897 CLK1/2-IN-3

CLK1/2 inhibitor 3,CLK1/2-inhibitor-3,CLK1/2 IN 3,CLK1/2IN3

CDK Cell Cycle/Checkpoint
CLK1/2-IN-3(Cpd-3) 是一种具有高效性和选择性的 CLK1 和 CLK2 抑制剂,抗增殖活性,抑制 CLK1、CLK2、SRPK1、SRPK2、SRPK3 的 的活性。CLK1/2-IN-3 可诱导核斑点扩大,可诱导S6K pre-mRNA选择性剪接和随后抑制多种癌细胞类型细胞生长。
T81041 TAS0612

Akt Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
TAS0612为口服新型抑制剂,具针对性地抑制RSK、AKT和S6K。此化合物展示了通过阻断细胞生长的机制,在多种肿瘤模型中表现出广泛的活性。
T11928 M2698

MSC2363318A

Akt; mTOR Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
M2698 (MSC2363318A) 是 p70S6K、Akt1 和 Akt3 的抑制剂,IC50 为 1 nM。 M2698 显示出抗癌活性。
T6303L CCT128930 hydrochloride

CCT128930 hydrochloride(885499-61-6 Free base)

Apoptosis; Akt; PKA; mTOR; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
CCT128930 hydrochloride (CCT128930 hydrochloride) 是一种选择性 AKT 抑制剂,具有抗肿瘤活性。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173),对 PKA 激酶具有 28 倍的选择性,对 p70S6K 具有 20 倍的选择性。
T22552 AD57 (hydrochloride)

Others Others
AD57, as polypharmacological cancer therapeutic, is designed to regulate multiple targets related to cancer blocks the receptor tyrosine kinase RET in Drosophila (IC50: 2 nM). AD57 effectively suppresses tyrosine kinase RET, weakens the activity of numero
T1920 Capivasertib

AZD5363

Akt; PKA; mTOR; Autophagy Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
Capivasertib (AZD5363) 是一种广谱的 AKT 抑制剂,对 Akt1、Akt2 和 Akt3 均有抑制活性 (IC50=3/7/7 nM),具有口服活性。Capivasertib 具有抗肿瘤活性,可以用于治疗乳腺癌。
T39733 Hu7691 free base

Hu7691 free base is an orally active, selective Akt inhibitor. It exhibits IC50 values of 4.0 nM, 97.5 nM, and 28 nM for Akt1, Akt2, and Akt3, respectively. Furthermore, it effectively inhibits tumor growth and facilitates a reduction in cutaneous toxicity in mice.
T11900 LY-2584702 hydrochloride

S6 Kinase MAPK; PI3K/Akt/mTOR signaling
Ly-2584702 hydrochloride is a p70S6K selective ATP competitive inhibitor with IC50 of 4 nM.In the S6K1 enzyme assay, the IC50 of LY-2584702 was 2 nM.
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...
T10275 AKT-IN-3

Akt Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1
T10274 AKT-IN-2

Akt Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
AKT-IN-2 is a selective, and orally bioavailable AKT inhibitor (IC50: 5 nM for AKT1).
T39899 Hu7691

Akt Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
Hu7691 是一种具有口服活性、选择性和高效性的 Akt 抑制剂,抑制 Akt1、Akt2 和 Akt3,抑制神经母细胞瘤细胞增殖,诱导神经母细胞瘤细胞的分化。

化合物

S6K-18
Cat.No: T22422
Synonym:
Target: S6 Kinase
LJH685
Cat.No: T6877
Synonym:
Target: Apoptosis, S6 Kinase
BIX 02565
Cat.No: T5428
Synonym:
Target: LRRK2, S6 Kinase
PF-4708671
Cat.No: T2002
Synonym: PF4708671
Target: S6 Kinase, Autophagy
AD80
Cat.No: T4301
Synonym:
Target: Raf, c-RET, Src, S6 Kinase
PS210
Cat.No: T16670
Synonym:
Target: PDK
LJI308
Cat.No: T6878
Synonym:
Target: S6 Kinase
BI-D1870
Cat.No: T6171
Synonym:
Target: S6 Kinase, Autophagy
Pluripotin
Cat.No: T6948
Synonym: SC1
Target: ERK, Raf, S6 Kinase
AT7867
Cat.No: T6304
Synonym:
Target: Akt, PKA, S6 Kinase
BRD7389
Cat.No: T14779
Synonym:
Target: SGK, FLT, Pim, CDK, S6 Kinase, DAPK
LY-2584702 free base
Cat.No: T6159
Synonym:
Target: S6 Kinase, mTOR
Bisindolylmaleimide V
Cat.No: T7790
Synonym: 双吲哚马来酰亚胺 V,双吲哚马来酰亚胺
Target: PKC, S6 Kinase
LY-2584702 tosylate salt
Cat.No: T1746
Synonym: LY2584702 tosylate
Target: S6 Kinase
GSK-25
Cat.No: T4488
Synonym: GSK25
Target: ROCK, S6 Kinase, mTOR
AT13148
Cat.No: T2482
Synonym:
Target: ROCK, SGK, Akt, PKA, S6 Kinase
DD1
Cat.No: T8978
Synonym: 3,3'-Diamino-4'-methoxyflavone,HUN85111
Target: Proteasome
CKI-7
Cat.No: T19913
Synonym: CKI 7 2HCl,CKI-7 dihydrochloride,N-(2-氨基乙基)-5-氯异喹啉-8-磺酰胺二盐酸盐,CKI7 2HCl,CKI 7 dihydrochloride,CKI7 dihydrochloride,CKI-7 2HCl
Target: ROCK, SGK, Casein Kinase, CDK, S6 Kinase
S6K1-IN-DG2
Cat.No: T28652
Synonym: S6K1 Inhibitor DG2,S6K1-Inhibitor-DG2,S6K1 IN DG2,S6K1INDG2,S6K1InhibitorDG2
Target: mTOR
S6K2-IN-1
Cat.No: T79871
Synonym:
Target: FGFR
WAY-600
Cat.No: T6730
Synonym: 6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶,WAY600
Target: VEGFR, PI3K, Src, mTOR
WYE-354
Cat.No: T6731
Synonym: 4-[6-[4-[(甲氧羰基)氨基]苯基]-4-(4-吗啉基)-1H-吡唑并[3,4-D]嘧啶-1-基]-1-哌啶羧酸甲酯
Target: Apoptosis, PI3K, mTOR, Autophagy
CLK1/2-IN-3
Cat.No: T23897
Synonym: CLK1/2 inhibitor 3,CLK1/2-inhibitor-3,CLK1/2 IN 3,CLK1/2IN3
Target: CDK
TAS0612
Cat.No: T81041
Synonym:
Target: Akt
M2698
Cat.No: T11928
Synonym: MSC2363318A
Target: Akt, mTOR
CCT128930 hydrochloride
Cat.No: T6303L
Synonym: CCT128930 hydrochloride(885499-61-6 Free base)
Target: Apoptosis, Akt, PKA, mTOR, Autophagy
AD57 (hydrochloride)
Cat.No: T22552
Synonym:
Target: Others
Capivasertib
Cat.No: T1920
Synonym: AZD5363
Target: Akt, PKA, mTOR, Autophagy
Hu7691 free base
Cat.No: T39733
Synonym:
Target:
LY-2584702 hydrochloride
Cat.No: T11900
Synonym:
Target: S6 Kinase
CC260
Cat.No: T35874
Synonym:
Target:
AKT-IN-3
Cat.No: T10275
Synonym:
Target: Akt
AKT-IN-2
Cat.No: T10274
Synonym:
Target: Akt
Hu7691
Cat.No: T39899
Synonym:
Target: Akt
Cat. No. Product Name Target Signaling Pathways
T3836 Eudesmin

MAPK; S6 Kinase MAPK; PI3K/Akt/mTOR signaling
Eudesmin 通过抑制S6K1信号通路来干扰成脂分化,具有抗肿瘤、抗炎和抗菌活性。
T6S1302 Carnosol

Nrf2; Endogenous Metabolite; S6 Kinase Immunology/Inflammation; MAPK; Metabolism; PI3K/Akt/mTOR signaling
Carnosol 是 Nrf2激活剂,增加 Nrf2 的水平以及能促进血红素氧合酶 1(HMOX1) 表达。它是核糖体 S6激酶(RSK2)抑制剂,可用于胃癌相关研究,IC50值约为 5.5 μM。
T2871 Quercitrin

Sophoretin,3-rhamnosyl quercetin,Quercetin 3-rhamnoside,Xanthaurine,槲皮苷,Meletin

Reactive Oxygen Species; S6 Kinase; Autophagy Autophagy; Immunology/Inflammation; MAPK; Metabolism; NF-κB; PI3K/Akt/mTOR signaling
Quercitrin (3-rhamnosyl quercetin) 是苦荞麦中的一种天然产物,具有抗炎作用,有用于心血管疾病的研究潜力。
T0335 Sodium salicylate

水杨酸钠,Salicylic acid sodium salt,2-Hydroxybenzoic acid sodium salt

Apoptosis; NF-κB; COX; S6 Kinase; Autophagy Apoptosis; Autophagy; Immunology/Inflammation; MAPK; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling
Sodium salicylate (2-Hydroxybenzoic acid sodium salt) 是一种S6K 的抑制剂,可抑制COX-2活性。它还是一种NF-κB 抑制剂,可降低炎症基因的表达,促进老化肌肉的修复。

天然产物

Eudesmin
Cat.No: T3836
Synonym:
Target: MAPK, S6 Kinase
Carnosol
Cat.No: T6S1302
Synonym:
Target: Nrf2, Endogenous Metabolite, S6 Kinase
Quercitrin
Cat.No: T2871
Synonym: Sophoretin,3-rhamnosyl quercetin,Quercetin 3-rhamnoside,Xanthaurine,槲皮苷,Meletin
Target: Reactive Oxygen Species, S6 Kinase, Autophagy
Sodium salicylate
Cat.No: T0335
Synonym: 水杨酸钠,Salicylic acid sodium salt,2-Hydroxybenzoic acid sodium salt
Target: Apoptosis, NF-κB, COX, S6 Kinase, Autophagy
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