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34

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T2253 TCS PIM-1 1

3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮,SC 204330

Pim Chromatin/Epigenetic; JAK/STAT signaling
TCS PIM-1 1 (SC 204330) 是一种特异性有效的 ATP 竞争性 Pim-1 激酶抑制剂,IC50为 50 nM,对 MEK1/MEK2 和 Pim-2 表现出良好的特异性,IC50值大于 20000 nM。
T9229 Pim-1/2 kinase inhibitor 1

Pim Chromatin/Epigenetic; JAK/STAT signaling
Pim-1/2 kinase inhibitor 1 是一种具有口服活性的 Pim-1/2 激酶抑制剂。Pim-1/2 kinase inhibitor 1 能阻断 Pim 激酶磷酸化肽的能力,并且抑制4E-BP1和p27Kip1Pim 蛋白激酶定向磷酸化。Pim-1/2 kinase inhibitor 1 可用于癌症,尤其是前列腺癌的研究。
T4215 TCS-PIM-1-4a

5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮,SMI-4a

Apoptosis; Pim Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling
TCS-PIM-1-4a (SMI-4a) 是一种泛-Pim 激酶抑制剂,可通过激活 AMPK 来阻断 mTORC1的活性。它可杀死多种髓样和淋巴样细胞系,IC50值为 0.8 μM 至 40 μM。
T3058 (Z)-SMI-4a

TCS PIM-1 4a,SMI-4a

Pim Chromatin/Epigenetic; JAK/STAT signaling
(Z)-SMI-4a (TCS PIM-1 4a) 是一种选择性的,细胞可渗透的且具有 ATP 竞争性的 Pim-1抑制剂,IC50为 24 μM,Ki 为 0.6 μM。它还抑制 Pim-2,IC50为 100 μM,具有抗癌活性。
T40319 PIM-IN-1

PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC 50 = 61 nM; pS6, EC 50 = 71 nM).
T23158 PIM-1 Inhibitor 2

Others Others
PIM-1 Inhibitor 2 is an effective Pim-1 kinase inhibitor (Ki = 91 nM).
T5093 Pim1/AKK1-IN-1

LKB1/AAK1 dual inhibitor,MDK-2275

Pim; Hippo pathway Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) 是多种酶抑制剂,能够作用于Pim1、AKK1、MST2 和 LKB1,Kd 值分别为 35、53、75 和 380 nM,还抑制 MPSK1 和 TNIK。
T40092 MNK/PIM-IN-1

MNK/PIM-IN-1 is a novel dual inhibitor targeting both MNK and PIM pathways, characterized by its favorable pharmacokinetic profile.
T83627 Pim-1 kinase inhibitor 8

Pim; PKC Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling
Pim-1 kinase inhibitor 8 是一种高效的 Pim-1 kinase 抑制剂,具有抗癌活性,可有效抑制细胞迁移。Pim-1 kinase inhibitor 8 对 MCF-7 和 HepG2 细胞有细胞毒性,是研究乳腺癌的候选化合物。
T77526 Pim-1 kinase inhibitor 4

Apoptosis; Pim Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling
Pim-1 kinase inhibitor 4 是一种高效的 Pim-1 激酶 抑制剂,IC50 值为 17.01 nM。Pim-1 kinase inhibitor 4 还具有抗氧化活性和潜在的抗癌活性,对 DPPH 有抑制作用。Pim-1 kinase inhibitor 4 促进 PC-3 细胞凋亡 (apoptosis),对 PC-3 细胞生长有抑制作用,IC50 为 16 nM。Pim-1 kinase inhibitor 4 可用于研究前列腺癌。
T24166 Inecalcitol

TX 522,TX-522,TX522,伊奈骨化醇

Apoptosis Apoptosis
Inecalcitol (TX 522) 是一种独特的维生素 D3 类似物,可诱导细胞凋亡,有抗癌活性。它是一种具有口服活性维生素 D 受体激动剂,Kd 为 0.53 nM。
T12474 PIM1-IN-1

Pim Chromatin/Epigenetic; JAK/STAT signaling
PIM1-IN-1 is a potent and highly selective inhibitor of PIM1/3(IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively),with Antiproliferative and anti-cancer activity.
T60972 Pim-1 kinase inhibitor 1

Pim-1 kinase inhibitor 1 可用于癌症领域研究, 通过促进细胞凋亡对多种癌细胞系表现出抗癌活性。Pim-1 kinase inhibitor 1 是一种Pim-1 激酶抑制剂 (IC50 = 0.11 μM)。
T61510 PIM-1/HDAC-IN-1

PIM-1/HDAC-IN-1 (compound 4d) is a potent inhibitor of PIM-1, with an IC 50 of 343.87 nM. It also exhibits strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC 50 values of 63.65 and 62.39 nM, respectively. Furthermore, PIM-1/HDAC-IN-1 demonstrates apoptosis-inducing potential in MCF-7 cell lines, specifically inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase [1].
T78980 Pim-1 kinase inhibitor 5

Pim Chromatin/Epigenetic; JAK/STAT signaling
Pim-1 kinase inhibitor 5 (Compound 4c)是一种选择性Pim-1激酶抑制剂,具有0.61 μM的半抑制浓度(IC50)。该化合物对HepG2、MCF-7、PC3和HCT-116癌细胞系表现出细胞毒性,其IC50s值介于6.95至20.19 μM之间。
T61074 Pim-1 kinase inhibitor 3

Pim-1 kinase inhibitor 3 (Compound H5) 是一种有效的Pim-1激酶抑制剂,IC50为 35.13 nM。
T62001 Pim-1 kinase inhibitor 2

Pim-1 kinase inhibitor 2 (Compound 13) 为高效Pim-1激酶抑制剂,能诱导细胞凋亡(apoptosis),显示出在癌症疾病研究中的应用潜力。
T4523 TP-3654

Pim Chromatin/Epigenetic; JAK/STAT signaling
TP3654是一种Pim 激酶抑制剂,对Pim-1Pim-3的Ki 值分别为5和42 nM。
T15830 M-110

Pim Chromatin/Epigenetic; JAK/STAT signaling
M-110 是一种高选择性的,ATP 竞争性的 PIM 激酶抑制剂,M-110 对 PIM-3 抑制作用较好,IC50=47 nM。M-110 抑制 PIM-1PIM-2 的IC50 为 2.5 μM。M-110 抑制前列腺癌细胞的增殖,IC50 为 0.6-0.9 μM。
T3078 SGI-1776

SGI-1776 free base,Pim-Kinase Inhibitor IX

Apoptosis; FLT; Pim; Autophagy Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Tyrosine Kinase/Adaptors
SGI-1776 (Pim-Kinase Inhibitor IX) 是一种Pim 抑制剂,抑制 Pim-1Pim-2 和 Pim-3 的活性,IC50值分别为 7 nM、363 nM 和 69 nM。
T1834 CX-6258

CX 6258

Pim Chromatin/Epigenetic; JAK/STAT signaling
CX-6258是一种强效选择性的泛 Pim 激酶抑制剂,对Pim-1Pim-2 和 Pim-3 作用的IC50值分别为 5、25 和 16 nM。
T6148 CX-6258 hydrochloride

CX-6258 HCl,Pim-Kinase Inhibitor X

Pim Chromatin/Epigenetic; JAK/STAT signaling
CX-6258 hydrochloride (Pim-Kinase Inhibitor X) 是一种强效选择性的泛 Pim 激酶抑制剂,对Pim-1Pim-2 和 Pim-3 作用的IC50值分别为 5、25 和 16 nM。
T27704 K00135

K-00135,Imidazol[1,2-b]pyridazine 1,K 00135,IMIDAZOPYRIDAZIN 1

Pim Chromatin/Epigenetic; JAK/STAT signaling
K00135 (IMIDAZOPYRIDAZIN 1) 是 Pim 激酶的选择性抑制剂,可用于胃癌和抗白血病治疗的研究。
T3989 SMI-16a

PIM1/2 Kinase Inhibitor VI

Pim Chromatin/Epigenetic; JAK/STAT signaling
SMI-16a (PIM1/2 Kinase Inhibitor VI) 是选择性 Pim 激酶抑制剂,对 Pim1Pim2 和 PC3 细胞的 IC50值分别为0.15、0.02 和48 μM。
T63589 CX-6258 hydrochloride hydrate

CX-6258 hydrochloride hydrate 是强效的、选择性的 pan-Pim 激酶抑制剂,能够作用于 Pim-1 (IC50: 5 nM)、 Pim-2 (IC50: 25 nM) 和 Pim-3 (IC50: 16 nM)。
TP2128 R8-T198wt

Cell-permeable peptide inhibitor of Pim-1 kinase, derived from p27Kip1. Inhibits Pim-1 phosphorylation of p27Kip1 and Bad; induces cell cycle arrest (at G1) and apoptosis in DU145 prostate cancer cells. Also inhibits Pim-1-dependent growth of DU145 cells
T71558 Pim-IN-14j

Pim-IN-14j is a potent, highly selective, and orally bioavailable inhibitor of PIM-1 kinases.
T81460 PIM-IN-2

Pim Chromatin/Epigenetic; JAK/STAT signaling
PIM-IN-2是Pim激酶抑制剂,具有25 nM 的半抑制浓度(IC50)。它能增强细胞存活、防止凋亡,并在多种人类肿瘤中高表达。
T68341 HS56

HS56 是一种 ATP 竞争性 Pim/DAPK3双重抑制剂,对 DAPK3、Pim-3、Pim-1Pim-2 的 Ki 值分别为 0.26、0.208、2.94 和 >100 μM。 HS56 抑制 LC20 磷酸化和平滑肌收缩。HS56 降低自发性高血压小鼠的血压。HS56可用于高血压研究。
T63720 PIM1-IN-3

PIM1-IN-3 (Compound HL8) 是一种 PIM1 的有效抑制剂,能够选择性抑制 PIM-1 酶,可有效的诱导 Colo320 细胞凋亡。PIM1-IN-3 对癌症疾病表现出研究潜力。
T62188 PIM1-IN-6

PIM1-IN-6 (compound 5h) 是一种 PIM-1 的有效抑制剂 (IC50: 0.60 μM)。PIM1-IN-6 对 HCT-116 和 MCF-7 细胞具有较高的细胞毒作用,他们的 IC50 值分别为 1.5115.2 μM。
T61700 PIM1-IN-7

PIM1-IN-7 (compound 6c) is a powerful inhibitor of PIM-1, effectively suppressing its activity with an IC50 of 0.67 μM. This compound also exhibits significant cytotoxicity against HCT-116 and MCF-7 cells, as demonstrated by their respective IC50 values of 42.9 and 7.68 μM [1].
T79556 NDBM

Autophagy Autophagy
NDBM为一种结合Pim-1 kinase的肿瘤特异性探针,具备释放强荧光及细胞毒性,用于筛选及杀伤肿瘤细胞。该化合物特异性地靶向溶酶体并对pH值具有高度敏感性,适用于监测自噬(autophagy)过程及细胞内环境在外部刺激下的pH变化。
T79456 FD1024

Pim Chromatin/Epigenetic; JAK/STAT signaling
FD1024是一种PIM抑制剂,对PIM1PIM2和PIM3的IC50s分别为1.96、38.9及4.17 nM。用于急性髓系白血病研究的FD1024,对AML细胞系显示出显著的抗增殖效果,其对EOL-1、MV-4-11、KG-1和MOLM-16细胞的抑制浓度(IC50s)分别为0.16 μM、0.12 μM、1.05 μM和1.39 μM。此外,FD1024在小鼠模型中也表现出抗肿瘤活性。

化合物

TCS PIM-1 1
Cat.No: T2253
Synonym: 3-氰基-4-苯基-6-(3-溴-6-羟基苯基)-2(1H)-吡啶酮,SC 204330
Target: Pim
Pim-1/2 kinase inhibitor 1
Cat.No: T9229
Synonym:
Target: Pim
TCS-PIM-1-4a
Cat.No: T4215
Synonym: 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮,SMI-4a
Target: Apoptosis, Pim
(Z)-SMI-4a
Cat.No: T3058
Synonym: TCS PIM-1 4a,SMI-4a
Target: Pim
PIM-IN-1
Cat.No: T40319
Synonym:
Target:
PIM-1 Inhibitor 2
Cat.No: T23158
Synonym:
Target: Others
Pim1/AKK1-IN-1
Cat.No: T5093
Synonym: LKB1/AAK1 dual inhibitor,MDK-2275
Target: Pim, Hippo pathway
MNK/PIM-IN-1
Cat.No: T40092
Synonym:
Target:
Pim-1 kinase inhibitor 8
Cat.No: T83627
Synonym:
Target: Pim, PKC
Pim-1 kinase inhibitor 4
Cat.No: T77526
Synonym:
Target: Apoptosis, Pim
Inecalcitol
Cat.No: T24166
Synonym: TX 522,TX-522,TX522,伊奈骨化醇
Target: Apoptosis
PIM1-IN-1
Cat.No: T12474
Synonym:
Target: Pim
Pim-1 kinase inhibitor 1
Cat.No: T60972
Synonym:
Target:
PIM-1/HDAC-IN-1
Cat.No: T61510
Synonym:
Target:
Pim-1 kinase inhibitor 5
Cat.No: T78980
Synonym:
Target: Pim
Pim-1 kinase inhibitor 3
Cat.No: T61074
Synonym:
Target:
Pim-1 kinase inhibitor 2
Cat.No: T62001
Synonym:
Target:
TP-3654
Cat.No: T4523
Synonym:
Target: Pim
M-110
Cat.No: T15830
Synonym:
Target: Pim
SGI-1776
Cat.No: T3078
Synonym: SGI-1776 free base,Pim-Kinase Inhibitor IX
Target: Apoptosis, FLT, Pim, Autophagy
CX-6258
Cat.No: T1834
Synonym: CX 6258
Target: Pim
CX-6258 hydrochloride
Cat.No: T6148
Synonym: CX-6258 HCl,Pim-Kinase Inhibitor X
Target: Pim
K00135
Cat.No: T27704
Synonym: K-00135,Imidazol[1,2-b]pyridazine 1,K 00135,IMIDAZOPYRIDAZIN 1
Target: Pim
SMI-16a
Cat.No: T3989
Synonym: PIM1/2 Kinase Inhibitor VI
Target: Pim
CX-6258 hydrochloride hydrate
Cat.No: T63589
Synonym:
Target:
R8-T198wt
Cat.No: TP2128
Synonym:
Target:
Pim-IN-14j
Cat.No: T71558
Synonym:
Target:
PIM-IN-2
Cat.No: T81460
Synonym:
Target: Pim
HS56
Cat.No: T68341
Synonym:
Target:
PIM1-IN-3
Cat.No: T63720
Synonym:
Target:
PIM1-IN-6
Cat.No: T62188
Synonym:
Target:
PIM1-IN-7
Cat.No: T61700
Synonym:
Target:
NDBM
Cat.No: T79556
Synonym:
Target: Autophagy
FD1024
Cat.No: T79456
Synonym:
Target: Pim
Cat. No. Product Name Target Signaling Pathways
TQ0201 Hispidulin

Dinatin

Pim Chromatin/Epigenetic; JAK/STAT signaling
Hispidulin 是存在于豚草中的一种黄酮,是Pim-1抑制剂,IC50值为2.71 μM。
T8114 Quercetagetin

栎草亭,6-Hydroxyquercetin

Pim Chromatin/Epigenetic; JAK/STAT signaling
Quercetagetin (6-Hydroxyquercetin) 是存在于万寿菊中的一种类黄酮,是一种选择性和细胞渗透性的pim-1激酶抑制,IC50为 0.34 μM,具有抗炎和抗肿瘤活性。

天然产物

Hispidulin
Cat.No: TQ0201
Synonym: Dinatin
Target: Pim
Quercetagetin
Cat.No: T8114
Synonym: 栎草亭,6-Hydroxyquercetin
Target: Pim
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