Akt

Catalog No.Inhibitor Name Akt Akt1 Akt2 Akt3 Other Targets
A10003MK-2206 2HCl
***
***
**
A10709Perifosine
*
A11030GSK690693
****
***
***
PKCθ,PKCη,PrkX
A11246Ipatasertib
****
**
***
A11759AZD5363
****
***
***
ROCK2
A11024PF-04691502
****
PI3Kδ,PI3Kα,PI3Kγ
A10094AT7867
**
***
**
PKA,p70 S6K
A13210Triciribine
*
HIV-1
A11031CCT128930
****
p70 S6K,PKA
A11034A-674563
***
PKA,CDK2,GSK-3β
A11032PHT-427
*
PDK-1
A11286Akti-1/2
**
*
*
A15809Uprosertib
*
*
**
A16392Afuresertib
****
****
****
A12464AT13148
**
*
**
PKA,ROCK2,ROCK1
A14138Miltefosine
PI3K,PKC
A10453Honokiol
MEK
A12720TIC10 Analogue
ERK
A13460Deguelin
PI3K
A15903TIC10
ERK
A11287A-443654
****
A1359010-DEBC HCl
*
A16286ARQ-092 (Miransertib)
****
****
***

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

43 个项目

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  1. SC 66

    Catalog No. A12081
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    Akt 抑制剂
    SC 66是Akt的变构抑制剂,促进Akt的泛素化和失活。它在体外和体内显示抗癌活性。 了解更多
  2. GSK2141795 (Uprosertib, GSK795)

    Catalog No. A15809
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    Akt 抑制剂
    GSK2141795 (Uprosertib,GSK795)结合并抑制Akt的活性,这可能导致PI3K/Akt信号传导途径的抑制和肿瘤细胞的增殖以及肿瘤细胞凋亡的诱导。 了解更多
  3. SC79

    Catalog No. A15541
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    Akt phosphorylation activator
    SC79是AKT激活剂。SC79绑定到模仿PtdIns(3,4,5)P3的结合的Akt的plecktrin同源(PH)域,以诱导Akt的构象变化,从而增强磷酸化和激活。 了解更多
  4. TIC10

    Catalog No. A15903
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    Akt 抑制剂?
    TIC10通过Foxo3a使Akt和ERK失活,从而诱导TRAIL,具有优越的药物特性:跨血脑屏障传递,优异的稳定性和改善的药代动力学。 了解更多
  5. Afuresertib HCl

    Catalog No. A13030
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    AKT 抑制剂?
    Afuresertib HCl,也称为GSK2110183,是具有潜在抗肿瘤活性的丝氨酸/苏氨酸蛋白激酶Akt(蛋白激酶B)的生物利用抑制剂。它结合并抑制Akt的活性,这可能导致PI3K/Akt信号传导途径的抑制和肿瘤细胞的增殖以及肿瘤细胞凋亡的诱导.PI3K/Akt信号传导途径的激活通常与肿瘤发生有关,PI3K/Akt信号传导失调可能有助于肿瘤对多种抗肿瘤药的耐药性。 了解更多
  6. SR-13668

    Catalog No. A13554
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    AKT 抑制剂?
    SR-136683是一种口服制剂,其中含有血管内皮生长因子受体(VEGFR)和血小板衍生生长因子受体(PDGFR)的小分子受体酪氨酸激酶抑制剂,具有潜在的抗肿瘤活性。 了解更多
  7. 10-DEBC HCl

    Catalog No. A13590
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    AKT/PKB 抑制剂?
    10-DEBC HCl是Akt/PKB的选择性抑制剂。它抑制IGF-1刺激的磷酸化和Akt的激活(在2.5μM时完全抑制),抑制mTOR,p70 S6激酶的下游激活。 了解更多
  8. TIC10 isomer

    Catalog No. A12720
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    AKT 抑制剂?
    TIC10通过Foxo3a使Akt和ERK失活,从而诱导TRAIL,具有优越的药物特性:跨血脑屏障传递,优异的稳定性和改善的药代动力学。 了解更多
  9. Akt1 and Akt2-IN-1

    Catalog No. A16285
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    AKT 1/2 抑制剂
    Akt1 and Akt2-IN-1是Akt1(IC50 = 3.5 nM)和Akt2(IC50 = 42 nM)的变构抑制剂,具有有效且平衡的活性。 了解更多
  10. ARQ-092 (Miransertib)

    Catalog No. A16286
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    AKT 抑制剂
    ARQ 092是一种口服活化,有效和选择性的AKT抑制剂,IC50值:5.0 nM(AKT1);4.5 nM(AKT2);16 nM(AKT3)。 了解更多
  11. GDC-0068 (Ipatasertib, RG-7440)

    Catalog No. A11246
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    Akt 抑制剂
    GDC-0068 (Ipatasertib,RG-7440)是一种选择性的,具有ATP竞争性的pan-Akt抑制剂,在无细胞试验中,其靶向Akt1、2和3的IC50值分别为5、18和8 nM。 了解更多
  12. AZD5363

    Catalog No. A11759
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    AKT 抑制剂
    AZD5363是有效的AKT抑制剂,在体内具有药效学活性,有潜力作为单一疗法或联合用药来治疗一系列实体瘤和血液肿瘤。 了解更多
  13. MK-2206 2HCl

    Catalog No. A10003
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    AKT 抑制剂
    MK-2206 2HCl是Akt1/2/3的高选择性抑制剂,IC50分别为8 nM/12 nM/65 nM。 了解更多
  14. AKT inhibitor VIII (AKTI-1/2)

    Catalog No. A11286
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    AKT 抑制剂
    AKT inhibitor VIII (AKTI-1/2)是一种细胞可渗透且可逆的喹喔啉化合物,在体外激酶测定中,该化合物有效和选择性地抑制Akt1/Akt2活性(对于Akt1,Akt2和Akt3,IC50分别为58 nM,210 nM和2.12μM)。 了解更多
  15. Perifosine (NSC-639966)

    Catalog No. A10709
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    Akt 抑制剂
    Perifosine (也为KRX-0401) 充当Akt抑制剂和PI3K抑制剂。 了解更多
  16. Palomid 529 (P529)

    Catalog No. A10693
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    AKT 抑制剂
    Palomid 529是PI3K/Akt/mTOR途径的双重TORC1/2抑制剂,在血管生成和细胞增殖中具有广泛的活性。 了解更多
  17. GSK690693

    Catalog No. A11030
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    AKT 抑制剂
    GSK690693是一种新型的ATP竞争性低纳摩尔泛Akt激酶抑制剂(IC50值分别为Akt1、2和3的2、13和9 nM)。 了解更多
  18. A-674563

    Catalog No. A11034
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    Akt 抑制剂
    A-674563是一种B/Akt抑制剂,IC50为14 nM,并且还显示出对PKA和CDK2的抑制活性,IC50分别为16和46 nM。 了解更多
  19. AKT-IN-1

    Catalog No. A21009
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    AKT inhibitor
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM. 了解更多
  20. PF-AKT400

    Catalog No. A21991
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    Akt inhibitor
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM). 了解更多
  21. Ipatasertib dihydrochloride

    Catalog No. A21734
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    pan-Akt inhibitor
    Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA. 了解更多
  22. Tomatidine

    Catalog No. A16233
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    ERK/Akt/NF-kB 抑制剂
    Tomatidine抑制ERK,Akt的磷酸化以及NF-kB的核含量。具有抗炎特性。 了解更多
  23. YS-49

    Catalog No. A21198
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    PI3K/Akt activator
    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. 了解更多
  24. Solenopsin

    Catalog No. A21087
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    ATP-competitive AKT inhibitor
    Solenopsin is an ATP-competitive AKT inhibitor with IC50 value of 10 μM . 了解更多
  25. Afuresertib

    Catalog No. A16392
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    Akt 抑制剂
    Afuresertib是一种有效的口服生物利用性Akt抑制剂,对于Akt1,Akt2和Akt3,Ki分别为0.08 nM,2 nM和2.6 nM。 了解更多
  26. Borussertib

    Catalog No. A13364
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    Akt inhibitor
    Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt. 了解更多
  27. AKT Kinase Inhibitor

    Catalog No. A11285
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    Akt kinase inhibitor
    AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity. 了解更多
  28. 3CAI

    Catalog No. A20924
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    AKT1/AKT2 inhibitor
    3CAI is a potent and specific AKT1 and AKT2 inhibitor. 了解更多
  29. Isobavachalcone

    Catalog No. A11453
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    Akt inhibitor
    Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). 了解更多
  30. AT7867 2HCl

    Catalog No. A15006
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    Akt 抑制剂
    AT7867 dihydrochloride是一种有效的ATP竞争性Akt1/2/3和p70S6K/PKA抑制剂,IC50分别为32 nM/17 nM/47 nM和85 nM/20 nM,在AGC激酶家族之外几乎没有活性。 了解更多
  31. Miltefosine

    Catalog No. A14138
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    PI3K/Akt 抑制剂
    Miltefosine在癌细胞系A431和HeLa中抑制PI3K/Akt活性,ED50为17.2μM和8.1μM。 了解更多
  32. AT13148

    Catalog No. A12464
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    multi-AGC kinase 抑制剂
    AT13148是一种新型多AGC激酶抑制剂,具有强大的药效和抗肿瘤活性,与其他AKT抑制剂相比,具有独特的作用机理。 了解更多
  33. Akt-l-1

    Catalog No. A12435
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    AKT1 抑制剂
    Akt-I-1是Akt1(IC50为4.6 μM)的特异性抑制剂,不抑制AKT2或AKT3。 了解更多
  34. Triciribine

    Catalog No. A13210
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    AKT 抑制剂
    Triciribine,也称为API-2,可抑制Akt的磷酸化水平和激酶活性。 了解更多
  35. Deguelin

    Catalog No. A13460
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    Deguelin是一种天然产物,具有很强的抗增殖活性。 了解更多
  36. KP372-1

    Catalog No. A12877
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    Akt 抑制剂
    KP372-1是合成的小分子AKT抑制剂。 了解更多
  37. A-443654

    Catalog No. A11287
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    Akt 抑制剂
    A-443654是Ki值为160 pM的特异Akt抑制剂,可干扰有丝分裂进程和双极纺锤体形成。 了解更多
  38. Honokiol

    Catalog No. A10453
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    Antiangiogenic and Antitumor Agent
    Honokiol是存在于广玉兰的球果、树皮和叶子中的木脂素,在黑色素瘤、肉瘤、骨髓瘤、白血病、膀胱、肺、前列腺、口腔鳞状细胞癌和结肠癌细胞系中显示促凋亡作用。 了解更多
  39. Triciribine phosphate (NSC-280594)

    Catalog No. A11033
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    AKT 抑制剂
    Triciribine phosphate是一种DNA synthesis抑制剂,也抑制PC3细胞系中的Akt和CEM-SS,H9,H9IIIB,U1细胞中的HIV-1,IC50分别为130 nM和20 nM;对PI3K/PDK1没有抑制作用;作用于缺乏腺苷激酶的细胞,活性降低5000 了解更多
  40. PHT-427

    Catalog No. A11032
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    AKT 抑制剂
    PHT-427是一种新型的Akt/磷脂酰肌醇依赖性蛋白激酶1 pleckstrin同源域抑制剂。 了解更多
  41. CCT128930

    Catalog No. A11031
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    AKT 抑制剂
    CCT128930是一种具有ATP竞争性的AKT抑制剂,是一种有效的高级吡咯并嘧啶铅化合物,相对于PKA表现出对AKT的选择性,可通过靶向单个氨基酸差异实现。 了解更多
  42. AT7867

    Catalog No. A10094
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    AKT 抑制剂
    AT7867是AKT和下游激酶p70 S6激酶(p70S6K)以及蛋白激酶A的新型有效抑制剂。 了解更多
  43. PF-04691502

    Catalog No. A11024
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    PI3K/mTOR 抑制剂
    PF-04691502是PI3K/mTOR激酶抑制剂,也是在PI3K/mTOR信号传导途径中靶向磷脂酰肌醇3激酶(PI3K)和雷帕霉素(mTOR)哺乳动物靶标的药物。 了解更多

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