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Search Results for " pakt "

13

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8656	CAY10404 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T	Apoptosis; Akt; COX	Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Neuroscience; PI3K/Akt/mTOR signaling
	CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) 是一种有效且高度选择性的 COX-2 和 COX-1 抑制剂。它还是 PKB/Akt 和 MAPK 信号通路的有效抑制剂，可诱导 NSC-LC 细胞凋亡，具有镇痛、抗炎和抗癌活性。
T70942	AM-8508
	AM-8508 is a potent and selective PI3Kδ inhibitor. AM-8508 showed good cellular potency (in vitro pAKT IC50 = 4.6 nM ). AM-8505 xhibited excellent HWB potency (HWB (pAKT) IC50 = 2.7 nM). AM-8508 inhibit KLH-specific antibodies in animal models, signifying its potential for the treatment of human inflammatory diseases. PI3Kα and PI3Kβ are ubiquitously expressed and play a role in cell growth, division, and survival.
T26608	AM-1430 AM1430
	AM-1430 is a potent and selective PI3Kδ inhibitor. AM-1430 has cellular potency: pAKT IC50 = 0.8 nM; HWB,u (pAKT) IC 50 = 7.7 nM. Rat KLH: IgG ED50 -= 0.016 mg/kg; IhM ED50 = 0.015 mg/kg. Rat PK Clu = 1.7 L/hr/kg.
T74361	MEK/PI3K-IN-2
	MEK/PI3K-IN-2 (compound 6s) 是一种有效的 MEK/PI3K 抑制剂，其 IC50值分别为 352 nM (MEK1), 107 nM (PI3Kα), 和 137 nM (PI3Kδ)。MEK/PI3K-IN-2 抑制 pAKT 和 pERK1/2 水平。MEK/PI3K-IN-2 对肿瘤细胞具有抗增殖活性。
T26607	AM-0687 AM 0687
	AM-0687 is a potent and selective PI3Kδ inhibitor. AM-0687 has Cellular potency: pAKT IC50 = 0.7 nM; HWB, u (pAKT) IC 50 = 4.6 nM. Rat KLH: IgG ED50 -= 0.026 mg/kg; IgM ED50 = 0.016 mg/kg. Rat PK Clu = 2.3 L/hr/kg.
T68980	MRK003
	MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cel...
T74360	MEK/PI3K-IN-1
	MEK/PI3K-IN-1（compound 6r）是一种高效的MEK/PI3K抑制剂，IC50值为124 nM（MEK1）、130 nM（PI3Kα）及236 nM（PI3Kδ）。该化合物能够降低pAKT和pERK1/2的活性，并展现对肿瘤细胞的抗增殖作用。
T79311	CNBCA
	CNBCA是一种有效的SHP2酶抑制剂，具有选择性和竞争性，IC50值为0.87 μM。该化合物可结合SHP2全长蛋白并抑制其酶活性，进而阻止Akt和ERK1/2的磷酸化，以及抑制BT474和MDA-MB468乳腺癌细胞的生长。CNBCA主要用于乳腺癌的研究。
T1961	Vistusertib AZD2014	Apoptosis; Akt; PI3K; S6 Kinase; mTOR; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling
	Vistusertib (AZD2014) 是一种ATP 竞争性的mTOR 抑制剂，IC50为 2.81 nM。它抑制mTORC1和mTORC2复合物。
T70943	AM-9635
	AM-9635 is a potent and selective PI3Kδ inhibitor. AM-9635 showes good cellular potency (in vitro pAKT IC50 = 4.2 nM ). AM-96352 inhibits KLH-specific IgG and IgM in a dosedependent manner AM-9635 is well tolerated at all doses and exhibits significantly reduced IgG and IgM specific antibodies . PI3Kα and PI3Kβ are ubiquitously expressed and play a role in cell growth, division, and survival.
T6251	PF-04691502 PF4691502	Akt; PI3K; mTOR; Autophagy	Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	PF-04691502 是一种有效的选择性 PI3K 和 mTOR 激酶抑制剂，具有抗肿瘤活性。它与人 PI3Kα、β、δ、γ和 mTOR 结合的 Ki 分别为1.8、2.1、1.6、1.9和16 nM。
T16841	SAR-260301	PI3K	PI3K/Akt/mTOR signaling
	SAR-260301 is an orally available and selective inhibitor of PI3Kβ (IC50: 23 nM).
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...

化合物

Cat.No: T8656

Synonym: 3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T

Target: Apoptosis, Akt, COX

Cat.No: T70942

Cat.No: T26608

Synonym: AM1430

Cat.No: T74361

Cat.No: T26607

Synonym: AM 0687

Cat.No: T68980

Cat.No: T74360

Cat.No: T79311

Cat.No: T1961

Synonym: AZD2014

Target: Apoptosis, Akt, PI3K, S6 Kinase, mTOR, Autophagy

Cat.No: T70943

Cat.No: T6251

Synonym: PF4691502

Target: Akt, PI3K, mTOR, Autophagy

Cat.No: T16841

Target: PI3K

Cat.No: T36308

Cat. No.	Product Name	Target	Signaling Pathways
T3S1701	Dihydrocurcumin	PPAR; Fatty Acid Synthase	DNA Damage/DNA Repair; Metabolism
	Dihydrocurcumin 是姜黄素的主要代谢物，具有减少脂肪积累和减少氧化应激反应的作用。Dihydrocurcumin 可调控SREBP-1C，PNPLA3 和 PPARα 的 mRNA 和蛋白表达水平，使pAKT 和 PI3K 的蛋白表达水平增高，通过 Nrf2 信号通路使细胞胞内 NO 和 ROS 的含量减少。
TMA1743	Ergosterol peroxide	ERK; VEGFR; p38 MAPK; Wnt/beta-catenin; Akt; JAK; CDK; JNK; STAT; Antifection	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Foxo3a activity by inhibiting pAKT and c-Myc and activating pro-apoptotic protein Puma and Bax to

天然产物

Dihydrocurcumin

Cat.No: T3S1701

Target: PPAR, Fatty Acid Synthase

Ergosterol peroxide

Cat.No: TMA1743

Target: ERK, VEGFR, p38 MAPK, Wnt/beta-catenin, Akt, JAK, CDK, JNK, STAT, Antifection

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