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Cell Cycle/DNA Damage——PAK

PAKs (p21-activated kinases) are a family of six serine/threonine kinases that act as key effectors of RHO family GTPases in mammalian cells. PAKs are subdivided into two groups: group I (PAK1, PAK2, and PAK3) and group II (PAK4, PAK5, and PAK6), based on their domain architecture and regulation. Group I PAKs are activated by GTPases such as Cdc42, Rac, TC10, CHP, and Wrch-1, as well as in a GTPase-independent manner. Group II PAKs are generally not activated by Cdc42/Rac binding. PAK plays important roles in cytoskeletal organization, cellular morphogenesis, and survival, and members of this family have been implicated in many diseases including cancer, infectious diseases, and neurological disorders.

PAKs participate in various signaling networks. PAKs activate the MAPK pathway by phosphorylating Raf1 in addition to NF-κB. PAKs also phosphorylate a number of regulators of the cytoskeleton such as MLCK, LIMK, filamin A, ILK, merlin, and Arpc1b. In addition, PAKs regulate survival and apoptotic pathways through phosphorylation of its effectors such as DLC1 and BimL. On translocation to the nucleus, PAKs directly affect gene transcription. Several transcription factors and transcriptional co-regulators such as FKHR, SHARP, CTBP1 and SNAI1 are substrates to PAK1. PAKs also regulate cell cycle progression through phosphorylation of histone H3, Aurora A and PlK1.

Cell Cycle/DNA Damage——PAK(17)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM11150 5-Aminosalicylic Acid

5-Aminosalicylic acid (Mesalamine) 是一种特异性的 PPARγ 激动剂,还抑制 p21-激活激酶1 (PAK1) 和 NF-κB

89-57-6 ≥98%
KM8117 5-Aminosalicylic Acid-D3 hydrochloride

5-Aminosalicylic Acid-D3 (Mesalamine-D3) hydrochloride 是 5-Aminosalicylic Acid hydrochloride 的氘代物。5-Aminosalicylic acid (Mesalamine) hydrochloride 是一种特异性的 PPARγ 激动剂,还抑制 p21-激活激酶1 (PAK1) 和 NF-κB

1346601-18-0
KM6048 Fingolimod

Fingolimod (FTY720 free base) 是一种 1-磷酸鞘氨醇 (sphingosine 1-phosphateS1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50 为 0.033 nM。Fingolimod 还是一种 pak1 激活剂,免疫抑制剂。

162359-55-9 98%
KM10245 Fingolimod hydrochloride

Fingolimod hydrochloride (FTY720) 是鞘氨醇的类似物,是一种有效的 1-磷酸鞘氨醇 (S1P) 受体调节剂。Fingolimod hydrochloride 被鞘氨醇激酶磷酸化,特别是被 SK2 磷酸化,然后可与 S1PR1、3、4 和 5 结合。Fingolimod hydrochloride 诱导 S1P1 的内在化,因此抑制 S1P 的活性。Fingolimod hydrochloride 还是一种 pak1 激活剂。

162359-56-0 98%
KM14571 FRAX1036

FRAX1036 是一种 PAK 抑制剂,对 PAK1,PAK2 和 PAK4 的 Ki 值分别为 23.3 nM,72.4 nM 和 2.4 μM。

1432908-05-8 99%
KM6643 FRAX486

FRAX486 是一种 PAK抑制剂,对 PAK1,PAK2 和 PAK3 的 IC50 值分别为 14,33 和 39 nM。

1232030-35-1 98%
KM6642 FRAX597

FRAX597 是一种有效的 I型 P21激活激酶 (PAK)抑制剂,作用于 PAK123IC50 分别为 8,13 和 19 nM。

1286739-19-2 99%
KM12958 G-5555

G-5555 是有效 PAK1 抑制剂,对 PAK1 和 PAK2 的 Ki 值分别为 3.7 nM 和 11 nM。

1648863-90-4 99%
KM12969 G-5555 hydrochloride

G-5555 hydrochloride是有效,选择性的PAK1抑制剂,Ki值为3.7 nM。

98%
KM3132 GNE 2861

GNE 2861 是 PAK 的抑制剂,对 group II 具有选择性。GNE 2861 抑制 PAK4,PAK5 和 PAK6 的 IC50 值分别为7.5,36和126 nM。

1394121-05-1 99%
KM7127 IPA-3

IPA-3 是一种选择性的,ATP 非竞争的 PAK1 抑制剂,IC50 值为 2.5 μM,对 PAKs 4-6 没有抑制作用。

42521-82-4 99%
KM10410 LCH-7749944

LCH-7749944 (GNF-PF-2356) 是一种有效的 PAK4 抑制剂,IC50 为 14.93 μM。LCH-7749944通过下调 PAK4/c-Src/EGFR/cyclin D1 途径有效抑制人胃癌细胞的增殖,并诱导凋亡 (apoptosis)。

796888-12-5 99%
KM10614 Mesalamine impurity P

Mesalamine impurity P 是 Mesalamine 的杂质。5-Aminosalicylic acid (Mesalamine) 是一种特异性的 PPARγ 激动剂,还抑制 p21-激活激酶 1 (PAK1) 和 NF-κB。

887256-40-8
KM7171 MRIA9

MRIA9 是 ATP 竞争性的、pan-SIKPAK2/3 抑制剂,其对 SIK1、SIK2 和 SIK3 的 IC50 值分别为 516 nM, 180 nM 和 127 nM。

98%
KM4324 NVS-PAK1-1

NVS-PAK1-1是有效,选择性的 PAK1 变构抑制剂,IC50值为5 nM。

1783816-74-9 ≥99%
KM9475 PF-3758309

PF-3758309 是一种有效的、口服的、可逆的 ATP 竞争性 PAK4 抑制剂 (Kd= 2.7 nM; Ki=18.7 nM)。PF-3758309 具有 PAK4 抑制剂的预期细胞功能:抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。

898044-15-0 99%
KE9810 PIR 3.5 6088-51-3 ≥95%
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