PAK
PAK(p21激活激酶)
PAKs (p21-activated kinases) are key regulators of actin dynamics, cell proliferation and cell survival. PAKs are Ser/Thr kinases that are classified into two groups on the basis of their structural and functional features: group I (PAK1–3) and group II (PAK4–6). Group I PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain, CD) and are activated by the binding of the active (that is, GTP-bound) forms of Rho GTPases, such as Cdc42 and Rac1. Group II PAKs have no auto-inhibitory domains and are not activated by active Rho GTPases. Because the deregulation of PAKs is closely associated with various human diseases,small-molecule inhibitors of these kinases have great potential as therapeutic agents. In addition, these compounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway.
PAKs are considered prime regulators of the actin cytoskeleton and motility. Due to their central role in actin remodelling and their ability to activate Matrix metalloproteinases (MMPs), Rho GTPases play an important role in tumor cell invasion and metastasis. The current evidence suggests the involvement of PAKs in motility, cell survival, anchorage-independent growth, angiogenesis, invasion, migration and regulation of cell cycle and mitosis. Consequently, PAKs have also been implicated in a number of pathological conditions including cancer.
PAK 相关产品(24)
- GC17214PF-3758309CAS: 898044-15-0纯度: >98.50%
PF-3758309是 ATP竞争性p21活化激酶4(PAK4)抑制剂,其Kd值为2.7nM,Ki值为18.7nM。
- GC14807Fingolimod (FTY720) HClCAS: 162359-56-0纯度: >99.50% / >99.00%
芬戈莫德(FTY720)是一种免疫抑制剂,通常用于治疗多发性硬化症,也有抗癌作用,可以作为HDACi(组蛋白脱乙酰酶抑制剂)。
- GC16607MesalamineCAS: 89-57-6纯度: >98.00%
An NSAID and active metabolite of sulfasalazine, balsalazide, and olsalazine
- GC39209LCH-7749944CAS: 796888-12-5纯度: >99.00%
LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.
- GC43666FingolimodCAS: 162359-55-9纯度: >99.50% / >99.00%
A fungal metabolite with immune modulating activities
- GC50314PF 3758309 dihydrochloride
PF 3758309 dihydrochloride是 ATP竞争性p21活化激酶4(PAK4)抑制剂,其Kd值为2.7nM,Ki值为18.7nM。
- GC50370AZ 13705339CAS: 2016806-57-6
AZ 13705339 是一种高效的选择性 PAK1 抑制剂,对 PAK1 和 pPAK1 的 IC50 分别为 0.33 nM 和 59 nM。 AZ 13705339 与 PAK1 和 PAK2 具有结合亲和力,Kds 分别为 0.28 nM 和 0.32 nM。 AZ 13705339 可用于癌症研究。
- GC61043Mesalamine impurity PCAS: 887256-40-8
MesalamineimpurityP是Mesalamine的杂质。5-Aminosalicylicacid(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。
- GC66036AZ13705339 hemihydrate纯度: >99.00%
AZ13705339 hemihydrate 是一种高效且具有选择性的 PAK1 抑制剂,对 PAK1 和 pPAK1 的 IC50 分别为 0.33 nM 和 59 nM。AZ13705339 hemihydrate 对 PAK1 和 PAK2 具有结合亲和力,Kd 分别为 0.28 nM 和 0.32 nM。AZ13705339 hemihydrate 可用于癌症研究。
- GC73424PRT062607 acetateCAS: 1370261-98-5纯度: >99.00%
PRT062607 acetate是一种口服Syk抑制剂(IC50: 1 nM),可抑制炎症和诱导细胞凋亡。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC10251 | FRAX1036 | 1432908-05-8 | >99.00% | |
A selective PAK1 inhibitor | ||||
| GC12261 | FRAX597 | 1286739-19-2 | >98.00% | |
A PAK1, PAK2, and PAK3 inhibitor | ||||
| GC14615 | KPT-9274 | 1643913-93-2 | - | |
Orally acitve allosteric inhibitor of PAK4 | ||||
| GC16075 | FRAX486 | 1232030-35-1 | >98.00% | |
A group I PAK inhibitor | ||||
| GC16225 | IPA-3 | 42521-82-4 | >99.00% / >98.00% | |
An allosteric inhibitor of PAK1 | ||||
| GC17214 | PF-3758309 | 898044-15-0 | >98.50% | |
PF-3758309是 ATP竞争性p21活化激酶4(PAK4)抑制剂,其Kd值为2.7nM,Ki值为18.7nM。 | ||||
| GC14807 | Fingolimod (FTY720) HCl | 162359-56-0 | >99.50% / >99.00% | |
芬戈莫德(FTY720)是一种免疫抑制剂,通常用于治疗多发性硬化症,也有抗癌作用,可以作为HDACi(组蛋白脱乙酰酶抑制剂)。 | ||||
| GC16607 | Mesalamine | 89-57-6 | >98.00% | |
An NSAID and active metabolite of sulfasalazine, balsalazide, and olsalazine | ||||
| GC18720 | G-5555 | 1648863-90-4 | >99.00% | |
A PAK1 inhibitor | ||||
| GC32830 | NVS-PAK1-1 | 1783816-74-9 | >99.00% | |
An allosteric inhibitor of PAK1 | ||||
| GC33421 | PAK-IN-1 | 1394121-05-1 | >99.00% | |
A group 2 PAK inhibitor | ||||
| GC36095 | G-5555 hydrochloride | - | >98.50% | |
A PAK1 inhibitor | ||||
| GC39209 | LCH-7749944 | 796888-12-5 | >99.00% | |
LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4. | ||||
| GC43666 | Fingolimod | 162359-55-9 | >99.50% / >99.00% | |
A fungal metabolite with immune modulating activities | ||||
| GC44478 | NVS-PAK1-C | 2250019-95-3 | >98.00% | |
A negative control for NVS-PAK1-1 | ||||
| GC50314 | PF 3758309 dihydrochloride | - | - | |
PF 3758309 dihydrochloride是 ATP竞争性p21活化激酶4(PAK4)抑制剂,其Kd值为2.7nM,Ki值为18.7nM。 | ||||
| GC50370 | AZ 13705339 | 2016806-57-6 | - | |
AZ 13705339 是一种高效的选择性 PAK1 抑制剂,对 PAK1 和 pPAK1 的 IC50 分别为 0.33 nM 和 59 nM。 AZ 13705339 与 PAK1 和 PAK2 具有结合亲和力,Kds 分别为 0.28 nM 和 0.32 nM。 AZ 13705339 可用于癌症研究。 | ||||
| GC61043 | Mesalamine impurity P | 887256-40-8 | - | |
MesalamineimpurityP是Mesalamine的杂质。5-Aminosalicylicacid(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。 | ||||
| GC62657 | MRIA9 | 2750707-05-0 | >98.00% | |
MRIA9 是 ATP 竞争性的、pan-SIK 和 PAK2/3 抑制剂,其对 SIK1、SIK2 和 SIK3 的 IC50 值分别为 516 nM, 180 nM 和 127 nM。 | ||||
| GC66036 | AZ13705339 hemihydrate | - | >99.00% | |
AZ13705339 hemihydrate 是一种高效且具有选择性的 PAK1 抑制剂,对 PAK1 和 pPAK1 的 IC50 分别为 0.33 nM 和 59 nM。AZ13705339 hemihydrate 对 PAK1 和 PAK2 具有结合亲和力,Kd 分别为 0.28 nM 和 0.32 nM。AZ13705339 hemihydrate 可用于癌症研究。 | ||||
| GC72148 | st-Ht31 ammonium | - | >95.00% | |
st-Ht31 ammonium是蛋白激酶a (PKA)锚定的膜渗透性肽抑制剂。 | ||||
| GC72868 | AZA197 | 1249398-09-1 | >98.00% | |
AZA197是Cdc42的选择性小分子抑制剂。 | ||||
| GC73301 | 5-Aminosalicylic acid-d3 | 1309283-32-6 | >99.00% | |
5-Aminosalicylic acid-d3是氘标记的5-氨基水杨酸。 | ||||
| GC73424 | PRT062607 acetate | 1370261-98-5 | >99.00% | |
PRT062607 acetate是一种口服Syk抑制剂(IC50: 1 nM),可抑制炎症和诱导细胞凋亡。 | ||||
