66
12
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11342L |
G-5555
|
PAK | Cytoskeletal Signaling |
G-5555 是 PAK1有效抑制剂,对 PAK1 和 PAK2 的Ki 值分别为 3.7 nM 和 11 nM。 | |||
T16429 |
GNE 2861
|
PAK | Cytoskeletal Signaling |
GNE 2861 是一种 PAK 抑制剂,具有 II 组的选择性。它抑制 PAK4、PAK5 和 PAK6 的IC50值分别为7.5、36和126 nM。 | |||
T6014 |
FRAX597
|
PAK | Cytoskeletal Signaling |
FRAX597 是一种有效的 ATP 竞争性 I 组 PAK 抑制剂,作用于PAK1、2和3,IC50分别为 8、13 和 19 nM。 | |||
T6840 |
FRAX486
|
PAK | Cytoskeletal Signaling |
FRAX486 是一种有效的 p21 活化激酶 (PAK) 抑制剂,对 PAK1、PAK2、PAK3 和 PAK4 的 IC50 值分别为 14、33、39 和 575 nM。 | |||
T6839 |
FRAX1036
|
PAK | Cytoskeletal Signaling |
FRAX1036 是一种有效的选择性 PAK1 抑制剂,对 PAK1、PAK2 和 PAK4 的 Ki 值分别为 23.3 nM、72.4 nM 和 2.4 μM。 | |||
T16367 |
NVS-PAK1-1
|
PAK | Cytoskeletal Signaling |
NVS-PAK1-1 是一种有效的选择性变构 PAK1 抑制剂,IC50值为5 nM。 | |||
T6546 |
IPA-3
IPA3,IPA 3 |
PAK | Cytoskeletal Signaling |
IPA-3 是一种选择性的非 ATP 竞争性 Pak1 抑制剂,IC50 为 2.5 μM。 | |||
T9698 |
UC2288
|
Mdm2; p53 | Apoptosis |
UC2288 是新型的、细胞通透性、口服有效的p21衰减试剂,基于索拉非尼的结构合成。在不依赖 于p53的情况下,它可以下调 p21 mRNA 的表达,降低 p21 蛋白水平,对 p21 蛋白的稳定性影响很小。它对VEGFR2 和 Raf 激酶没有抑制作用,即使在 10 μM。 | |||
T7697 |
BIX-01294
|
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
BIX-01294 是高度选择性的G9a 和GLP 组蛋白甲基转移酶可逆抑制剂。它通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP,可诱导坏死性凋亡和自噬,具有抗肿瘤活性。 | |||
T1959 |
BIX-01294 trihydrochloride
BIX 01294 |
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
BIX-01294 trihydrochloride 是可逆且高度选择性的G9a 和GLP 组蛋白甲基转移酶抑制剂,IC50分别为 1.9 μM 和 0.7 μM。它可诱导坏死性凋亡和自噬,具有抗肿瘤活性。它通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP。 | |||
T7539 |
O6-Benzylguanine
O-6-苄基鸟嘌呤 |
Apoptosis; DNA Alkylation; DNA/RNA Synthesis | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
O6-Benzylguanine 是鸟嘌呤类似物,是 DNA 修复酶 O6 烷基鸟嘌呤DNA 烷基转移酶(MGMT/AGT)抑制剂,可诱导肿瘤细胞凋亡,具有抗肿瘤活性。它作为 AGT 底物,将其苄基转移到 AGT 半胱氨酸残基上,从而不可逆地灭活 AGT 并阻止 DNA 修复。 | |||
T2539 |
Fingolimod hydrochloride
Fingolimod (FTY720) HCl,FTY720,盐酸芬戈莫德 |
TRP/TRPV Channel; S1P Receptor; PAK; LPL Receptor | Cytoskeletal Signaling; GPCR/G Protein; Membrane transporter/Ion channel |
Fingolimod hydrochloride (FTY720) 是一种新型免疫调节剂,是一种 1-磷酸鞘氨醇(S1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50为 0.033 nM。它诱导 S1P1 的内化,从而抑制 S1P 活性。它被鞘氨醇激酶磷酸化,尤其是被 SK2 磷酸化,从而可与 S1PR1、3、4 和 5 结合 | |||
T11826 |
LCH-7749944
GNF-PF-2356 |
Apoptosis; PAK | Apoptosis; Cytoskeletal Signaling |
LCH-7749944 (GNF-PF-2356) 是一种 PAK4抑制剂,IC50为 14.93 μM。它通过下调 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。 | |||
T6626 |
PF-3758309
PF-309,PF-03758309,PF 3758309 |
Apoptosis; PAK | Apoptosis; Cytoskeletal Signaling |
PF-3758309 (PF-03758309) 是一种可口服的、可逆的 ATP 竞争性 PAK4抑制剂。它是一种 PAK4 抑制剂,可抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。 | |||
T12472 |
Pifithrin-α, p-Nitro, Cyclic
PFN-α |
p53 | Apoptosis |
Pifithrin-α, p-Nitro, Cyclic (PFN-α) 是 p53 的细胞渗透性和活性形式抑制剂。它对暴露于 Etoposide 的皮层神经元的保护作用比 Pifithrin-α 强一个数量级,ED50为30 nM。它也作为 p53 转录后的活性抑制剂。 | |||
T4230 |
PF-3758309 hydrochloride
PF-03758309 hydrochloride |
Apoptosis; PAK | Apoptosis; Cytoskeletal Signaling |
PF-3758309 hydrochloride (PF-03758309 hydrochloride) 是一种口服的、可逆的 ATP 竞争性PAK4抑制剂,Kd 为 2.7 nM,Ki 为 18.7 nM。它抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖,具有 PAK4 抑制剂的预期细胞功能。 | |||
T3684 |
CP21R7
CP21 |
GSK-3; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells |
CP21R7 (CP21) 是一种 GSK-3β抑制剂,其 IC50=1.8 nM。它也是一种 PKCα抑制剂,其 IC50=1900 nM。 | |||
TP2149 |
NP213 TFA (942577-31-3 free base)
NP213 TFA |
Others | Others |
NP213 TFA is a rapidly acting and first-in-class synthetic antimicrobial peptide (AMP) with anti-fungal activity. It targets the fungal cytoplasmic membrane via membrane perturbation and disruption. | |||
T39772 |
BRK inhibitor P21d hydrochloride
BRK inhibitor P21d hydrochloride |
||
BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK/PTK6), displaying an IC50 of 30 nM. Additionally, it effectively suppresses p-SAM68 with an IC50 value of 52 nM. This compound, BRK inhibitor P21d hydrochloride, serves as a valuable tool for evaluating the efficacy of BRK inhibitors in xenograft breast tumor models, enabling the assessment of their in vivo activity. | |||
T71870 |
CP21
|
||
CP21 is an iron chelator that binds to iron in a 3:1 (ligand:iron) ratio. It is active against P. falciparum when used at concentrations of 10 and 100 µM. CP21 inhibits production of prostaglandin I2 induced by epinephrine, arachidonic acid, or A23187 in isolated rat aortic rings with IC50 values of 1.3, 1.3, and 1.4 mM, respectively. It inhibits glutamate-induced oxytosis, as well as decreases iodoacetic acid-induced cytotoxicity in an in vitro model of ischemia, in HT22 mouse hippocampal cells... | |||
T62252 | R-HP210 | ||
R-HP210 能够抑制 LPS 诱导的多种促炎基因(IL-1β、IL-6 和 COX-2)的转录。R-HP210 对 NF-κB 介导的栓系反式抑制功能的 IC50 值为 3.80 μM。R-HP210 不诱导糖皮质激素 (GCs) 的反式激活功能。 | |||
T73916 |
NP213 TFA
|
||
NP213 TFA是一种具有抗真菌(anti-fungal)活性的快速、新颖的合成抗菌肽(AMP)。该化合物通过瞄准真菌胞质膜并扰乱及破坏其结构来发挥作用,对甲真菌感染显示出高效与良好耐受性。 | |||
TP2149L |
NP213
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
NP213 is a rapidly acting synthetic antimicrobial peptide (AMP). NP213 is effective and well-tolerated in resolving nail fungal infections. NP213 has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays its role via membrane perturbation and disruption. | |||
T78073 |
HP210
|
Glucocorticoid Receptor | Endocrinology/Hormones |
HP210是一种选择性糖皮质激素受体调节剂(SGRM),可以抑制IL-1β和IL-6的mRNA表达,有望用于研究炎症相关疾病。 | |||
T36240 |
AP219
|
||
AP39 is a compound used to increase the levels of hydrogen sulfide (H2S) within mitochondria. It consists of a mitochondria-targeting motif (triphenylphosphonium) coupled to an H2S-donating moiety (dithiolethione) by an aliphatic linker. AP219 is a control compound for AP39, containing the triphenylphosphonium scaffold but lacking the H2S-releasing portion. | |||
T62253 | S-HP210 | ||
S-HP210 是一种选择性的、有效的糖皮质激素受体 (GR) 调节剂,能够抑制 NF-κB 转录 (IC50: 1.92 μM)。S-HP210 对于 LPS 诱导的多种促炎基因(如 IL-1β、IL-6 和 COX-2)的转录具有抑制作用。S-HP210 在有效剂量下对小鼠成纤维细胞 3T3 没有毒性。 | |||
T41169 | P21d hydrochloride | ||
P21d hydrochloride is a potent and selective breast tumor Ki nase (Brk) inhibitor (IC50 = 30 nM). Exhibits >650-fold selectively for Brk over Aurora B Ki nase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also activein vivoand orally bioavailable. | |||
T2454 |
Dacinostat
NVP-LAQ824,达西司特,LAQ824 |
HDAC; Autophagy | Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Dacinostat (NVP-LAQ824) 是一种新型 HDAC 抑制剂,IC50 为 32 nM,是 p21 启动子的激活剂。它也可抑制HDAC1的活性,IC50值为 9 nM,主要用于癌症研究。 | |||
T6840L |
FRAX486 HCL(1232030-35-1 free base)
|
PAK | Cytoskeletal Signaling |
FRAX486 HCL(1232030-35-1 free base) 是一种有效的 p21 活化激酶 (PAK) 抑制剂,对 PAK1、PAK2、PAK3 和 PAK4 的 IC50 值分别为 14、33、39 和 575 nM。 | |||
T0005 |
Aspirin
阿司匹林,Acetylsalicylate,Acetylsalicylic Acid,邻乙酰水杨酸,ASA |
Mitophagy; Virus Protease; COX; Autophagy | Autophagy; Immunology/Inflammation; Microbiology/Virology; Neuroscience |
Aspirin (Acetylsalicylic Acid) 是一种选择性 COX 抑制剂,具有多种药理活性。它是组蛋白去乙酰化酶抑制剂,可上调细胞周期阻滞蛋白 p21,抑制携带 COX-1 的卵巢 Y 细胞。 它还抑制 HUVEC 和新生大鼠心室心肌细胞中 COX-2 的表达,分别减少 PG 的产生和 ERK 和 NF-KB 的下调。 | |||
T8554 |
KCC-07
|
DNA Alkylator/Crosslinker | DNA Damage/DNA Repair |
KCC-07 是一种甲基-CpG 结合域蛋白 2 (MBD2) 的选择性、强效和脑渗透抑制剂,具有抗癌活性。它阻止 MBD2 与甲基化 DNA 结合并激活脑特异性血管生成抑制剂 1,诱导抗增殖 BAI1/p53/p21 信号传导。 | |||
T3465 |
Vesnarinone
维司力农,OPC-8212,Arkin,Piteranometozine |
HIV Protease; PDE | Metabolism; Microbiology/Virology; Proteases/Proteasome |
Vesnarinone (Arkin) 是一种喹啉酮衍生物,可抑制磷酸二酯酶III 活性,增加钙通量和减小钾通量。 | |||
T4321 |
Indisulam
E 7070 |
CDK; Carbonic Anhydrase | Cell Cycle/Checkpoint; Metabolism |
Indisulam (E 7070) 是碳酸酐酶抑制剂。它是细胞周期 G1期的靶向化合物,能够抑制 CDK2及周期蛋白 E 的激活,阻止 G1/S 的转化。它可以募集 DCAF15诱导RBM39降解来靶向剪接,具有抗癌作用。 | |||
T21806 |
HNHA
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HNHA 是组蛋白去乙酰化酶抑制剂。它通过 p21诱导将细胞周期阻滞在 G1/S 期,抑制肿瘤生长及肿瘤新生血管形成。HNHA 可能是一种有效的抗乳腺癌药物。 | |||
T13349 |
WS-383
|
E1/E2/E3 Enzyme | Ubiquitination |
WS-383 是高效、选择性、可逆的DCN1-UBC12相互作用抑制剂,IC50为11 nM。它抑制 Cul3/1 的类泛素化修饰,引起 NRF2,p21和p27 的积累。 | |||
T70371 |
Xylarianaphthol-1
|
||
Xylarianaphthol-1 is an activator of p21 promoter in a p53-independent manner. | |||
T28733 | SCH-53870 | ||
SCH-53870 inhibits p21-hRas nucleotide exchange in vitro. | |||
T24274 |
KY-04031
|
||
KY-04031 is an inhibitor of p21-activated kinase 4. | |||
T37026 |
Mesalamine impurity P
|
||
Mesalamine impurity P is an impurity of Mesalamine . 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[1]. [1]. Kyle Dammann, et al.PAK1 modulates a PPARγ/NF-κB cascade in intestinal inflammation.Biochim Biophys Acta. 2015 Oct;1853(10 Pt A):2349-60. | |||
T26259 |
Tenovin-D3
TenovinD3 |
||
Tenovin-D3 is a sirtuin SirT2 inhibitor. It acts by increasing p21 (CDKN1A) expression in a p53-independent manner. | |||
T11342 |
G-5555 hydrochloride (1648863-90-4 free base)
G-5555 hydrochloride |
PAK | Cytoskeletal Signaling |
G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM. | |||
T71034 |
Bizelesin
|
||
Bizelesin is a synthetic cyclopropylpyrroloindole antineoplastic antibiotic. Bizelesin binds to the minor groove of DNA and induces interstrand cross-linking of DNA, thereby inhibiting DNA replication and RNA synthesis. Bizelesin also enhances p53 and p21 induction and triggers G2/M cell-cycle arrest, resulting in cell senescence without apoptosis. | |||
T22490 |
2,3-DCPE hydrochloride
|
Others | Others |
Induces p21 expression and S-phase arrest in cancer cells via ERK-mediated pathways. IC50 values are 0.89 and 12.6 μM for LoVo human colon cancer cell line and normal human fibroblasts respectively. | |||
T69243 |
AK963
|
||
AK963, also known as 40708899, is a potent PAK1 (p21-activated kinase 1) inhibitor, which suppresses the proliferation of human gastric cancer cells significantly by downregulation of PAK1-NFκB-CyclinB1 pathway. | |||
T73579 |
YM-1
|
||
YM-1 是稳定的和可溶性的MKT-077 类似物和具有口服活性的Hsp70抑制剂。YM-1 诱导 HeLa 细胞死亡,上调p53和p21的蛋白水平。 | |||
T62916 |
GEM144
|
||
GEM144 是一种有效的、口服具有活力的 DNA polymerase α(POLA1) 和HDAC 11 双重抑制剂。GEM144 能够诱导 p53 乙酰化、激活 p21,将细胞周期阻滞在 G1/S 期,并诱导细胞凋亡。 | |||
T15580 |
Inolitazone dihydrochloride
RS5444 dihydrochloride,CS-7017 dihydrochloride,Efatutazone dihydrochloride |
PPAR | DNA Damage/DNA Repair; Metabolism |
Inolitazone dihydrochloride 一种有效的、高亲和力的 PPARγ 激动剂,其生物活性的体现依赖于 PPARγ(IC50:0.8 nM),对细胞生长具有抑制作用。Inolitazone dihydrochloride 加强细胞周期激酶抑制剂p21 WAF1/CIP1的作用。 | |||
T62917 |
MIR002
|
||
MIR002 是一种有效的、口服具有活力的 DNA polymerase α (POLA1) 和 HDAC 11 双重抑制剂,具有显著的体内抗肿瘤活性。MIR002 能够诱导 p53 乙酰化、激活 p21,将细胞周期阻滞在 G1/S 期,并诱导细胞凋亡。 | |||
T73792 |
(S)-(-)-Perillic acid
|
||
(S)-(-)-Perillic acid 是一种萜类植物提取物,具有抗菌和抗癌活性。(S)-(-)-Perillic acid 诱导细胞凋亡和细胞周期阻滞,增加细胞内 Bax,Bcl2,p21和 caspase-3的蛋白水平。(S)-(-)-Perillic acid 可用于癌症和感染研究。 | |||
T64179 | Anticancer agent 65 | ||
Anticancer agent 65 在肿瘤细胞系中显示出良好的效果,尤其是 A549 细胞 (IC50: 1.07 μM)。Anticancer agent 65 能够将 A549 细胞的细胞周期阻滞在 S 期,诱导细胞凋亡,增加 p53、p21 的表达水平,并促使 ROS 生成和 MMP 崩溃。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7939 |
Fingolimod
2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇,FTY-720A,FTY-720,芬戈莫德 |
S1P Receptor; PAK; LPL Receptor | Cytoskeletal Signaling; GPCR/G Protein |
Fingolimod (FTY-720A) 是一种 1-磷酸鞘氨醇 (S1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50为 0.033 nM。它还是pak1激活剂和免疫抑制剂。 | |||
T0646 |
5-Aminosalicylic Acid
Mesalazine,5-ASA,5-氨基水杨酸,Mesalamine |
NF-κB; Lipoxygenase; COX; Glutathione Peroxidase; Endogenous Metabolite; PAK; PPAR | Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB |
5-Aminosalicylic Acid (5-ASA) 是一种特异性的PPARγ激动剂,还抑制 p21-激活激酶1(PAK1) 和NF-κB,具有抗炎活性。 | |||
T8678 |
Naphthazarin
萘茜,5,8-Dihydroxy-1,4-naphthoquinone,DHNQ |
Apoptosis | Apoptosis |
Naphthazarin (5,8-Dihydroxy-1,4-naphthoquinone) 是来自毛紫草的一种天然产物,通过氧化应激、线粒体凋亡诱导因子的激活、微管的解聚、干扰溶酶体功能和 p53 依赖性 p21 激活,可触发细胞凋亡并具有抗肿瘤作用。 | |||
T1633 |
β-Carotene
beta-胡萝卜素,Carotaben,Beta-Carotene,Provitamin A,β-胡萝卜素 |
Apoptosis; ROS; Endogenous Metabolite | Apoptosis; Immunology/Inflammation; Metabolism |
β-Carotene (Provitamin A) 是一种天然存在的视黄醇(维生素 A)前体。它是一种 ROS 调节剂,具有抗氧化和抗炎活性。它可作为抗氧化剂或者促氧化剂,可诱导乳腺癌细胞凋亡,具有抗癌活性。 | |||
T5429 |
Theaflavin 3,3'-digallate
茶黄素-3,3'-双没食子酸,8-Gingerol,TFDG |
Virus Protease; Antioxidant; HIV Protease; HSV | Microbiology/Virology; oxidation-reduction; Proteases/Proteasome |
Theaflavin 3,3'-digallate (8-Gingerol) 是一种寨卡病毒蛋白酶抑制剂,IC50为 2.3 μM。它直接与 ZIKVpro 结合并抑制 ZIKV 复制,可抑制 gp41 和 NS2B-3 蛋白酶的活性,并具有抗 HSV 和 HIV-1病毒活性。它是红茶中的主要多酚,有抗肿瘤作用。 | |||
T6S1917 |
Schisandrol B
Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B |
P450; Reactive Oxygen Species; Autophagy | Autophagy; Immunology/Inflammation; Metabolism; NF-κB |
Schisandrol B (Besigomsin) 是华中五味子的主要活性成分,具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生,也抑制 P-糖蛋白和CYP3A 的活性。 | |||
TN2080 |
Pinoresinol
松脂酚,松脂素,(+)-Pinoresinol |
Apoptosis; NF-κB; CDK; p53 | Apoptosis; Cell Cycle/Checkpoint; NF-κB |
Pinoresinol ((+)-Pinoresinol) 是一种植物来源的木质素,具有抗炎、保肝和杀真菌活性。它导致 CDK 抑制剂 p21(WAF1/Cip1) 在 mRNA 和蛋白质水平上调,抑制 NF-kappaB 和激活蛋白 1 。 | |||
T3314 |
Perillyl alcohol
Isocarveol,Perilla alcohol,紫苏醇 |
Apoptosis; Endogenous Metabolite | Apoptosis; Metabolism |
Perillyl alcohol (Isocarveol) 是一种单萜,可在不影响正常细胞的情况下诱导肿瘤细胞凋亡。 | |||
T16942 |
Sterigmatocystine
|
Others | Others |
Sterigmatocystine is an inhibitor of G1 Phase and DNA synthesis and is used to inhibit p21 activity. Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor. | |||
TN1354 | Aaptamine | c-Myc; TNF; p53 | Apoptosis; Cell Cycle/Checkpoint |
Aaptamine functions as a proteasome inhibitor, it activates p21 promoter in a p53-independent manner. | |||
TMA0918 |
Neochamaejasmine A
|
Caspase | Apoptosis; Proteases/Proteasome |
Neochamaejasmin A can inhibit cellular (3)H-thymidine incorporation (IC 50 12.5 microg/mL) and subsequent proliferation of human prostate cancer LNCaP cells, it blocks cell cycle progression at the G1 phase by activating the p21 protein and ultimately pro | |||
T38243 | Hygrolidin | ||
Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng/ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovan... |