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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11228 |
ERK2 IN-1
|
ERK | MAPK |
ERK2 IN-1 is a selective ERK2 inhibitor with an IC50 of 7 nM. | |||
T9034 |
MK2-IN-3
MK2 Inhibitor III |
MAPK | MAPK |
MK2-IN-3 (MK2 Inhibitor III) 是选择性的 MAPKAP-K2 (MK-2)抑制剂(IC50:8.5 nM),能够抑制 U937 细胞及体内 TNFα 的生成。 | |||
T7005 |
Ulixertinib
BVD-523,VRT752271,优立替尼 |
ERK | MAPK |
Ulixertinib (VRT752271) 是一种有效且可逆的 ERK1/ERK2 抑制剂,可抑制 ERK2 和下游蛋白 RSK 的磷酸化,对 ERK2 的IC50值小于 0.3 nM。 | |||
T10429 |
Tizaterkib
AZD-0364 |
ERK | MAPK |
Tizaterkib (AZD-0364) 是一种选择性ERK2抑制剂,IC50为 0.6 nM。 | |||
T1956 |
FR 180204
FR180204 |
Apoptosis; ERK | Apoptosis; MAPK |
FR 180204 是一种 ATP 竞争性的选择性ERK 抑制剂,对ERK1和ERK2的Ki 值分别为 0.31 μM 和 0.14 μM,IC50值分别为0.51 μM 和0.33 μM。 | |||
T11226 |
ERK1/2 inhibitor 1
|
ERK | MAPK |
ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively. | |||
T5358 |
Longdaysin
|
ERK; Casein Kinase; CDK | Cell Cycle/Checkpoint; MAPK; Metabolism; Stem Cells |
Longdaysin 是一种 CK1α 和 CK1δ 的抑制剂,IC50为5.6和8.8 µM。它还抑制ERK2,IC50值为52 µM。它是Wnt/β-catenin 信号通路的抑制剂,通过阻断CK1δ/ε依赖性 Wnt 信号通路发挥抗肿瘤作用。 | |||
T6066 |
SCH772984
|
ERK; MEK | MAPK |
SCH772984 是高选择性和 ATP 竞争性ERK 抑制剂,对 ERK1 和 ERK2 的IC50分别为 4 和 1 nM。它在含有 BRAF 或 RAS 突变的 MAPK 抑制剂初治和 MAPK 抑制剂耐药细胞中具有抗肿瘤活性。 | |||
T3074 |
CHIR 98024
CHIR98014 |
GSK-3; S6 Kinase | MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
CHIR 98024是一种有效的 GSK-3α/β 抑制剂,在无细胞试验中 IC50 为 0.65 nM/0.58 nM,能够区分 GSK-3 与其接近的同源物 Cdc2 和 ERK2。 | |||
T6511 |
Ravoxertinib
GDC-0994 |
ERK | MAPK |
Ravoxertinib (GDC-0994) 是可口服的ERK 激酶抑制剂,抑制ERK1和ERK2的IC50分别为 6.1 和 3.1 nM。 | |||
T4091 |
Temuterkib
LY3214996 |
ERK | MAPK |
Temuterkib (LY3214996) 是高效选择性的ERK1和ERK2抑制剂,IC50为 5 nM,具有潜在的抗肿瘤活性。 | |||
TP1970L |
Prosaptide TX14(A) acetate
Prosaptide TX14(A) acetate(196391-82-9 free base) |
ERK; GPR | Endocrinology/Hormones; GPCR/G Protein; MAPK |
Prosaptide TX14(A) acetate 是一种有效的 GPR37L1 和 GPR37 激动剂。 它增加雪旺细胞中的 ERK1 和 ERK2 磷酸化。 | |||
T4092 |
AG126
Tyrphostin AG126,AG 126 |
ERK; COX | Immunology/Inflammation; MAPK; Neuroscience |
AG126 (Tyrphostin AG126) 是一种酪氨酸激酶抑制剂,可阻止丝裂原活化蛋白激酶 p42MAPK(ERK2) 的激活。 | |||
T6324 |
(E/Z)-BIX02188
334949-59-6 |
ERK; MEK; TGF-beta/Smad | MAPK; Stem Cells |
BIX02188 是一种特异性 MEK5 抑制剂 (IC50: 4.3 nM),也抑制 ERK5 催化活性 (IC50: 810 nM),并且不抑制密切相关的激酶 MEK1/2、JNK2 和 ERK2。 | |||
T6673 |
SKI II
SphK-I2 |
Apoptosis; Wnt/beta-catenin; S1P Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Stem Cells |
SKI II (SphK-I2) 是一种口服有效的合成鞘氨醇激酶 (SK)抑制剂,抑制 SK1 和 SK2,IC50值分别为 78 μM 和 45 μM。它通过诱导溶酶体/蛋白酶体降解,不可逆地抑制SK1。 | |||
T3623 |
Cobimetinib
可美替尼,考比替尼,RG7420,XL518,GDC-0973 |
Apoptosis; MEK | Apoptosis; MAPK |
Cobimetinib (GDC-0973) 是一种可口服的 MEK1选择性抑制剂,抑制MEK1的IC50为4.2 nM。 | |||
T2310L |
CHIR-99021 HCl
CT99021 HCl,Laduviglusib HCl |
GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
CHIR-99021 HCl (Laduviglusib HCl) 是GSK-3α/β的高效选择性抑制剂,IC50值分别为10 nM和6.7 nM。它对GSK-3表现出显著的选择性,对CDC2、ERK2和其他蛋白激酶的选择性超过500倍。此外,CHIR-99021 HCl 是Wnt/β-catenin信号通路的强大激活剂。此外,它在小鼠和人类胚胎干细胞中都表现出增强自我更新的能力。此外,拉杜维格西单盐酸盐诱导自噬[1][2][3]。 | |||
T2608 |
CHIR-98014
CHIR 98014,CT98014,CHIR98014 |
FGFR; GSK-3; Src; S6 Kinase | Angiogenesis; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
CHIR-98014 (CT98014) 是有效的,细胞通透的GSK-3抑制剂,可抑制 GSK-3α (IC50:0.65 nM) 和 GSK-3β (IC50:0.58 nM) 的活性,对 cdc2 和 erk2 的作用较弱。 | |||
T62929 |
RLX-33
|
ERK; RXFP receptor | GPCR/G Protein; MAPK |
RLX-33 是一种有效的、选择性的、能够透过血脑屏障的松弛素家族肽 3 (RXFP3) 拮抗剂,也能够阻断松弛素 3 (relaxin 3) 诱导的 ERK1/2 磷酸化。RLX-33 作用于 RXFP3、ERK1 和 ERK2 磷酸化的 IC50 分别为 2.36 μM、7.82 μM 和 13.86 μM。RLX-33 可以阻断 RXFP3 选择性激动剂 R3/I5 诱导的大鼠食物摄取增加。RLX-33 能够用于研究代谢综合征。 | |||
T36675 |
ERK-IN-4
ERK Inhibitor |
ERK | MAPK |
ERK-IN-4 是一种具有细胞渗透性的 ERK 抑制剂,具有潜在的抗增殖作用,可用于研究免疫功能异常引起的疾病。 | |||
T12069 |
MK-8353
SCH900353 |
ERK | MAPK |
MK-8353 (SCH900353) 是口服有效的ERK1/2选择性抑制剂,IC50分别为 23.0 nM 和 8.8 nM。它显示出抗肿瘤活性。 | |||
T3166 |
VX-11e
Vertex-11e,VTX-11e,TCS ERK 11e |
ERK; GSK-3; FLT; CDK; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
VX-11e (TCS ERK 11e) 是可口服的ERK 高效选择性抑制剂,Ki 值小于 2 nM。 | |||
T11225 |
ERK-IN-2
|
ERK | MAPK |
ERK-IN-2 是ERK2抑制剂,IC50值为 1.8 nM。 ERK-IN-2 在剂量 >10 μM 可能引起脱靶毒性和/或脱靶活性。 | |||
T15377 |
Ravoxertinib hydrochloride
GDC-0994 (hydrochloride) |
ERK | MAPK |
Ravoxertinib hydrochloride is an orally bioavailable and selective inhibitor for ERK kinase activity (IC50: 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively). | |||
T78143 |
(R)-VX-11e
|
ERK | MAPK |
(R)-VX-11e(化合物1)为ERK2抑制剂,具有选择性地阻断ERK2活性的能力。 | |||
T63331 | ERK1/2 inhibitor 8 | ||
ERK1/2 inhibitor 8 是 ERK 的有效抑制剂,能够作用于 ERK2 (IC50: 0.48 nM)。 | |||
T62933 | ERK1/2 inhibitor 7 | ||
ERK1/2 inhibitor 7 是一种 ERK 的有效抑制剂,作用于 ERK2 (IC50: 0.94 nM)。 | |||
T72517 | ERK-IN-2 free base | ||
ERK-IN-2 free base是ERK2抑制剂,IC50为1.8 nM。使用剂量>10 μM时,可能引起脱靶毒性和/或脱靶活性。 | |||
T76556 |
MEK1 Derived Peptide Inhibitor 1
|
||
MEK1Derived Peptide Inhibitor 1,一种肽抑制剂,以IC50值30 μM抑制MEK1激活ERK2。适用于细胞渗透性研究。 | |||
T36672 |
CAY10561
|
||
The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary. CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM). This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 μM) and JNK3 (Ki = 4 μM). CAY10561... | |||
T8461 |
SKI V
|
Apoptosis; PI3K; S1P Receptor | Apoptosis; GPCR/G Protein; PI3K/Akt/mTOR signaling |
SKI V 是一种非竞争性非脂质鞘氨醇激酶抑制剂,对 GST-hSK 的IC50为 2 μM。 它减少有丝分裂的第二信使鞘氨醇-1-磷酸的形成,可诱导细胞凋亡并具有抗肿瘤活性。它还抑制PI3K,对 hPI3k 的IC50为 6 μM。 | |||
T12058 |
MK2-IN-3 hydrate
MK-2 Inhibitor III |
ERK; MAPK; MNK | MAPK |
MK2-IN-3 hydrate (MK-2 Inhibitor III) 是一种口服有活性的、ATP 竞争性的MAPKAP-K2 (MK-2)选择性抑制剂(IC50:0.85 nM)。 | |||
T81387 |
Prosaptide Tx14(A) TFA
|
||
Prosaptide Tx14(A) TFA 为prosaposin衍生的肽类化合物,可有效激活GPR37L1及GPR37,其EC50值分别为5 nM与7 nM。该化合物亦能促进Schwann细胞内ERK1与ERK2的磷酸化作用。 | |||
T62939 | SHR2415 | ||
SHR2415 是一种选择性的、高效的、口服具有活力的 ERK1/2 抑制剂。SHR2415 能够抑制 ERK1 (IC50: 2.8 nM) 和 ERK2 (IC50: 5.9 nM)。SHR2415 在 Colo205 细胞中表现出高效力 (IC50: 44.6 nM)。SHR2415 能够用于癌症的研究。 | |||
T64001 | MAP855 | ||
MAP855 是一种高效的、选择性的、口服具有活力的具、 ATP 竞争性的 MEK1/2 激酶抑制剂,对 MEK1 ERK2 cascade 的 IC50 值为 3 nM,pERKEC50 值为 5 nM。MAP855 对野生型和突变型 MEK1/2 表现出同等的抑制效果。 | |||
T61755 |
E6201
|
||
E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2]. | |||
T38377 |
ADTL-EI1712
ADTL-EI1712 |
||
ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).1It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 μM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 μM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a do... | |||
T2029 |
Bohemine
|
ERK; CDK | Cell Cycle/Checkpoint; MAPK |
Bohemine 是一种合成的选择性CDK 抑制剂,是嘌呤类似物,具有抗癌活性。它对Cdk2/cyclin E、Cdk2/cyclin A 和Cdk9/cyclin T1的IC50分别为 4.6 μM、83 μM 和 2.7 μM。 | |||
T4444 |
A-674563 HCl (552325-73-2(free base))
|
ERK; Akt; PKA; CDK; PKC | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
A-674563 HCl (552325-73-2(free base)) 是一种口服的、ATP 竞争性的、可逆的 Akt 抑制剂(Akt1 的 Ki:11 nM)。它对 PKA 和 Cdk2 具有抑制活性(IC50:16/46 nM),但对 Akt1 的选择性比 CMGC、CAMK 和 TK 家族中的其他激酶高 10 至 >1800 倍。 | |||
T35696 |
Olomoucine II
|
||
Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively... | |||
T2095 |
Seliciclib
Roscovitine,R-roscovitine,CYC202 |
CDK | Cell Cycle/Checkpoint |
Seliciclib (Roscovitine) 是 Cdk2/cyclin E 的有效抑制剂,IC50为0.1 µM。它还抑制 Cdk7/cyclin H、Cdk5/p35 和 Cdc2/cyclin B,IC50为 0.49、0.16和0.65 µM。 | |||
T12102 |
Mps1-IN-1
|
Others | Others |
Mps1-IN-1 is a potent, selective and ATP-competitive inhibitor of Mps1 kinase (IC50 : 367 nM ) | |||
T14072 |
A-443654
|
ERK; VEGFR; GSK-3; FLT; Casein Kinase; MAPK; Akt; PKA; Chk; CDK; Src; PKC; S6 Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
A-443654 是 pan-Akt 抑制剂,对Akt1,Akt2,和Akt3具有同等效力的抑制作用,Ki=均为 160 pM。 | |||
T23337 |
SCH772984 HCl
|
ERK; Others | MAPK; Others |
SCH772984 HCl 是一种特异性的 ERK1/2 抑制剂,具有 I 型和 II 型激酶抑制剂的特性,其 IC50 分别为 4 和 1 nM。 SCH772984 HCl 在 BRAF、NRAS 或 KRAS 突变的肿瘤细胞中具有纳摩尔级细胞效力,并诱导肿瘤消退。 SCH772984 HCl 可用于 MAPK 抑制剂难治性肿瘤的研究。 | |||
T21377 | Aloisine A | ||
Aloisine A is a potent and selective CDK/GSK-3 inhibitor. IC50 data of Aloisine A: Cdk1/cyclin B (IC50: 150nM), Cdk2/cyclin A (IC50: 120nM), Cdk2/cyclin E (IC50: 400nM), Cdk5/p25 (IC50: 200nM), Cdk5/p35 (IC50: 160nM), GSK-3α (IC50: 500nM), GSK-3β (IC50: 6 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3001 |
Honokiol
和厚朴酚,NSC 293100 |
ERK; HCV Protease; MEK; Akt; Autophagy | Autophagy; Cytoskeletal Signaling; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Honokiol (NSC-293100) 是厚朴提取物的活性成分,靶向多种信号分子,具有抗氧化,抗炎,抗血管生成和抗癌活性。它可抑制 Akt 的激活并增强 ERK1/ERK2 的磷酸化。 | |||
T3857 |
magnolin
木兰脂素,(+)-Magnolin,木兰苷 |
ERK | MAPK |
Magnolin 是辛夷的一种主要成分,靶向作用于ERK1和ERK2,IC50值分别为 87 和 16.5 nM,可抑制Ras/ERKs/RSK2信号通路。它在体内外降低肾脏氧化应激,抑制 caspase-3 活性,并增加 Bcl-2 表达,具有抗炎和抗氧化作用。 | |||
T6S0655 |
Corynoxeine
|
ERK | MAPK |
Corynoxeine 是从钩藤中分离的一种天然产物,是 PDGF-BB 诱导血管平滑肌细胞 (VSMCs) 增殖过程中的 ERK1/ERK2抑制剂。 | |||
T15542 |
Hypothemycin
|
Others | Others |
Hypothemycin is a fungal polyketide and is a multikinase inhibitor (Kis: 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively). |