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Cat. No. | Product Name | Form | Specificity Of Inhibition |
---|---|---|---|
CL0118 |
p38 inhibitor kit
p38 inhibitor kit |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T67830 |
p38α inhibitor 3
|
p38 MAPK | MAPK |
p38α inhibitor 3是一种丝裂原活化蛋白激酶P38α的抑制剂,可以有效阻断成肌细胞分化。 | |||
T78652 |
p38α inhibitor 4
|
p38 MAPK | MAPK |
p38α inhibitor 4 是一种选择性 MAPK p38α抑制剂,看而用于研究糖尿病、疼痛和慢性炎症。 | |||
T36012 |
p38α inhibitor 2
|
||
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets[1]. [1]. Raubo P, et al. The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors [published online ahead of pr... | |||
T67944 |
p38 MAP Kinase Inhibitor Ⅵ
|
p38 MAPK | MAPK |
p38 MAP Kinase Inhibitor Ⅵ是一种有效的p38 MAP Kinase 抑制剂,具有抗炎活性。 | |||
T36010 |
p38 MAPK Inhibitor
|
p38 MAPK | MAPK |
p38 MAPK Inhibitor 是p38 MAPK 激酶的有效抑制剂(IC50= 35 nM)。p38 MAPK Inhibitor 抑制癌基因RAS 诱导的衰老。 | |||
T12997 |
SR-318
|
p38 MAPK; TNF | Apoptosis; MAPK |
SR-318 是p38 MAPK 的选择性抑制剂,对 p38α,p38β 和 p38α/β 的IC50分别为 5 nM,32 nM 和 6.11 μM。它有效抑制全血中TNF-α的释放,IC50为 283 nM。它显示出抗癌和抗炎活性。 | |||
T13018 |
SU3327
halicin |
JNK | MAPK |
SU3327 (halicin) 是具有底物竞争性的 JNK 选择性抑制剂,IC50为 0.7 μM。它还抑制 JNK 和 JIP 之间的蛋白相互作用,IC50值为 239 nM。 | |||
T12347 |
p38-α MAPK-IN-1
|
p38 MAPK; Autophagy | Autophagy; MAPK |
p38-α MAPK-IN-1 是一种 MAPK14 (p38-α) 抑制剂,在 EFC 置换试验和 HTRF 试验中 IC50 分别为 2300 nM 和 5500 nM。 | |||
T7661 |
SD-169
SD 169,1H-吲哚-5-甲酰胺 |
p38 MAPK | MAPK |
SD-169 (SD 169) 是一种可口服的 ATP 竞争性MAPK p38α抑制剂,IC50值为 3.2 nM。它对p38β MAPK 的IC50值为 122 nM。它通过抑制 T 细胞的浸润和活化阻止糖尿病的发展。 | |||
T16812 |
RWJ-67657
JNJ 3026582 |
p38 MAPK | MAPK |
RWJ-67657 (JNJ 3026582) 是一种可口服的选择性p38α和p38β抑制剂,IC50分别为 1 和 11 μM。它是心脏保护剂,具有抗炎和抗肿瘤活性。 | |||
T6927 |
Pamapimod
R1503,帕吡莫德,Ro4402257 |
p38 MAPK; Autophagy | Autophagy; MAPK |
Pamapimod (R1503) 是一种新型的选择性 p38 丝裂原活化蛋白激酶抑制剂,对于p38α和p38β的IC50分别为 14 nM 和 480 nM,Ki 分别为 1.3 nM 和 120 nM,对 p38δ 或 p38γ 亚型没有活性,可研究类风湿关节炎和其他自身免疫性疾病。 | |||
T6496 |
Vactosertib
TEW-7197,EW-7197 |
ALK; TGF-beta/Smad | Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors |
Vactosertib (EW-7197) 是有效的、具有 ATP 竞争性的、具有口服活性的激活素受体样激酶 5 (ALK5) 抑制剂(IC50:12.9 nM)。它还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC50为 17.3 nM),表现出强大的抗转移活性和抗癌作用。 | |||
T36011 |
p38 MAP Kinase Inhibitor IV
p38 MAPK Inhibitor IV |
||
p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38 MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38x, and p38δ, respectively, in vitro.[1] It also inhibits LPS-induced TNF-α and IL-1β cytokine production (IC50s = 22 and 44 nM, respectively) in human peripheral blood mononuclear cells. | |||
T35420 |
(S)-p38 MAPK Inhibitor III
(S)-p38 MAPK Inhibitor III |
||
(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively). | |||
T79028 |
p38 Kinase inhibitor 4
|
p38 MAPK | MAPK |
p38 Kinase inhibitor 4 (compound 135) 是高效的 p38 MAP Kinase 抑制剂,具有显著的生物活性。 | |||
T81441 |
PLK1/p38γ-IN-1
|
p38 MAPK | MAPK |
PLK1/p38γ-IN-1(化合物14)为PLK1与p38γ多靶点抑制剂,体外有效抑制人肝细胞癌与肝母细胞瘤细胞增殖。 | |||
T61803 |
p38 MAPK-IN-3
|
||
p38 MAPK-IN-3 (Compound 2c) is a potent inhibitor of p38α MAPK, displaying antitumor properties by promoting apoptosis and increasing reactive oxygen species (ROS) production [1]. | |||
T12871 |
Talmapimod
他匹莫德,SCIO-469 |
p38 MAPK | MAPK |
Talmapimod (SCIO-469) 是 选择性的,具有口服活性的,ATP 竞争性的 p38α抑制剂,对 p38α和 p38β的 IC50 值分别是 9 nM 和90 nM。Talmapimod 在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。 | |||
T2513 |
VX-702
|
p38 MAPK; Autophagy | Autophagy; MAPK |
VX702 是一种高度特异性的 p38α MAPK 抑制剂,对 p38α 的选择性比 p38β 高 14 倍。它是一种小分子研究口服抗细胞因子疗法,用于治疗炎症性疾病,如类风湿性关节炎。 | |||
T3462 |
BMS-582949 hydrochloride
BMS-582949 HCl |
p38 MAPK; Autophagy | Autophagy; MAPK |
BMS-582949 hydrochloride (BMS-582949 HCl) 是一种高度特异性的 p38α MAPK 抑制剂,其 IC50值为13 nM,可研究炎症性疾病。 | |||
T1974 |
PH-797804
PH797804 |
p38 MAPK; Autophagy | Autophagy; MAPK |
PH-797804 是一种 ATP 竞争性的,选择性的p38α/p38β抑制剂,对 p38α 的IC50为 26 nM,Ki 值为 5.8 nM,对 p38β 的Ki 值为 40 nM。 | |||
T5494 |
MW-150
MW01-18-150SRM |
p38 MAPK; Autophagy | Autophagy; MAPK |
MW-150 (MW01-18-150SRM) 是一种选择性、CNS 渗透性和口服活性的 p38α MAPK 抑制剂,Ki 为 101 nM。它可抑制内源性 p38α MAPK 在活化的神经胶质中磷酸化内源性底物 MK2 的能力。 | |||
T6150 |
TAK-715
|
p38 MAPK; Casein Kinase; JNK | MAPK; Metabolism; Stem Cells |
TAK-715 是一种具有口服活性的p38 MAPK 抑制剂,对 p38α 和 p38β 的IC50分别为 7.1 nM 和200 nM。它抑制酪蛋白激酶 I (CK1δ/ε),调节 Wnt/β-catenin 信号传导的激活,有抗炎活性。 | |||
T2277 |
Losmapimod
GSK-AHAB,GW856553X,6-[5-(环丙基氨基甲酰基)-3-氟-2-甲基苯基]-N-(2,2-二甲基丙基)吡啶-3-甲酰胺,GW856553,洛批莫德,SB856553 |
p38 MAPK; Autophagy | Autophagy; MAPK |
Losmapimod (GSK-AHAB) 是一种可口服的特异性 p38 MAPK 抑制剂,抑制 p38α 和 p38β 的 pKi 值分别为 8.1 和 7.6。 | |||
T10277 |
AL 8697
|
p38 MAPK | MAPK |
AL 8697 是一种特异性 p38α MAPK 抑制剂 (IC50 = 6 nM),其特异性是 p38β (IC50 = 82 nM) 的 14 倍,是其他 91 种激酶的 300 倍。 AL 8697 具有抗炎活性。 | |||
T6089 |
Neflamapimod
VX-745 |
p38 MAPK; Autophagy | Autophagy; MAPK |
Neflamapimod (VX-745) 是一种可穿过血脑屏障的,高选择性的p38α抑制剂,对 p38α 的IC50值为 10 nM,p38β 的IC50值为 220 nM。它对 p38β 的特异性高 22 倍,具有抗炎活性。 | |||
T7367 |
Acumapimod
BCT-197 |
p38 MAPK; Autophagy | Autophagy; MAPK |
Acumapimod (BCT-197) 是一种有口服活性的p38 MAP 激酶抑制剂,IC50值小于1 μM。 | |||
T7667 |
R1487
|
p38 MAPK | MAPK |
R1487 是一种口服生物可利用的高选择性 p38α 丝裂原活化蛋白激酶抑制剂。 | |||
T9581 |
ARRY-797
ARRY-371797 |
IL Receptor; p38 MAPK | Immunology/Inflammation; MAPK |
ARRY-797 (ARRY-371797) 是一种有效的选择性 p38α 抑制剂,可抑制 LPS 诱导的 IL-6。 | |||
T1953 |
L-779450
L 779450 |
Raf; Autophagy | Autophagy; MAPK |
L-779450 是一种有效的 ATP 竞争性 Raf 激酶抑制剂,IC50为 10 nM,Kd 为 2.4 nM。 | |||
T2301 |
SB 202190
FHPI,SB202190 |
Apoptosis; p38 MAPK; Autophagy | Apoptosis; Autophagy; MAPK |
SB 202190 (FHPI) 是一种 p38 MAPK 抑制剂,可以抑制 p38α 和 p38β2 (IC50=50/100 nM),具有选择性和细胞渗透性。SB 202190 具有抗肿瘤活性,还可以诱导人胚胎干细胞向心肌细胞分化。 | |||
T4597 |
UM-164
UM164,DAS-DFGO-II |
p38 MAPK; Src; Autophagy | Angiogenesis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
UM-164 (DAS-DFGO-II) 是一种高效的c-Src 抑制剂,Kd 为 2.7 nM。它还抑制p38α和p38β活性。 | |||
T15572 |
IN-1130
|
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
IN-1130 是一种选择性的 ALK5 抑制剂,对 ALK5 介导的 Smad3 磷酸化、酪蛋白和 p38α 丝裂原活化蛋白激酶的 ALK5 磷酸化,IC50 值为 5.3 nM、36 nM 和 4.3 μM。 | |||
T7123 |
AMG-47a
|
VEGFR; p38 MAPK; JAK; Src | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Stem Cells; Tyrosine Kinase/Adaptors |
AMG-47a 是具有口服活性的 Lck 抑制剂,IC50值为 0.2 nM。它具有抗炎作用,对 VEGF2、p38α、p38α、Jak3、MLR 和 IL-2的 IC50值分别为 1、3、72、30 和 21 nM。 | |||
T63067 |
Emprumapimod
|
||
Emprumapimod 是一种选择性的、口服具有活力的 p38α MAPK 抑制剂。Emprumapimod 能够作用于 RPMI-8226 细胞,直接抑制 LPS 诱导产生的 IL-6,其 IC50 值为 100 pM。Emprumapimod 能够用于研究扩张型心肌病和急性炎性疼痛。 | |||
T6784 |
BI-78D3
|
JNK | MAPK |
BI-78D3 是底物竞争性的 JNK 抑制剂(IC50:280 nM),对 JNK 激酶活性具有抑制作用。 | |||
T6380 |
AMG 900
AMG900,AMG-900,莪术醇.姜黄醇 |
p38 MAPK; Tyrosine Kinases; Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; Tyrosine Kinase/Adaptors |
AMG 900 是一种有效且高度选择性的泛极光激酶抑制剂,对Aurora A、B 和C 的IC50分别为 5 nM、4 nM 和 1 nM。 | |||
T2293 |
SGX-523
|
Raf; p38 MAPK; c-Met/HGFR; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
SGX523 是选择性的和 ATP 竞争性的MET 抑制剂 (IC50:4 nM)。它对 MET 的选择性其它他蛋白激酶高 1000 倍。它具有抗肿瘤特性。 | |||
T6976 |
SB 239063
SB239063 |
p38 MAPK; Autophagy | Autophagy; MAPK |
SB 239063 (SB239063) 是一种选择性、可口服的 p38 MAPK 抑制剂,对重组纯化的人 p38α 的 IC50值为 44 nM,具有抗哮喘作用,还被用于增强因衰老或疾病受损的记忆,如阿尔茨海默病。 | |||
T1811 |
WH-4-023
KIN112,KIN001-112,Dual LCK/SRC inhibitor |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
WH-4-023 (Dual LCK/SRC inhibitor) 是选择性Lck 和Src 抑制剂,它们的 IC50 分别为 2 nM、6 nM,对p38α 和 KDR 作用效果稍弱。 | |||
T38752 |
EW-7195
|
ALK; TGF-beta/Smad | Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors |
EW-7195 是一种具有选择性和高效性的 ALK5 (TGFβR1) 抑制剂,IC50 值为 4.83 nM。EW-7195 对 ALK5 的亲和力是 p38α 的 300 多倍。EW-7195 对 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移有抑制作用。 | |||
T7276 |
SD 0006
SD-06,3-[N-(2-羟基乙酰基)-4-哌啶基]-4-(4-嘧啶基)-5-(4-氯苯基)吡唑 |
p38 MAPK; Autophagy | Autophagy; MAPK |
SD 0006 (SD-06) 是一种选择性的、ATP 竞争性的、口服有效的p38α MAPK 的二芳基吡唑抑制剂,IC50值为 110 nM。它可用于治疗关节炎。 | |||
T6047 |
Ralimetinib dimesylate
LY2228820 dimesylate,Ralimetinib,LY2228820,Ralimetinib Mesylate |
Apoptosis; p38 MAPK; Autophagy | Apoptosis; Autophagy; MAPK |
Ralimetinib dimesylate (LY2228820 dimesylate) 是一种选择性,ATP 竞争性的 p38 MAPK α/β抑制剂,IC50分别为5.3 和 3.2 nM。 | |||
T6130 |
Skepinone-L
CBS3830 |
p38 MAPK; Autophagy | Autophagy; MAPK |
Skepinone-L (CBS3830) 是一种选择性 p38 丝裂原活化蛋白激酶抑制剂。 | |||
T68134 |
Ro-3201195
|
p38 MAPK | MAPK |
Ro-3201195是一种新型可口服的p38 MAPK 抑制剂,具有很高的选择性。 | |||
T39343 |
MW-150 hydrochloride
MW01-18-150SRM hydrochloride,MW-150 hydrochloride |
||
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK, with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells. | |||
T7162 |
R1487 Hydrochloride
R1487 (Hydrochloride) |
p38 MAPK; Autophagy | Autophagy; MAPK |
R1487 Hydrochloride (R1487(Hydrochloride)) 是一种可口服的高选择性 p38α 抑制剂,对 p38α 和 p38β 的Kd 值分别为 0.2 nM 和 29 nM。 | |||
T18682 |
SJFδ
|
Others | Others |
SJFδ is a 10-atom linker PROTAC. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ[1]. | |||
T12871L |
Talmapimod hydrochloride
SCIO-469 hydrochloride |
p38 MAPK | MAPK |
Talmapimod hydrochloride is a selective and ATP-competitive p38α inhibitor (IC50: 9 nM). It also shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs. | |||
T36017 |
PF-05381941
|
||
PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively[1]. PF-05381941 inhibits LPS-stimulated release of TNF-αfrom human peripheralmononuclear (PMN) cells with an IC50 of 8 nM[1]. [1]. Kilty I, et al. TAK1 inhibition in the DFG-out conformation. Chem Biol Drug Des. 2013;82(5):500-505. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-04260 |
p38 Protein, Human, Recombinant (His)
mitogen-activated protein kinase 14,CSPB1,PRKM14,RK,p38α... |
Human | Baculovirus Insect Cells |
MAPK14 contains 1 protein kinase domain and belongs to the MAP kinase family. MAP kinases act as an integration point for multiple biochemical signals and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation, and development. MAPK14 can be detected in the brain, heart, placenta, pancreas, and skeletal muscle and it is expressed to a lesser extent in the lung, liver, and kidney. MAPK14 is activated by various environmental stresses ... | |||
TMPY-04430 |
p38 gamma/MAPK12 Protein, Human, Recombinant
mitogen-activated protein kinase 12,SAPK-3,P38 γ/MAPK12,SAPK... |
Human | Baculovirus Insect Cells |
p38 gamma/MAPK12 Protein, Human, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 42.1 kDa and the accession number is P53778. | |||
TMPY-04429 |
p38 gamma/MAPK12 Protein, Human, Recombinant (His & GST)
ERK3,SAPK3,PRKM12,ERK6,P38γ,P38GAMMA,mitogen-activated prote... |
Human | Baculovirus Insect Cells |
p38 gamma/MAPK12 Protein, Human, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 69.8 kDa and the accession number is P53778. | |||
TMPY-04551 |
p38 delta/MAPK13 Protein, Human, Recombinant (GST)
MAPK13,p38δ,PRKM13,MAPK-13,mitogen-activated protein kinase ... |
Human | Baculovirus Insect Cells |
p38 delta/MAPK13 Protein, Human, Recombinant (GST) is expressed in Baculovirus insect cells with GST tag. The predicted molecular weight is 68.4 kDa and the accession number is O15264. | |||
TMPY-04531 |
p38 delta/MAPK13 Protein, Human, Recombinant (GST), Activated in vitro
P38 δ/MAPK13,MAPK13,PRKM13,MAPK-13,p38δ,p38delta,mitogen-act... |
Human | Baculovirus Insect Cells |
p38 delta/MAPK13 Protein, Human, Recombinant (GST), Activated in vitro is expressed in Baculovirus insect cells with GST tag. The predicted molecular weight is 68.4 kDa and the accession number is O15264. | |||
TMPK-00723 |
RANK/TNFRSF11A Protein, Mouse, Recombinant (hFc)
CD265,Rank,FEO,ODFR,NF-KB,OSTS,TNFRSF11A,OPTB7,NFKB,TRANCER,... |
Mouse | HEK293 Cells |
TNFRSF11A, also known as receptor activator of NF-κB (RANK), activates several signaling pathways, such as NF-κB, JNK, ERK, p38α, and Akt/PKB. RANK/TNFRSF11A is a novel and frequent target for de novo methylation in gliomas, which affects apoptotic activity and focus formation thereby contributing to the molecular pathogenesis of gliomas. RANK/TNFRSF11A Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 47.0 kDa and the acce... | |||
TMPK-00351 |
RANK/TNFRSF11A Protein, Human, Recombinant (aa 30-212, hFc)
NF-KB,ODFR,PDB2,Rank,OSTS,NFKB,OPTB7,TNFRSF11A,LOH18CR1,CD26... |
Human | HEK293 Cells |
TNFRSF11A, also known as receptor activator of NF-κB (RANK), activates several signaling pathways, such as NF-κB, JNK, ERK, p38α, and Akt/PKB. RANK/TNFRSF11A is a novel and frequent target for de novo methylation in gliomas, which affects apoptotic activity and focus formation thereby contributing to the molecular pathogenesis of gliomas. RANK/TNFRSF11A Protein, Human, Recombinant (aa 30-212, hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 46.85 kDa ... |