51
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9966 |
GSK-1520489A
|
Wee1 | Cell Cycle/Checkpoint |
GSK-1520489 A 是一种活性 PKMYT1 抑制剂。 | |||
T21976 |
ONO-8130
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
ONO-8130 是前列腺素 EP1 受体选择性拮抗剂,口服有活力,能够阻断 L6 脊髓中ERK 的磷酸化。它可缓解环磷酰胺致膀胱炎小鼠的膀胱疼痛,可用于研究间质性膀胱炎。 | |||
T5401 |
GSK2983559 active metabolite
GSK2983559,RIPK2 inhibitor 1,RIPK2-IN-1 |
RIP kinase | Apoptosis; NF-κB |
GSK2983559 active metabolite (RIPK2-IN-1) 是一种受体相互作用蛋白-2 激酶抑制剂。 | |||
T22436 |
Takeda-6d
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Takeda-6d 是一种新型、有效的 DFG-out RAF/血管内皮生长因子受体 2 (VEGFR2) 抑制剂,IC50 分别为 7.0 nM 和 2.2 nM。 | |||
T1606 |
Fasudil
HA-1077,AT877,法舒地尔 |
ROCK; Serine/threonin kinase; Calcium Channel; PKA; PKC; Autophagy | Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors |
Fasudil (HA-1077) 是一种非特异性 RhoA/ROCK 抑制剂,也是 Ca2+通道拮抗剂和血管扩张剂。它对蛋白激酶有抑制作用,ROCK1 的 Ki 值为 0.33 μM,ROCK2 和 PKA、PKC、PKG 的 IC50值分别 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM。 | |||
T9831 |
MKC-1
Ro-31-7453 |
Apoptosis; Akt; Microtubule Associated; mTOR | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MKC-1 (Ro-31-7453) 是一种口服生物可利用的小分子双吲哚基马来酰亚胺细胞周期抑制剂,具有潜在的抗肿瘤活性。 | |||
T2171 |
SEW2871
SEW2871 |
S1P Receptor; LPL Receptor | GPCR/G Protein |
SEW 2871 是一种可口服的高选择性 S1P1激动剂,EC50为 13.8 nM。它减少血液中的淋巴细胞数量,可用于糖尿病、阿尔茨海默氏病、肝纤维化和炎症相关研究。它激活 ERK、Akt 和 Rac 信号通路,并诱导 S1P1 内在化和再循环。 | |||
T3060 |
Fasudil hydrochloride
Fasudil (HA-1077) HCl,盐酸法舒地尔,HA-1077,Fasudil HCl,HA-1077 hydrochloride,AT-877 |
ROCK; Serine/threonin kinase; Calcium Channel; HIV Protease; PKA; PKC; Autophagy | Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors |
Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA/ROCK 抑制剂,也抑制蛋白激酶,对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。 | |||
T1725 |
Y-27632 dihydrochloride
反式-4-[(R)-1-氨基乙基]-N-(4-吡啶基)环己烷甲酰胺二盐酸盐,Y-27632 2HCl |
ROCK; Apoptosis | Apoptosis; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Y-27632 dihydrochloride (Y-27632 2HCl) 是一种 ROCK-I 和 ROCK-II 抑制剂,具有口服有效性、ATP 竞争性。Y-27632 dihydrochloride 还抑制分离诱导的小鼠前列腺干或祖细胞凋亡。 | |||
T21312 |
Afatinib
阿法替尼,Afatinib free base,BIBW 2992 |
EGFR; Autophagy | Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Afatinib (BIBW 2992) 是一种不可逆的 EGFR 家族抑制剂,抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。 | |||
T1773 |
Afatinib Dimaleate
马来酸阿法替尼,双马来酸盐阿法替尼,BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate |
EGFR; HER; Autophagy | Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Afatinib Dimaleate (BIBW 2992MA2) 是一种可口服的苯胺基-喹唑啉衍生物和受体酪氨酸激酶表皮生长因子受体家族的抑制剂,具有抗肿瘤活性。它抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。 | |||
T15780 |
LP-922761
|
AAK1 (AP2 associated kinase 1) | Neuroscience |
LP-922761 是一种具有有效性、选择性和口服活性的 AAK1 抑制剂,对 BMP-2 诱导蛋白激酶 (BIKE)有抑制作用。LP-922761 可用于治疗治疗神经性疼痛。 | |||
T29071 |
UR13870
Org 48762-0,POLB 001,UR-13870,UR 13870 |
p38 MAPK | MAPK |
UR-13870 (Org 48762-0) 是一种具有口服活性和选择性的 p38 丝裂原活化蛋白激酶(MAPK)抑制剂,可防止小鼠胶原诱导的关节炎中的骨损伤。 | |||
T11184 |
EML4-ALK kinase inhibitor 1
EML4 ALK kinase inhibitor 1,EML4-ALK kinase inhibitor 1 |
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) 是有效的、具有口服活性的类棘皮细胞微管相关蛋白4-间变性淋巴瘤激酶 (EML4-ALK) 的抑制剂,其 IC50 值为 1 nM。 | |||
T5600 |
Darovasertib
LXS196 |
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
Darovasertib (LXS196) 是一种有效的、选择性的和具有口服活性的蛋白激酶C(PKC) 抑制剂,有用于葡萄膜黑素瘤的研究潜力,对 PKCα、PKCθ 和 GSK3β 的 IC50值分别为 1.9、0.4 和 3.1 μM。 | |||
T9556 |
TNIK-IN-3
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM. Additionally, TNIK-IN-3 demonstrates inhibitory activity against Flt4 (IC50 = 0.030 μM), Flt1 (IC50 = 0.191 μM), and DRAK1 (IC50 = 0.411 μM). This compound holds potential for carrying out research on colorectal cancer (CRC) [1]. | |||
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。 | |||
T9229 |
Pim-1/2 kinase inhibitor 1
|
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
Pim-1/2 kinase inhibitor 1 是一种具有口服活性的 Pim-1/2 激酶抑制剂。Pim-1/2 kinase inhibitor 1 能阻断 Pim 激酶磷酸化肽的能力,并且抑制4E-BP1和p27Kip1的Pim 蛋白激酶定向磷酸化。Pim-1/2 kinase inhibitor 1 可用于癌症,尤其是前列腺癌的研究。 | |||
T9498 |
BAY-8400
|
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
BAY-8400是一种具有口服活性、有效和选择性 DNA 依赖蛋白激酶 (DNA-PK) 抑制剂(IC50=81 nM),与靶向α疗法联合使用显示协同疗效。BAY-8400 可用于癌症研究。 | |||
T3579 |
PLX8394
|
Raf | MAPK |
PLX8394 是一种口服活性的丝氨酸/苏氨酸蛋白激酶 B-Raf (BRAF) 蛋白抑制剂。 PLX8394 可以选择性地结合并抑制野生型和突变形式的 BRAF 的活性,然后抑制表达 BRAF 突变形式的肿瘤细胞的增殖。 PLX8394 似乎对表达多种激酶突变形式的肿瘤有效,并且可能是对其他对 BRAF V600E 突变体特异的 BRAF 抑制剂疗法耐药的肿瘤的有效治疗剂。 | |||
TP1924L1 |
ZIP acetate(863987-12-6 free base)
|
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
ZIP acetate(863987-12-6 free base) 是一种新型的细胞渗透性蛋白激酶 Mζ (PKMζ) 抑制剂,它是一种参与 LTP 维持的组成型活性非典型 PKC 同工酶。在体外选择性阻断 PKMζ 诱导的海马切片突触增强。逆转晚期 LTP (IC50 = 1 - 2.5 μM) 并在体内中央给药后导致 1 天前的空间记忆持续丧失。 | |||
T6931L |
PD0166285 dihydrochloride
PD-166285 |
||
PD-166285 is an effective and broadly active inhibitor of protein tyrosine kinase. | |||
T71600 | Benazoline oxalate salt | ||
Benazoline oxalate salt is a pharmacological active compound that inhibits casein kinase Iε (CKIε) or CKIδ phosphorylation of the PER2 protein. | |||
T68477 | XL-418 | ||
XL-418 is a selective, orally active small molecule, targeting protein kinase B (PKB or AKT) and ribosomal protein S6 Kinase (p70S6K), with potential antineoplastic activity. XL418 inhibits the activities of PKB and p70S6K, both acting downstream of phosphoinosotide-3 kinase (PI3K). These kinases are often upregulated in a variety of cancers. Inhibition of PKB by this agent will induce apoptosis, while inhibition of p70S6K will result in the inhibition of translation within tumor cells. | |||
T75937 |
Pep2m, myristoylated TFA
|
||
Pep2m, myristoylated TFA (Myr-Pep2m TFA)为具备细胞渗透性的肽。该化合物通过破坏PKMζ与其下游靶点NSF/GluR2的相互作用而发挥作用,其中PKMζ为具有自主活性的PKC同工酶。 | |||
TP1924 |
ZIP
|
||
Novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-phase LTP (IC50 = 1 | |||
T36019 |
PKA Inhibitor (5-24) (trifluoroacetate salt)
|
||
PKI PKA Inhibitor (5-24) is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki= 2.3 nM) derived from the active site of the skeletal muscle inhibitor protein.1It mimics the protein substrate by binding to the catalytic site through the arginine-cluster basic subsite.1The prominent enzyme-substrate interaction site occurs where PKA catalytic subunit residues Tyr235and Phe239form a sandwich-like structure with residue Phe10of PKI (5-24).2 | |||
T71556 |
MK-1496
|
||
MK1496 is a n orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a n... | |||
T76399 |
PKI(5-22)amide
|
||
PKI(5-22)amide 是环 AMP 依赖性蛋白激酶 (PKA) 抑制剂的活性片段。PKI(5-22)amide 抑制PKA 激活,但不能减弱 CRF1 受体的同源脱敏作用。 | |||
T36673 | CC 401 dihydrochloride | ||
High affinity JNK inhibitor (Ki values are 25-50 nM). Inhibits JNK via competitive binding of the ATP-binding site of active, phosphorylated JNK. Exhibits > 40-fold selectivity for JNK over p38, ERK, IKK2, protein kinase C, Lck and ZAP70. Hepatoprotective. Also inhibits HCMV replication. Uehara et al (2004) c-Jun N-terminal kinase mediates hepatic injury after rat liver transplantation. Transplantation. 78 324 PMID:15316358 |Uehara et al (2005) JNK mediates hepatic ischemia reperfusion injury. J... | |||
T61604 |
PKC-IN-4
|
||
PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), exhibiting an IC 50 value of 0.52 μM. In vitro studies have demonstrated that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α. Moreover, this compound effectively impedes the permeability of the retinal vasculature, induced by both VEGF and TNFα. [1] | |||
T63008 | PERK-IN-5 | ||
PERK-IN-5 是一种高度选择性的、高效的、口服具有活力的蛋白激酶 R 样内质网 (ER) 激酶 (PERK) 抑制剂,能够作用于 PERK (IC50: 2 nM) 与 p-eIF2α (IC50: 9 nM)。在 786-O 肾细胞癌异种移植瘤模型中,PERK-IN-5 可以明显抑制肿瘤生长。 | |||
T60515 | CaMKIIα-IN-1 | ||
CaMKIIα-IN-1 (Compound 4d) 是一种具有口服活性的 Ca 2+/钙调素依赖性蛋白激酶 II α (CaMKIIα) 抑制剂。CaMKIIα-IN-1对 CaMKIIα WT hub 的 Kd 值为 219 nM。CaMKIIα-IN-1 表现出良好的代谢稳定性。 | |||
T76482 |
PKI (5-24),amide
|
||
PKI (5-24),amide (IP20-amide)为对应于cAMP依赖性蛋白激酶热稳定抑制蛋白活性部分的20残基肽。该化合物是一种高效的cAMP依赖性蛋白激酶(PKA)抑制剂,具有2.3 nM的Ki值。 | |||
T38269 | Purfalcamine | ||
Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras... | |||
T80210 |
TAT-GluN2BCTM
|
DAPK | Apoptosis |
TAT-GluN2BCTM 是一种靶向DAPK1的膜透性肽,能够促使活性DAPK1定向降解于溶酶体。该化合物通过降低DAPK1的表达,有助于防护神经元免遭氧化应激和NMDAR-介导的兴奋毒性。TAT-GluN2BCTM常用于神经保护性研究领域。 | |||
T80269 |
AC3-I, myristoylated
Autocamtide-3 Derived Inhibitory Peptide |
CaMK | Neuroscience |
AC3-I, myristoylated 为一种具有高度特异性的 CaMKII 抑制剂,为 Autocamtide-3 衍生的生物活性肽。通过将 Autocamtide-3 中的 Thr-9 磷酸化位点替换为 Ala,赋予该肽抗蛋白水解能力,从而制备出该肉豆蔻酰化形式。 | |||
T35829 | CC-90005 | ||
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS... | |||
T63057 |
LRRK2-IN-5
|
||
LRRK2-IN-5 (compound 25) 是一种口服具有活力的、能透过血脑屏障的、选择性富含亮氨酸重复蛋白激酶 2 基因 (LRRK2) 抑制剂,对 GS LRRK2 (IC50: 1.2 μM) 和 WT LRRK2 (IC50: 16 μM) 具有抑制作用。LRRK2-IN-5 能够抑制 LRRK2 Ser1292 和 Ser925 的自磷酸化。 | |||
T70865 |
BMY-42393
|
||
BMY-42393 is orally active and selective platelet aggregation inhibitor. BMY-42393 is also a prostacyclin partial agonist that inhibited ADP, collagen and thrombin-induced platelet aggregation (IC50 range 0.3 - 2.0 microM). BMY-42393 stimulated platelet adenylate cyclase activity (EC50 = 25 nM). Platelets treated with BMY 42393 showed an elevation of cAMP levels and activation of cAMP-dependent protein kinase. BMY 42393 also inhibited thrombin-induced elevation of intracellular free calcium. B... | |||
T62871 | LRRK2-IN-6 | ||
LRRK2-IN-6 (compound 22) 是一种具有血脑屏障通透性的、口服具有活力的、选择性富含亮氨酸重复蛋白激酶 2 基因 (LRRK2) 抑制剂,能够抑制 GS LRRK2 (IC50: 4.6 μM) 和 WT LRRK2 (IC50: 49 μM)。LRRK2-IN-6 对 LRRK2 Ser1292 和 Ser925 的自磷酸化表现出抑制作用。 | |||
T61828 |
DNA-PK-IN-8
|
||
DNA-PK-IN-8(化合物DK1)是一种高效、选择性且口服活性的DNA依赖蛋白激酶 (DNA-PK) 抑制剂,其IC50值为0.8 nM。与Doxorubicin联合应用时,该化合物能在多种癌细胞中展现出协同的抗增殖效应,并能显著地抑制HL-60肿瘤生长。 | |||
T63362 |
Ulecaciclib
|
||
Ulecaciclib 是口服具有活力的、能够透过血脑屏障的、表现出良好的药代动力学特征的细胞周期蛋白依赖激酶 (CDK) 抑制剂,对CDKs 的ki 为 0.62 μM (CDK2/Cyclin A)、3 nM (CDK6/Cyclin D3) 、0.2 nM (CDK4/Cyclin D1)和 0.63 μM (CDK7/Cyclin H)。 | |||
T78218 |
Ilaprazole sodium hydrate
IY-81149 sodium hydrate |
Proton pump | Membrane transporter/Ion channel |
Ilaprazole (IY-81149) sodium hydrate是一种具有口服活性的质子泵抑制剂,可以量依赖性地不可逆抑制H+/K+-ATPase,并在兔壁细胞制剂中展示出IC50为6μM的效力。该化合物主要用于胃溃疡的研究,并已证实是一种有效的T细胞起源蛋白激酶(TOPK)抑制剂。 | |||
T63741 | SGK1-IN-3 | ||
SGK1-IN-3 是有效的、口服具有活力的 SGK1 抑制剂。其中丝氨酸/苏氨酸激酶 SGK1 是 β-连环蛋白途径的激活剂,也是强大的软骨降解刺激剂,在患病的骨关节炎软骨中被发现在基因组控制下被上调。SGK1-IN-3 对骨关节炎表现出研究潜力。 | |||
T64266 | KR-39038 | ||
KR-39038 是一种口服具有活力的 GRK5 (G 蛋白偶联受体激酶 5) 抑制剂 (IC50: 0.02 μM)。KR-39038 能够抑制新生儿心肌细胞的 HDAC5 通路,明显抑制血管紧张素 II 诱导的细胞肥大,具有显著的抗心肌肥厚和改善心功能作用。KR-39038 能够用于进行心力衰竭的研究。 | |||
T62143 | LP-922761 hydrate | ||
LP-922761 hydrate 是一种选择性的、有效的、口服具有活力的 AAK1 抑制剂,在酶和细胞分析中 IC50 值分别为 4.8 nM 和 7.6 nM。LP-922761 hydrate 对 BMP-2 诱导蛋白激酶 (BIKE) 具有抑制作用 (IC50: 24 nM)。LP-922761 hydrate 对细胞 GAK、阿片类药物、肾上腺素 α2 或 GABAa 受体没有明显作用。 | |||
T63991 | BRD4/CK2-IN-1 | ||
BRD4/CK2-IN-1 是高效的、口服具有活力的 BRD4/CK2 (含溴结构域蛋白 4/酪蛋白激酶 2) 双靶点抑制剂,能够作用于 BRD4 (IC50: 180 nM) 和 CK2 (IC50: 230 nM)。在三阴性乳腺癌 (TNBC) 中,BRD4/CK2-IN-1 能够诱导细胞凋亡和自噬相关的细胞死亡。BRD4/CK2-IN-1 表现出显著的抗癌效果,且没有明显毒性。 | |||
T73359 |
NYX-2925
|
||
NYX-2925 是一种口服有效的NMDAR 调节剂。NYX-2925 恢复 mPFC 中 GluN2A 和 GluN2B 上活化的Src 和Src 磷酸化位点的水平。NYX-2925 对 CAMKII 没有影响,也没有任何成瘾或镇静/共济失调的副作用。NYX-2925 可用于多种 NMDA 受体介导的中枢神经系统疾病的研究。 | |||
T72658 | cRIPGBM chloride | ||
cRIPGBM chloride是一种口服有效的促凋亡衍生物,针对多形性胶质母细胞瘤(GBM)中的癌症干细胞(CSC)。该化合物通过靶向受体相互作用蛋白激酶2(RIPK2),诱导caspase 1依赖的细胞凋亡,抑制RIPK2/TAK1的活性,增加RIPK2/caspase 1复合物的形成,表现出强大的体内抗肿瘤效果。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1448 |
(-)-Bornyl acetate
L-(-)-Bornyl acetate,左旋乙酸冰片酯,Bornyl acetate,(-)-乙酸龙脑酯 |
p38 MAPK; NF-κB; JNK; Antifungal | MAPK; Microbiology/Virology; NF-κB |
(-)-Bornyl acetate (L-(-)-Bornyl acetate) 是存在于牛膝草油中的一种具有抗真菌活性的 (+)-Bornyl acetate 低活性异构体。 | |||
T1719 |
Bufalin
|
ATPase | Membrane transporter/Ion channel |
Bufalin 是蟾酥中的一种成分,是Na+/K+-ATPase 抑制剂,具有抗肿瘤活性,可与其基 α1、α2 和 α3 结合,Kd 值分别为 42.5、45 和 40 nM。 |