Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13000 |
Src Inhibitor 3
|
Others; Src | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
Src Inhibitor 3 是一种有效的 c-terminal Src 激酶抑制剂(CSK HTRF 中 IC50 <3 nM,Caliper 中 IC50 <4 nM)。 Src Inhibitor 3 增加由 T 细胞受体信号传导诱导的 T 细胞增殖。 | |||
T2640 |
Rebastinib
DCC2036,DCC 2036,DCC-2036 |
Apoptosis; FLT; Bcr-Abl; Src | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Rebastinib (DCC-2036) 是一种口服有效的,非 ATP 竞争性的 Bcr-Abl 抑制剂,作用于 Abl1WT 和 Abl1T315I,IC50分别为 0.8 nM 和 4 nM,还抑制 LYN、SRC、HCK、FGR、FLT3、KDR 和 Tie-2,对 c-Kit 的活性低。Rebastinib 对 Angiopoietin2-Tie2通路具有抑制作用。 | |||
T2358 |
ENMD-2076
|
Apoptosis; VEGFR; FGFR; FLT; c-RET; PDGFR; Src; Aurora Kinase | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
ENMD2076是一种多靶点激酶抑制剂,抑制Aurora A、Flt3、KDR/VEGFR2、Flt4/VEGFR3、FGFR1、FGFR2、Src、PDGFRα的IC50值分别为1.86、14、58.2、15.9、92.7、70.8、20.2 and 56.4 nM。 | |||
T3935 |
1-Naphthyl PP1
4 -氨基- 1 -叔丁基- 3 -(1' -萘基)吡唑并[3,4 - D]嘧啶,1-NA-PP 1 |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
1-Naphthyl PP1 (1-NA-PP 1) 是选择性的src 家族激酶抑制剂,能够抑制 v-Src (IC50:1.0 μM)、c-Fyn (IC50:0.6 μM)、c-Abl (IC50:0.6 μM)、CDK2 (IC50:18 μM) 和 CAMK II (IC50:22 μM)。 | |||
T7371 |
1-Naphthyl PP1 hydrochloride
1-叔丁基-3-(1-萘基)-1H-吡唑并[3,4-D]嘧啶-4-胺盐酸盐,1-NA-PP 1 hydrochloride |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) 是选择性的 src 家族激酶抑制剂,能够抑制 v-Src (IC50:1.0 μM)、c-Fyn (IC50:0.6 μM)、c-Abl (IC50:0.6 μM)、CDK2 (IC50:18 μM)、CAMK II (IC50:22 μM)。 | |||
T1826 |
PI3K-IN-1
Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409 |
DNA-PK; PI3K | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PI3K-IN-1 (Voxtalisib Analogue) 是 PI3K 抑制剂,PI3K-IN-1(25 μM) 能够阻断 PI3K/Akt 信号通路。 | |||
T6028 |
PF 477736
PF 00477736,PF-477736,PF-736,PF-00477736,PF477736 |
c-Fms; VEGFR; FGFR; FLT; c-RET; Chk; CDK; Src; Aurora Kinase | Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors |
PF 477736 (PF-736,PF-00477736) 是一种特异性、有效且具有 ATP 竞争性的 Chk1 抑制剂,Ki 值为0.49 nM。它也是Chk2抑制剂,Ki 值为 47 nM。它还抑制VEGFR2、Fms、Yes、Aurora-A、FGFR3、Flt3和Ret。 | |||
TQ0132 |
A 419259 trihydrochloride
RK 20449 trihydrochloride |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
A 419259 trihydrochloride (RK 20449 trihydrochloride) 是一种 Src 家族激酶抑制剂,能够抑制 Src (IC50:9 nM)、Lck (IC50:3 nM)、Lyn (IC50:3 nM)。 | |||
T23176 |
PP 3
|
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
PP 3 是 Src 激酶抑制剂 PP 2 的阴性对照 | |||
T12906 |
SI-2 hydrochloride
EPH 116 hydrochloride |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
SI-2 hydrochloride (EPH 116 hydrochloride) 是 SRC-3 的抑制剂,诱导乳腺癌细胞死亡的 IC50 值为 3-20 nM。SI-2 hydrochloride 具有良好的药代动力学特征和改善的毒性,以及可接受的口服可用性。 | |||
T9836 |
(E)-SI-2
|
Others | Others |
(E)-SI-2 是类固醇受体 coactivator-3(SRC-3 或 AIB1)的有效小分子抑制剂,可选择性抑制 SRC-3 的内在转录活性,也抑制 SRC-1 和 SRC-2。它选择性地降低 SRC-3 的细胞蛋白水平,但不降低 CARM-1 的细胞蛋白水平,阻断 MDA-MB-468 细胞生长,IC50 值为 3.4 nM,但不影响正常细胞。 | |||
T28773 |
SI-2
SI2,EPH 116,EPH116,EPH-116 |
Others | Others |
SI-2是类固醇受体辅激活因子-3(SRC-3或 AIB1)的抑制剂(SMI)。SI-2可选择性降低细胞中 SRC-3的转录活性和蛋白浓度,并选择性诱导低纳摩尔范围(3-20 nM)内的乳腺癌症细胞死亡,但不影响正常细胞存活率。 | |||
T6525 |
GW 5074
GW5074,3-(3,5-二溴-4-羟基苯亚甲基)-5-碘-1,3-二氢吲哚-2-酮,Raf1 Kinase Inhibitor I |
Apoptosis; Raf | Apoptosis; MAPK |
GW 5074 (Raf1 Kinase Inhibitor I) 是一种有效且特异性的 c-Raf 抑制剂,IC50值为 9 nM。 它对 JNK1/2/3、MEK1、MKK6/7、CDK1/2、c-Src、p38 MAP、VEGFR2 或 c-Fms 的活性没有影响。 | |||
T5524 |
Aurora kinase inhibitor-3
Aurora Kinase Inhibitor III |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) 是一种有效的,选择性 Aurora A 激酶抑制剂,IC50为 42 nM。 | |||
T9638 |
CCT241161
|
Raf | MAPK |
CCT241161 is an orally active pan-RAF inhibitor, with IC50 values of 3, 6, 10, 15, and 30 nM for LCK, CRAF, SRC, V600E-BRAF, and BRAF, respectively. It displays significant activity against BRAF and NRAS mutant melanomas, as well as demonstrating anticancer cell proliferative effects [1]. | |||
T9659 |
LCB 03-0110
3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol |
Discoidin Domain Receptor (DDR) | Tyrosine Kinase/Adaptors |
LCB 03-0110 (3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol) 是一种盘状结构域受体家族酪氨酸激酶的强效抑制剂,可强烈抑制多种酪氨酸激酶,包括 c-Src 家族、脾酪氨酸激酶、布鲁顿酪氨酸激酶和血管内皮生长因子受体 2,它们对免疫很重要细胞信号传导和炎症反应。 | |||
T36680 |
SM1-71
|
Serine/threonin kinase; MAPK; LIM Kinase; TGF-beta/Smad; AAK1 (AP2 associated kinase 1) | Cell Cycle/Checkpoint; MAPK; Metabolism; Neuroscience; Stem Cells |
SM1-71 是一种有效的多靶点丙烯酰胺修饰的 TAK1 抑制剂,抑制 MKNK2、MAP2K1/2/3/4/6/7、GAK、AAK1、BMP2K、MAP3K7、MAPKAPK5、GSK3A/B、MAPK1/3、SRC、YES1、FGFR1、ZAK (MLTK)、MAP3K1、LIMK1 和 RSK2。SM1-71 可作为激酶探针,具有抗癌活性,抑制多种癌细胞系的增殖。 | |||
T3211 |
Midostaurin
米哚妥林,N-Benzoylstaurosporine,PKC412,CGP41231,CGP 41251,苯甲酰基十字孢碱 |
Others; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Others |
Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂,有抗肿瘤活性,对 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1/2的IC50值范围为 22 到500 nM 之间。 | |||
T10206 |
A 419259
RK-20449 |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
A 419259 is a pyrrolo-pyrimidine inhibitor, designed to enhance selectivity towards the Src family (IC50s: 9 nM, <3 nM and <3 nM for Src, Lck and Lyn). | |||
T69982 |
VPC-16606
|
||
VPC-16606 is a potent and selective inhibitor of ERα-dependent cell growth and gene expression. VPC-16606 prevents the interaction between ERα-LBD and SRC-3 fusion proteins in a dose-dependent manner. | |||
T72363 |
Antiangiogenic agent 3
|
||
Antiangiogenic agent 3 是一种抗血管生成剂,具有抑制人脐静脉内皮细胞(HUVEC)生长、迁移与趋化运动的作用。此外,该化合物还能降低 Src、cdc42 以及 MAPK 的基因表达。 | |||
T79186 | STAT6-IN-3 | STAT | JAK/STAT signaling; Stem Cells |
STAT6-IN-3 (Compound 18a),一种针对STAT6的Src同源2 (SH2) 结构域的抑制剂,具有44 nM的IC50值。该化合物主要适用于研究哮喘等炎症性疾病。 | |||
T73039 |
CYP1B1-IN-3
|
||
CYP1B1-IN-3为选择性CYP1B1抑制剂,其IC50值分别针对CYP1B1、CYP1A1、CYP1A2为6.6, 347.3, >10000 nM。该化合物能够抑制细胞迁移与侵袭,并作用于P-gp、AKT/ERK、FAK/SRC及EMT信号通路。 | |||
T82022 | IVMT-Rx-3 | NF-κB | NF-κB |
IVMT-Rx-3是针对SDCBP的PDZ1和PDZ2结构域,特别是MDA-9/Syntenin的抑制剂。该化合物能够中断MDA-9/Syntenin与Src之间的互动,减少NF-κB的激活,并且降低MMP-2/MMP-9的表达量,从而抑制了黑色素瘤的转移。 | |||
T38653 |
HG-7-85-01
|
||
HG-7-85-01 is a type II ATP competitive inhibitor targeting wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. It effectively inhibits T315I mutant Bcr-Abl kinase, as well as KDR and RET kinases with IC50 values of 3 nM, 20 nM, and 30 nM, respectively. In contrast, HG-7-85-01 exhibits weak or no inhibition towards other kinases (IC50 >2 μM). Furthermore, this compound inhibits cell proliferation through the induction of apoptosis and by impeding cell-cycle progres... | |||
T35536 |
Tpl2 Kinase Inhibitor (hydrochloride)
|
||
Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5... | |||
T36779 |
NG 25 (hydrochloride hydrate)
|
||
NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv... |