12
6
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7007 |
UNC2025
mrx-6313,UNC-2025,UNC 2025 |
FLT; TAM Receptor | Angiogenesis; Tyrosine Kinase/Adaptors |
UNC2025 (mrx-6313) 是高效的、具有口服活性的、ATP 竞争性的Mer/Flt3双抑制剂,IC50值分别为 0.74 nM 和 0.8 nM。它对MERTK 的选择性比 Axl 高 45 倍(IC50:122 nM;Ki:13.3 nM)。它具有良好的 PK 特性,可用于研究急性白血病。 | |||
T16144 |
MRX-2843
UNC2371 |
Others; FLT | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
MRX-2843 (UNC2371) 是ATP 竞争性的、具有口服活性的MERTK 和FLT3酪氨酸激酶抑制剂 (TKI),它们的IC50分别为 1.3 nM 和 0.64 nM。 | |||
T17205 |
UNC2541
|
Others; FLT; TAM Receptor | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
UNC2541 是 Mer 酪氨酸激酶特异性抑制剂,与 MerTK ATP 结合口袋结合的IC50值为 4.4 nM,对其选择性远高于 Axl,Tyro3 和 Flt3。它能够抑制磷酸化的 MerTK (pMerTK;EC50,510 nM)。 | |||
T60197 |
UNC 1025
|
Others | Others |
UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 ... | |||
T63444 |
UNC4203
|
||
UNC4203 是一种有效的、高度选择性的、口服具有活力的 MERTK 抑制剂,能够作用于 MERTK (IC50: 1.2 nM)、AXL (IC50: 140 nM)、TYRO3 (IC50: 42 nM) 和 FLT3 (IC50: 90 nM)。 | |||
T8327 |
ONO-7475
|
Trk receptor; TAM Receptor | Tyrosine Kinase/Adaptors |
ONO-7475 是一种选择性的、有效的、具有口服活性的Axl/Mer 抑制剂。它使 AXL 过表达的EGFR 突变型 NSCLC 细胞对 EGFR-TKIs 敏感,抑制耐药细胞的产生和耐药性的维持。它与 Osimertinib 联合使用,具有用于 EGFR 突变非小细胞肺癌的潜力。 | |||
T29062 |
UNC3133
UNC 3133,UNC-3133 |
||
UNC3133 is a potent and selective Mer tyrosine kinase (MerTK) inhibitor with IC50 Mer 3.0 nM; Axl 17nM; Tyro 3.31 nM; FLT3 6.6 nM; PO Cmax = 0.023; IV T1/2 = 1.59 h, %F = 16. Mer tyrosine kinase (MerTK) is aberrantly elevated in various tumor cells and ha | |||
T69605 |
MRX-2843 trihydrochloride
|
||
MRX-2843 trihydrochloride is a potent and orally active MERTK and FLT3 inhibitor. | |||
T9134 | UNC5293 | ||
UNC5293 是一种有效的、口服的、高度 MERTK 选择性的抑制剂 (Ki=190 pM)。UNC5293 抑制 MERTK (IC50=0.9 nM),对 Axl、Tyro3 和 Flt3 更具选择性。UNC5293 表现出优异的小鼠药代动力学特性,并可以被用于骨髓白血病研究。 | |||
T63101 |
CJ-2360
|
||
CJ-2360 是一种有效的、口服具有活力的 ALK 抑制剂,能够作用于野生型 ALK (IC50: 2.2 nM) 和 F1197M (IC50: 4.0 nM)、G1269A (IC50: 8.8 nM)、L1196M (IC50: 6.3 nM) 和 S1206Y ALK 突变体(IC50: 8.9 nM)。CJ-2360 能够较强的抑制临床报道的两种 ALK 突变体 (C1156Y 和 L1196M) 以及 468 种激酶 (LTK、MERTK、CLK1、DAPK1 和 DAPK2)。 | |||
T15808 |
Merestinib dihydrochloride
LY2801653 dihydrochloride |
ROCK | Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells |
Merestinib dihydrochloride is an effective and orally bioavailable c-Met inhibitor (Ki=2 nM). It has anti-tumor activities and also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), RO | |||
T39474 |
UNC2025 hydrochloride
UNC2025 hydrochloride |
||
UNC2025 hydrochloride is a potent, ATP-competitive, highly orally active Mer/Flt3 inhibitor. It has IC50 values of 0.74 nM and 0.8 nM, respectively, for Mer and Flt3. UNC2025 hydrochloride demonstrates over 45-fold selectivity for MERTK compared to Axl (IC50 = 122 nM; Ki = 13.3 nM). Additionally, UNC2025 hydrochloride exhibits excellent PK properties, making it suitable for investigating acute leukemia. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPJ-01143 |
MERTK/Mer Protein, Human, Recombinant (aa 1-323, His)
MER,Receptor tyrosine kinase MerTK,Tyrosine-protein... |
Human | HEK293 Cells |
Tyrosine-protein kinase Mer (MERTK) is a single-pass type I membrane protein which belongs to the MER/AXL/TYRO3 receptor kinase family. MERTK include two fibronectin type-III domains, two Ig-like C2-type domains, and one tyrosine kinase domain. It can’t be expressed in normal B- and T-lymphocytes, but it is usually expressed in numerous neoplastic B- and T-cell lines. MERTK could regulate many physiological processes, such as cell survival, migration, differentiation. It was demonstrated that t... | |||
TMPK-00417 |
MERTK/Mer Protein, Human, Recombinant (His)
Tyro12,MGC133349,c-mer,MERTK,c-Eyk,RP38,MER |
Human | HEK293 Cells |
MER tyrosine kinase (MERTK) encodes a surface receptor localized at the apical membrane of the retinal pigment epithelium. It plays a critical role in photoreceptor outer segment internalization prior to phagocytosis. Mutations in MERTK have been associated with severe autosomal recessive retinal dystrophies in the RCS rat and in humans. MERTK/Mer Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 53.73 kDa and the accession... | |||
TMPK-00418 |
MERTK/Mer Protein, Human, Recombinant (mFc)
MER,Tyro12,MERTK,c-Eyk,MGC133349,c-mer,RP38 |
Human | HEK293 Cells |
MER tyrosine kinase (MERTK) encodes a surface receptor localized at the apical membrane of the retinal pigment epithelium. It plays a critical role in photoreceptor outer segment internalization prior to phagocytosis. Mutations in MERTK have been associated with severe autosomal recessive retinal dystrophies in the RCS rat and in humans. MERTK/Mer Protein, Human, Recombinant (mFc) is expressed in HEK293 mammalian cells with C-mFc tag. The predicted molecular weight is 78.9 kDa and the accession ... | |||
TMPK-01022 |
MERTK/Mer Protein, Mouse, Recombinant (His)
Tyro12,c-Eyk,MGC133349,RP38,c-mer,MERTK,MER |
Mouse | HEK293 Cells |
MER tyrosine kinase (MERTK) encodes a surface receptor localized at the apical membrane of the retinal pigment epithelium. It plays a critical role in photoreceptor outer segment internalization prior to phagocytosis. Mutations in MERTK have been associated with severe autosomal recessive retinal dystrophies in the RCS rat and in humans. MERTK/Mer Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 53.38 kDa and the accession... | |||
TMPY-04830 |
GAS6 Protein, Mouse, Recombinant (His)
growth arrest-specific 6,Gas-6 |
Mouse | HEK293 Cells |
The growth arrest-specific 6 gene (GAS6) is a member of the family of plasma vitamin K-dependent proteins, which are able to bind to phospholipids using an N-terminal gamma-carboxyglutamic acid domain. GAS6 is a vitamin K-dependent protein, plays a role in the survival, proliferation, migration, differentiation, adhesion, and apoptosis of cells. The growth arrest-specific 6 (GAS6) has been implicated in systemic inflammation and coagulation. Growth arrest-specific 6 (GAS6), plays a role in tumor... | |||
TMPY-04484 |
ACK1 Protein, Human, Recombinant (GST)
ACK-1,ACK1,p21cdc42Hs,ACK,tyrosine kinase, non-receptor, 2 |
Human | Baculovirus Insect Cells |
ACK1 (also known as ACK, TNK2, or activated Cdc42 kinase) is a structurally unique non-receptor tyrosine kinase that is expressed in diverse cell types. This downstream effector of CDC42 mediates CDC42-dependent cell migration via phosphorylation of BCAR1. The ACK1 protein may be involved in a regulatory mechanism that sustains the GTP-bound active form of Cdc42Hs and which is directly linked to a tyrosine phosphorylation signal transduction pathway. ACK1 integrates signals from plethora of liga... |