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Targets Recommended: FLT TAM Receptor

12

抑制剂 & 化合物

6

重组蛋白

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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.

化合物

UNC2025
Cat.No: T7007
Synonym: mrx-6313,UNC-2025,UNC 2025
Target: FLT, TAM Receptor
MRX-2843
Cat.No: T16144
Synonym: UNC2371
Target: Others, FLT
UNC2541
Cat.No: T17205
Synonym:
Target: Others, FLT, TAM Receptor
UNC 1025
Cat.No: T60197
Synonym:
Target: Others
UNC4203
Cat.No: T63444
Synonym:
Target:
ONO-7475
Cat.No: T8327
Synonym:
Target: Trk receptor, TAM Receptor
UNC3133
Cat.No: T29062
Synonym: UNC 3133,UNC-3133
Target:
MRX-2843 trihydrochloride
Cat.No: T69605
Synonym:
Target:
UNC5293
Cat.No: T9134
Synonym:
Target:
CJ-2360
Cat.No: T63101
Synonym:
Target:
Merestinib dihydrochloride
Cat.No: T15808
Synonym: LY2801653 dihydrochloride
Target: ROCK
UNC2025 hydrochloride
Cat.No: T39474
Synonym: UNC2025 hydrochloride
Target:
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...

重组蛋白

MERTK/Mer Protein, Human, Recombinant (aa 1-323, His)
Cat.No: TMPJ-01143
Species: Human
Expression System: HEK293 Cells
MERTK/Mer Protein, Human, Recombinant (His)
Cat.No: TMPK-00417
Species: Human
Expression System: HEK293 Cells
MERTK/Mer Protein, Human, Recombinant (mFc)
Cat.No: TMPK-00418
Species: Human
Expression System: HEK293 Cells
MERTK/Mer Protein, Mouse, Recombinant (His)
Cat.No: TMPK-01022
Species: Mouse
Expression System: HEK293 Cells
GAS6 Protein, Mouse, Recombinant (His)
Cat.No: TMPY-04830
Species: Mouse
Expression System: HEK293 Cells
ACK1 Protein, Human, Recombinant (GST)
Cat.No: TMPY-04484
Species: Human
Expression System: Baculovirus Insect Cells
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