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Targets Recommended: CXCR

9

抑制剂 & 化合物

13

重组蛋白

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Cat. No. Product Name Target Signaling Pathways
T10297L AMG 487

CXCR Autophagy; GPCR/G Protein; Immunology/Inflammation
AMG 487 是可口服的选择性趋化因子受体3拮抗剂,对 I-IP-10、I-ITAC 和 MIG 的 IC50 值分别为 8、15 和 36nM。
T36982 CXCR3 Antagonist 6c

CXCR3 antagonist 6c is an antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3).1It inhibits calcium mobilization induced by chemokine (C-X-C motif) ligand 11 (CXCL11) in HEK293 cells expressing the human receptor (IC50= 0.06 μM). It is selective for CXCR3 over a panel of 14 human G protein-coupled receptors at 10 μM. CXCR3 antagonist 6c inhibits CXCR3-mediated migration of isolated human T cells (IC50= ~100 nM). 1.Cole, A.G., Stroke, I.L., Brescia, M.-R., et al.Identification and initial eva...
T83769 TC 14012 hydrochloride

H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2

TC 14012是一种化学肽模拟的拮抗剂,针对趋化因子(C-X-C motif)受体4(CXCR4;IC50 = 2.9 nM)和CXCR7激动剂。它能在表达CXCR7的HEK293T细胞中诱导β-arrestin招募(EC50 = 350 nM)。TC 14012可减少HIV在MT-4细胞中的细胞病理效应(EC50 = 0.4 nM),并以CXCR4依赖的方式抑制HIV在体外进入(IC50 = 19.3 nM)。它还能抑制由趋化因子(C-X-C motif)配体12(CXCL12)在MDA-MB-231乳腺癌细胞和人脐静脉内皮细胞(HUVECs)中诱导的迁移,当使用浓度范围从10到1,000 nM时。在通过左前降(LAD)冠状动脉结扎诱导的急性心肌梗死小鼠模型中,TC 14012(10 mg/kg)能减少梗死面积。
T38160 STING Agonist 1a

STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based vir...
T83926 S-Geranylgeranyl-L-glutathione

GGG

S-Geranylgeranyl-L-glutathione是孤儿G蛋白偶联受体(GPCR)P2RY8的配体。该化合物在100 nM浓度下,选择性地诱导P2RY8而非鞘氨醇-1-磷酸受体2(S1P2)、GPR55、半胱氨酸白三烯受体1(CysLT1 receptor)以及CysLT2 receptor的内吞作用。在10 nM浓度下,S-Geranylgeranyl-L-glutathione抑制了表达P2RY8的WEHI-231 B细胞淋巴瘤细胞和分离的人扁桃体生发中心B细胞由趋化因子(C-X-C motif)配体12(CXCL12)诱导的迁移。
T36461 CAY10748

CAY10748

CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β an...
T83841 STING Agonist D61

D61,Stimulator of Interferon Genes Agonist D61

STING激动剂D61(D61)是干扰素基因刺激剂(STING)的激动剂。它在基于细胞的分析中诱导IFN3诱导的分泌性碱性磷酸酶(SEAP)报告基因和IFN-β诱导的报告基因的表达(EC50分别为52.9和116 nM)。D61(4, 6, 和8 µM)增加了编码IFN-β和化学因子(C-X-C基序)配体10CXCL10)的mRNA的表达以及TANK结合激酶1(TBK1)、IRF3和STING在THP-1单核细胞中的磷酸化。在体内,D61(每隔一天0.25 mg/kg)在CT26小鼠结肠癌模型中减少肿瘤体积,而不影响体重。
T83779 EP4 Antagonist 14

Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14

EP4 antagonist 14是一种前列腺素E2(PGE2)受体亚型EP4的拮抗剂,其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募(IC50 = 0.9 nM)。EP4 antagonist 14(10 µM)能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达,这些mRNA编码Il-4、巨噬细胞甘露糖受体1(Mrc1)、几丁质酶样蛋白3(Chil3)、趋化因子(C-X-C)基序配体1(Cxcl1)、表达在髓样细胞上的触发受体2(Trem2)和精氨酸酶-1(Arg1)。在体内,EP4 antagonist 14(每天30 mg/kg),结合抗PD-1抗体,能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。
T35463 (±)14(15)-EET

(±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET

(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage o...

化合物

AMG 487
Cat.No: T10297L
Synonym:
Target: CXCR
CXCR3 Antagonist 6c
Cat.No: T36982
Synonym:
Target:
TC 14012 hydrochloride
Cat.No: T83769
Synonym: H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2
Target:
STING Agonist 1a
Cat.No: T38160
Synonym:
Target:
S-Geranylgeranyl-L-glutathione
Cat.No: T83926
Synonym: GGG
Target:
CAY10748
Cat.No: T36461
Synonym: CAY10748
Target:
STING Agonist D61
Cat.No: T83841
Synonym: D61,Stimulator of Interferon Genes Agonist D61
Target:
EP4 Antagonist 14
Cat.No: T83779
Synonym: Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14
Target:
(±)14(15)-EET
Cat.No: T35463
Synonym: (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET
Target:
Cat. No. Product Name Species Expression System
TMPY-02234 CXCL9 Protein, Human, Recombinant

MIG,CMK,Humig,chemokine ...

Human E. coli
CXCL9 Protein, Human, Recombinant is expressed in E. coli expression system. The predicted molecular weight is 11.9 kDa and the accession number is Q07325.
TMPY-02970 CXCL10 Protein, Human, Recombinant

IFI10,IP-10,chemokine (<...

Human E. coli
CXCL10 Protein, Human, Recombinant is expressed in E. coli expression system. The predicted molecular weight is 8.8 kDa and the accession number is P02778.
TMPY-04943 CXCL10 Protein, Rat, Recombinant (His)

chemokine (C-X-...

Rat P. pastoris (Yeast)
CXCL10 Protein, Rat, Recombinant (His) is expressed in yeast with His tag. The predicted molecular weight is 10 kDa and the accession number is P48973.
TMPY-02203 CXCL9 Protein, Mouse, Recombinant

BB139920,Scyb9,MuMIG,crg...

Mouse E. coli
CXCL9 Protein, Mouse, Recombinant is expressed in E. coli expression system. The predicted molecular weight is 12.3 kDa and the accession number is P18340.
TMPK-01269 CXCL10 Protein, Cynomolgus, Recombinant (His)

IFI10,gIP-10,CX...

Cynomolgus E. coli
C-X-C motif ligand 10 (CXCL10), or interferon-inducible protein-10, is a small chemokine belonging to the CXC chemokine family. Its members are responsible for leukocyte trafficking and act on tissue cells, like endothelial and vascular smooth muscle cells. CXCL10 is secreted by leukocytes and tissue cells and functions as a chemoattractant, mainly for lymphocytes.
TMPJ-00008 CXCL10 Protein, Human, Recombinant (hFc & His)

INP10,10 kDa Interferon Gamma-Indu...

Human HEK293 Cells
Human C-X-C Motif Chemokine Ligand 10 (CXCL10) is a non-ELR chemokine secreted by various cell types, such as monocytes, endothelial cells and fibroblasts, in response to IFN-γ. CXCL10 functions via chemokine receptor CXCR3. CXCL10 has been attributed to several roles, such as chemoattraction for activated T-lymphocytes, inhibition of angiogenesis, and antitumor activity.
TMPY-01751 DR3/TNFRSF25 Protein, Human, Recombinant (hFc)

TRAMP,TR3,WSL-1,TNFRSF12,DR3,WSL-LR,tumor nec

Human HEK293 Cells
DR3/TNFRSF25 Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 45.9 kDa and the accession number is Q93038-10.
TMPY-05760 DR3/TNFRSF25 Protein, Human, Recombinant (hFc), Biotinylated

TRAMP,tumor necrosis fac...

Human HEK293 Cells
DR3/TNFRSF25 Protein, Human, Recombinant (hFc), Biotinylated is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 45.9 kDa and the accession number is Q93038-10.
TMPY-00961 ADAM15 Protein, Human, Recombinant (His)

MDC15,ADAM metallopeptidase domain 15

Human HEK293 Cells
ADAM15 Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 54 kDa and the accession number is Q13444-10.
TMPY-02300 BIN1 Protein, Human, Recombinant (His)

AMPHL,bridging integrator 1,AMPH2,SH3P9

Human E. coli
Amphiphysin 2, also named bridging integrator-1 (BIN1) or SH3P9, Amphiphysin2/BIN1 is a crescent-shaped N-BAR protein playing a key role in forming deeply invaginated tubes in muscle T-tubules, has been recently implicated in rare and common diseases affecting different tissues and physiological functions. BIN1 downregulation is linked to cancer progression and also correlates with ventricular cardiomyopathy and arrhythmia preceding heart failure. Increased BIN1 expression is linked to increased...
TMPK-01450 HLA-C*03:04&B2M&KRAS G12D (GADGVGKSAL) Monomer Protein, Human, MHC (His & Avi), Biotinylated

KRAS1,MHC,K-RAS4B,KRAS,C...

Human HEK293 Cells
Kirsten rat sarcoma 2 viral oncogene homolog (KRAS) is the most commonly mutated oncogene in human cancer. The developments of many cancers depend on sustained expression and signaling of KRAS, which makes KRAS a high-priority therapeutic target. The virtual screening approach to discover novel KRAS inhibitors and synthetic lethality interactors of KRAS are discussed in detail.
TMPK-01456 HLA-C*03:04&B2M&KRAS G12D (GADGVGKSAL) Tetramer Protein, Human, MHC (His & Avi)

KRAS2,NS,MHC,C-K-RAS,KRA...

Human HEK293 Cells
Kirsten rat sarcoma 2 viral oncogene homolog (KRAS) is the most commonly mutated oncogene in human cancer. The developments of many cancers depend on sustained expression and signaling of KRAS, which makes KRAS a high-priority therapeutic target. The virtual screening approach to discover novel KRAS inhibitors and synthetic lethality interactors of KRAS are discussed in detail.
TMPK-01451 HLA-C 03:04&B2M&KRAS G12D (GADGVGKSAL) Monomer Protein, Human, MHC (His & Avi)

NS3,K-RAS4A,K-Ras 2,NS,KRAS1,RASK2,MHC,KI-...

Human HEK293 Cells
Kirsten rat sarcoma 2 viral oncogene homolog (KRAS) is the most commonly mutated oncogene in human cancer. The developments of many cancers depend on sustained expression and signaling of KRAS, which makes KRAS a high-priority therapeutic target. The virtual screening approach to discover novel KRAS inhibitors and synthetic lethality interactors of KRAS are discussed in detail.

重组蛋白

CXCL9 Protein, Human, Recombinant
Cat.No: TMPY-02234
Species: Human
Expression System: E. coli
CXCL10 Protein, Human, Recombinant
Cat.No: TMPY-02970
Species: Human
Expression System: E. coli
CXCL10 Protein, Rat, Recombinant (His)
Cat.No: TMPY-04943
Species: Rat
Expression System: P. pastoris (Yeast)
CXCL9 Protein, Mouse, Recombinant
Cat.No: TMPY-02203
Species: Mouse
Expression System: E. coli
CXCL10 Protein, Cynomolgus, Recombinant (His)
Cat.No: TMPK-01269
Species: Cynomolgus
Expression System: E. coli
CXCL10 Protein, Human, Recombinant (hFc & His)
Cat.No: TMPJ-00008
Species: Human
Expression System: HEK293 Cells
DR3/TNFRSF25 Protein, Human, Recombinant (hFc)
Cat.No: TMPY-01751
Species: Human
Expression System: HEK293 Cells
DR3/TNFRSF25 Protein, Human, Recombinant (hFc), Biotinylated
Cat.No: TMPY-05760
Species: Human
Expression System: HEK293 Cells
ADAM15 Protein, Human, Recombinant (His)
Cat.No: TMPY-00961
Species: Human
Expression System: HEK293 Cells
BIN1 Protein, Human, Recombinant (His)
Cat.No: TMPY-02300
Species: Human
Expression System: E. coli
HLA-C*03:04&B2M&KRAS G12D (GADGVGKSAL) Monomer Protein, Human, MHC (His & Avi), Biotinylated
Cat.No: TMPK-01450
Species: Human
Expression System: HEK293 Cells
HLA-C*03:04&B2M&KRAS G12D (GADGVGKSAL) Tetramer Protein, Human, MHC (His & Avi)
Cat.No: TMPK-01456
Species: Human
Expression System: HEK293 Cells
HLA-C 03:04&B2M&KRAS G12D (GADGVGKSAL) Monomer Protein, Human, MHC (His & Avi)
Cat.No: TMPK-01451
Species: Human
Expression System: HEK293 Cells
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