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Targets Recommended: Raf Ras

23

抑制剂 & 化合物

3

天然产物

9

重组蛋白

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Cat. No. Product Name Target Signaling Pathways
T1892 Kobe2602

Raf; Ras GPCR/G Protein; MAPK
Kobe2602 是 Ras-Raf 相互作用抑制剂,具有抗癌化疗活性。它抑制 H-Ras·GTP 与 c-Raf-1 RBD 结合的Ki 值为 149 μM。
T2678 LB42708

Transferase Metabolism
LB42708 是一种口服有活力的特异性法尼基转移酶抑制剂。它对H-Ras、N-Ras 和K-Ras4B 的法尼基化均有抑制作用,其IC50分别为 0.8 nM、1.2 nM 和 2.0 nM。
T38050 CP-609754

Transferase Metabolism
CP-609754 是高效的、可逆的法尼基转移酶抑制剂,对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。
T6302 Lonafarnib

Sarasar,氯那法尼,Sch66336

Raf; Transferase; Autophagy; Ras Autophagy; GPCR/G Protein; MAPK; Metabolism
Lonafarnib (Sch66336) 是一种可口服的 FPTase 抑制剂,作用于 H-ras、K-ras 和 N-ras,IC50分别为 1.9 nM、5.2 nM 和 2.8 nM。它具有抗肝炎三角洲病毒的活性。
T1876 Kobe0065

Apoptosis; Raf; Ras Apoptosis; GPCR/G Protein; MAPK
Kobe0065 是一种新型 Ras-Raf 相互作用抑制剂,可完全抑制 H-Ras·GTP 与 c-Raf-1 RBD 的结合,Ki 值为 46±13 μM。
T5469 K-Ras-IN-1

Raf; Ras GPCR/G Protein; MAPK
K-Ras-IN-1 是K-Ras 抑制剂。K-Ras-IN-1 能与 K-Ras (WT)、K-Ras (G12D)、K-Ras (G12V) 和 H-Ras 结合。它对胰腺癌、结肠癌和肺癌的具潜在的研究价值。
T2700 FTI-277 hydrochloride

FTI 277 HCl

Apoptosis; Transferase; Ras Apoptosis; GPCR/G Protein; MAPK; Metabolism
FTI-277 hydrochloride (FTI 277 HCl) 是一种法尼基转移酶FTase 抑制剂,高效 Ras CAAX 肽模拟物,可抑制H-Ras 和K-Ras 信号转导,还可抑制hepatitis delta virus 感染。
T22106 MLS-573151

CDK; Ras Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
MLS-573151 是 GTPase Cdc42 的选择性抑制剂,EC50 为 2 μM。它通过阻止 GTP 与 Cdc42 的结合来发挥作用。
T69710 LB42908

Others Others
LB42908 is a highly potent Ras farnesyltransferase inhibitor(IC(50)=0.9 nM against H-Ras and 2.4 nM against K-Ras) with potential anticancer activity.
T27089 CRT0066854

CRT0066854 HCl,CRT-0066854 HCl,CRT 0066854,CRT-0066854

Others Others
CRT-0066854 is a PKCι and PKCζ inhibitor. CRT0066854 was able to restore polarized morphogenesis in the dysplastic H-Ras spheroids.
T41212 FTI 277

Others Others
FTI 277 is a prodrug form of FTI 276 that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10μM respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.
T62675 FTI-277

Others Others
FTI-277 是一种法尼基转移酶 FTase 抑制剂,也是一种高效 Ras CAAX 肽模拟物。FTI-277 对 H-Ras 和 K-Ras 信号转导具有抑制作用,能够抑制 hepatitis delta virus (HDV) 感染。
T26469 A-176120

Others Others
A-176120 is a potent farnesyl pyrophosphate (FPP) analogues, it selectively inhibits farnesyltransferase. It has anti-angiogenic potential and may reduce H-ras NIH3T3 tumour growth.
T15353 FTI-2153

Others Others
FTI-2153 is a potent and highly selective farnesyltransferase (FTase) inhibitor (IC50: 1.4 nM). FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing.
T72707 (Rac)-Lonafarnib

Sch66336 racemate

Others Others
(Rac)-Lonafarnib (Sch66336外消旋体) 作为Lonafarnib的外消旋体,属于一种口服有效的法尼基蛋白转移酶 (FPTase) 抑制剂,针对H-ras、K-ras及N-ras展现出杰出的抑制效能,其IC50值分别为1.9 nM、5.2 nM和2.8 nM。此外,Lonafarnib还显示出对抗肝炎三角洲病毒 (HDV) 的潜在活性。
T68227 BMS-214662 HCl

Others Others
BMS-214662 is a Farnesyltransferase inhibitor , is also a nonsedating benzodiazepine derivative with potential antineoplastic activity. BMS-214662 inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction, which may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. This agent may reverse the malignant phenotype of H-Ras-transformed cells and has been shown to be active against tumor cell...
T24188 J-104871

UNII-6137X5QNJF,J 104871

Others Others
J-104871 is an FTase inhibitor. J-104871 inhibits FTase in an FPP-competitive manner in whole cells as well as in the in vitro system. J-104871 suppressed tumor growth in nude mice transplanted with activated H-ras-transformed NIH3T3 cells.
T69618 XR3054

Others Others
XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kina...
T62379 GGTI-286

Others Others
GGTI-286 是一种高效的、具有细胞通透性 GGTase I 抑制剂 (IC50: 2 μM)。GGTI-286 对 NIH3T3 细胞中的 Rap1A 香叶香叶基化的(IC50: 2 μM)抑制作用强于 H-Ras 的法尼化作用(IC50>30 μM)。GGTI-286 也可以有效抑制 K-Ras4B 刺激(IC50: 1 μM)。
T73822 GGTI-286 TFA

Others Others
GGTI-286 TFA 是一种高效的细胞通透性 GGTase I 抑制剂,(IC50为 2 μM。在 NIH3T3 细胞中,GGTI-286 TFA 对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50s=2 和 >30 μM)。GGTI-286 TFA 还能有效抑制 K-Ras4B 刺激,IC50为 1 μM。
T85180 GGTI 2133 TFA

Others Others
GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM). The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 µM) without affecting the farnesylation of H-Ras (IC50= >30 µM). Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. ...
T62980 GGTI-286 hydrochloride

Others Others
GGTI-286 hydrochloride 是一种 GGTase I 的高效抑制剂 (IC50: 2 μM),也能够有效抑制 K-Ras4B (IC50: 1 μM)。GGTI-286 hydrochloride 在 NIH3T3 细胞中,对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50=2和 >30 μM)。
T64101 FTI-2153 TFA

Others Others
FTI-2153 TFA 是一种高选择性的、有效的法尼基转移酶 farnesyltransferase (FTase) 抑制剂 (IC50: 1.4 nM)。FTI-2153 TFA 可有效抑制 H-Ras 蛋白的加工修饰 (IC50: 10 nM),对其抑制活性是对 Rap1A 蛋白加工的 3000 多倍。

化合物

Kobe2602
Cat.No: T1892
Synonym:
Target: Raf, Ras
LB42708
Cat.No: T2678
Synonym:
Target: Transferase
CP-609754
Cat.No: T38050
Synonym:
Target: Transferase
Lonafarnib
Cat.No: T6302
Synonym: Sarasar,氯那法尼,Sch66336
Target: Raf, Transferase, Autophagy, Ras
Kobe0065
Cat.No: T1876
Synonym:
Target: Apoptosis, Raf, Ras
K-Ras-IN-1
Cat.No: T5469
Synonym:
Target: Raf, Ras
FTI-277 hydrochloride
Cat.No: T2700
Synonym: FTI 277 HCl
Target: Apoptosis, Transferase, Ras
MLS-573151
Cat.No: T22106
Synonym:
Target: CDK, Ras
LB42908
Cat.No: T69710
Synonym:
Target: Others
CRT0066854
Cat.No: T27089
Synonym: CRT0066854 HCl,CRT-0066854 HCl,CRT 0066854,CRT-0066854
Target: Others
FTI 277
Cat.No: T41212
Synonym:
Target: Others
FTI-277
Cat.No: T62675
Synonym:
Target: Others
A-176120
Cat.No: T26469
Synonym:
Target: Others
FTI-2153
Cat.No: T15353
Synonym:
Target: Others
(Rac)-Lonafarnib
Cat.No: T72707
Synonym: Sch66336 racemate
Target: Others
BMS-214662 HCl
Cat.No: T68227
Synonym:
Target: Others
J-104871
Cat.No: T24188
Synonym: UNII-6137X5QNJF,J 104871
Target: Others
XR3054
Cat.No: T69618
Synonym:
Target: Others
GGTI-286
Cat.No: T62379
Synonym:
Target: Others
GGTI-286 TFA
Cat.No: T73822
Synonym:
Target: Others
GGTI 2133 TFA
Cat.No: T85180
Synonym:
Target: Others
GGTI-286 hydrochloride
Cat.No: T62980
Synonym:
Target: Others
FTI-2153 TFA
Cat.No: T64101
Synonym:
Target: Others
Cat. No. Product Name Target Signaling Pathways
T5368 Eicosapentaenoic Acid

Histone Demethylase; Others; Endogenous Metabolite Chromatin/Epigenetic; Metabolism; Others
Eicosapentaenoic Acid 是一种 ω-3 脂肪酸。
T5S0620 3-Dehydrotrametenolic acid

Dehydrotrametenolic acid,松苓新酸,3-氢化去氢松苓酸

Apoptosis; Others; Dehydrogenase Apoptosis; Metabolism; Others
3-Dehydrotrametenolic acid 是从茯苓菌核分离的一种乳酸脱氢酶抑制剂,可诱导细胞凋亡,具有抗癌活性。它促进体外脂肪细胞分化,在体内起胰岛素增敏剂的作用。
T72152 Eicosapentaenoic Acid sodium

二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium

Others Others
Eicosapentaenoic Acid (EPA) sodium 为口服活性 ω-3 长链多不饱和脂肪酸 (ω-3 LC-PUFAs)。其通过DNA去甲基化,促进肿瘤抑制基因CCAAT/增强子结合蛋白δ (C/EBPδ)的重新表达,并通过H-RAS内含子1 CpG岛的去甲基化,激活U937白血病细胞中RAS/ERK/C/EBPβ途径。此外,该化合物能够促进血管平滑肌细胞松弛和血管舒张。

天然产物

Eicosapentaenoic Acid
Cat.No: T5368
Synonym:
Target: Histone Demethylase, Others, Endogenous Metabolite
3-Dehydrotrametenolic acid
Cat.No: T5S0620
Synonym: Dehydrotrametenolic acid,松苓新酸,3-氢化去氢松苓酸
Target: Apoptosis, Others, Dehydrogenase
Eicosapentaenoic Acid sodium
Cat.No: T72152
Synonym: 二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium
Target: Others
Cat. No. Product Name Species Expression System
TMPY-04311 RAB11B Protein, Human, Recombinant (His)

H-YPT3,RAB11B, member RAS oncogene family

Human HEK293 Cells
The two recurrent dominant mutations in RAB11B leading to a neurodevelopmental syndrome, likely caused by altered GDP/GTP binding that inactivate the protein and induce GEF binding and protein mislocalization.
TMPY-02220 HRAS Protein, Human, Recombinant (His)

HAMSV,Harvey rat sarcoma viral oncogene

Human Baculovirus Insect Cells
HRas, also known as HRAS, belongs to the small GTPase superfamily, Ras family, and is widely expressed. It functions in signal transduction pathways. HRas can bind GTP and GDP, and they have intrinsic GTPase activity. It undergoes a continuous cycle of de- and re-palmitoylation, which regulates its rapid exchange between the plasma membrane and the Golgi apparatus. Defects in HRAS are the cause of faciocutaneoskeletal syndrome (FCSS). FCSS is a rare condition characterized by prenatally increase...
TMPY-02132 LYPLA2 Protein, Human, Recombinant (His)

APT-2,lysophospholipase II,DJ886K2.4,APT2

Human E. coli
Lysophospholipase II (LYPLA2, LPL-II, or LysoPLA II), also known as Acyl-protein thioesterase 2 (APT-2), belongs to the AB hydrolase 2 family. This enzyme has lysophospholipase activity and may hydrolyze fatty acids from S-acylated cysteine residues in proteins such as trimeric G alpha proteins or HRAS. Acyl-protein thioesterase 1 (APT-1) and Acyl-protein thioesterase 2 (APT-2) are cytosolic lysophospholipids hydrolyzing enzymes. The serum activity of APT-1 may play an important role in the dete...
TMPY-01187 Rac1 Protein, Human, Recombinant (GST)

Rac-1,p21-Rac1,MIG5,ras-related C3 botulinum toxin ...

Human Baculovirus Insect Cells
RAC1 is a GTPase that belongs to the RAS superfamily of small GTP-binding proteins. Members of this superfamily appear to regulate a diverse array of cellular events, including the control of cell growth, cytoskeletal reorganization, and the activation of protein kinases. Two transcript variants encoding different isoforms have been found for RAC1 gene. RAC1 is a plasma membrane-associated small GTPase which cycles between active GTP-bound and inactive GDP-bound states. In its active state, bind...
TMPK-01413 H-2K (b) &B2M&OVA (SIINFEKL) Monomer Protein, Mouse, MHC (His & Avi)

H-2K,OVA,MHC,H2-K1

Mouse HEK293 Cells
Ovalbumin (OVA) has been historically a popular source of such antigens, since OVA can induce both humoral and cellular immune responses based on well-characterised peptide epitopes. The OVA257-264 octapeptide was one of the frst OVA epitopes to be characterised, it has an amino acid sequence SIINFEKL, which is recognised by cytotoxic T lymphocytes. SIINFEKL forms fbrillar assemblies similar to other peptide hydrogels. Te immunoactive properties of this peptide can therefore be related to its se...
TMPK-01534 Chimeric HLA-A*02:01 (mα3) &B2M&LMP2 (CLGGLLTMV) Monomer Protein, Human&Mouse, MHC (His & Avi)

RING12,PSMB9,Proteasome chain 7,RMF,LMP-2,LMP2,M

Human & Mouse HEK293 Cells
The immunoproteasome, having been linked to neurodegenerative diseases and hematological cancers, has been shown to play an important role in MHC class I antigen presentation. The development of molecular probes that selectively inhibit the major catalytic subunit, LMP2, of the immunoproteasome,LMP2-rich cancer cells compared to LMP2-deficient cancer cells are more sensitive to growth inhibition by the LMP2-specific inhibitor, implicating an important role of LMP2 in regulating cell growth of ma...
TMPK-01523 Chimeric HLA-A*02:01 (mα3) &B2M&WT-1 (RMFPNAPYL) Monomer Protein, Human&Mouse, MHC (His & Avi)

WAGR,WT33,AWT1,GUD,RMF,WT1,WIT-2,MHC,NPHS4...

Human & Mouse HEK293 Cells
The WT1 protein plays a role in cell growth, the process by which cells mature to perform specific functions (differentiation), and the self-destruction of cells (apoptosis). WT1 is differentially expressed in serous, endometrioid, clear cell, and mucinous carcinomas of the peritoneum, fallopian tube, ovary, and endometrium.The Human HLA-A*0201 WT-1 (RMFPNAPYL) complex Protein is a complex of HLA-A*0201 of  the MHC Class I, B2M and RMFPNAPYL peptide of  the WT-1.
TMPK-01535 Chimeric HLA-A*02:01 (mα3) &B2M&LMP2 (CLGGLLTMV) Tetramer Protein, Human&Mouse, MHC (His & Avi)

Macropain chain 7,LMP2,Proteasome chain 7,...

Human & Mouse HEK293 Cells
The immunoproteasome, having been linked to neurodegenerative diseases and hematological cancers, has been shown to play an important role in MHC class I antigen presentation. The development of molecular probes that selectively inhibit the major catalytic subunit, LMP2, of the immunoproteasome,LMP2-rich cancer cells compared to LMP2-deficient cancer cells are more sensitive to growth inhibition by the LMP2-specific inhibitor, implicating an important role of LMP2 in regulating cell growth of ma...
TMPK-01522 Chimeric HLA-A*02:01 (mα3) &B2M&WT-1 (RMFPNAPYL) Tetramer Protein, Human&Mouse, MHC (His & Avi)

RMF,WT33,WIT-2,MHC,WAGR,AWT1,GUD,WT1,NPHS4...

Human & Mouse HEK293 Cells
The WT1 protein plays a role in cell growth, the process by which cells mature to perform specific functions (differentiation), and the self-destruction of cells (apoptosis). WT1 is differentially expressed in serous, endometrioid, clear cell, and mucinous carcinomas of the peritoneum, fallopian tube, ovary, and endometrium.The Human HLA-A*0201 WT-1 (RMFPNAPYL) complex Protein is a complex of HLA-A*0201 of  the MHC Class I, B2M and RMFPNAPYL peptide of  the WT-1.

重组蛋白

RAB11B Protein, Human, Recombinant (His)
Cat.No: TMPY-04311
Species: Human
Expression System: HEK293 Cells
HRAS Protein, Human, Recombinant (His)
Cat.No: TMPY-02220
Species: Human
Expression System: Baculovirus Insect Cells
LYPLA2 Protein, Human, Recombinant (His)
Cat.No: TMPY-02132
Species: Human
Expression System: E. coli
Rac1 Protein, Human, Recombinant (GST)
Cat.No: TMPY-01187
Species: Human
Expression System: Baculovirus Insect Cells
H-2K (b) &B2M&OVA (SIINFEKL) Monomer Protein, Mouse, MHC (His & Avi)
Cat.No: TMPK-01413
Species: Mouse
Expression System: HEK293 Cells
Chimeric HLA-A*02:01 (mα3) &B2M&LMP2 (CLGGLLTMV) Monomer Protein, Human&Mouse, MHC (His & Avi)
Cat.No: TMPK-01534
Species: Human & Mouse
Expression System: HEK293 Cells
Chimeric HLA-A*02:01 (mα3) &B2M&WT-1 (RMFPNAPYL) Monomer Protein, Human&Mouse, MHC (His & Avi)
Cat.No: TMPK-01523
Species: Human & Mouse
Expression System: HEK293 Cells
Chimeric HLA-A*02:01 (mα3) &B2M&LMP2 (CLGGLLTMV) Tetramer Protein, Human&Mouse, MHC (His & Avi)
Cat.No: TMPK-01535
Species: Human & Mouse
Expression System: HEK293 Cells
Chimeric HLA-A*02:01 (mα3) &B2M&WT-1 (RMFPNAPYL) Tetramer Protein, Human&Mouse, MHC (His & Avi)
Cat.No: TMPK-01522
Species: Human & Mouse
Expression System: HEK293 Cells
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