Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11738 |
K-Ras G12C-IN-4
|
Ras | GPCR/G Protein; MAPK |
K-Ras G12C-IN-4 是一种 KRAS G12C 共价抑制剂。 | |||
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。 | |||
T6556 |
K-Ras(G12C) inhibitor 9
|
Raf | MAPK |
K-Ras(G12C) inhibitor 9 是致癌 K-Ras(G12C) 的变构抑制剂。 | |||
T3725 |
K-Ras(G12C) Inhibitor 6
|
Raf | MAPK |
KRas(G12C) inhibitor 6 是一种变构的,选择性的 K-Ras(G12C)抑制剂。 | |||
T6555 |
K-Ras(G12C) inhibitor 12
|
Apoptosis; Raf; Ras | Apoptosis; GPCR/G Protein; MAPK |
K-Ras(G12C) inhibitor 12是一种K-Ras(G12C)抑制剂,作用于H1792细胞,EC50为0.32 μM。 | |||
T8659 |
K-Ras-PDEδ-IN-1
|
PDE | Metabolism |
K-Ras-PDEδ-IN-1 是新型的 K-Ras-PDEδ 抑制剂,它能够以低纳摩尔Kd8 nM 与 PDEδ 的法尼基结合袋竞争性结合。 | |||
T13844 |
PROTAC K-Ras Degrader-1
|
Ras | GPCR/G Protein; MAPK |
PROTAC K-Ras Degrader-1 is potent degrader of K-Ras based PROTAC. | |||
T11735 |
K-Ras G12C-IN-1
|
Phosphatase | Metabolism |
K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C. | |||
T11737 |
K-Ras G12C-IN-3
|
Others | Others |
Heterocyclic compounds as covalent inhibitors of G12C mutant K-Ras protein useful for treating cancers.K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C. | |||
T11736 |
K-Ras G12C-IN-2
|
Others | Others |
K-Ras G12C-IN-2 is a covalent kras g12c inhibitor. | |||
T18057 |
K-Ras ligand-Linker Conjugate 4
|
Others | Others |
K-Ras ligand-Linker Conjugate 4 is a chemical compound that combines a ligand for K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The compound has the potential to be used in the synthesis of PROTAC K-Ras Degrader-1, a powerful degrader of K-Ras that has been shown to exhibit a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T18056 |
K-Ras ligand-Linker Conjugate 3
|
Others | Others |
K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound that consists of a ligand for K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential in the synthesis of PROTAC K-Ras Degrader-1, a potent PROTAC K-Ras degrader that demonstrates a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T18055 |
K-Ras ligand-Linker Conjugate 2
|
Others | Others |
K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker. This compound is capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC K-Ras Degrader-1, which is a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T18059 |
K-Ras ligand-Linker Conjugate 6
|
Others | Others |
K-Ras ligand-Linker Conjugate 6 is a chemical compound that combines a ligand for K-Ras recruiting moiety and a PROTAC linker. This compound can recruit E3 ligases, including VHL, CRBN, MDM2, and IAP. K-Ras ligand-Linker Conjugate 6 is particularly useful in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1]. | |||
T18058 |
K-Ras ligand-Linker Conjugate 5
|
Others | Others |
K-Ras ligand-Linker Conjugate 5 is a chemical compound that combines a ligand for the K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The K-Ras ligand-Linker Conjugate 5 plays a crucial role in the synthesis of PROTAC K-Ras Degrader-1, a highly potent K-Ras degrader. In SW1573 cells, this degrader exhibits an impressive degradation efficacy of ≥70% [1]. | |||
T18054 | K-Ras ligand-Linker Conjugate 1 | Others | Others |
K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1]. | |||
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。 | |||
T1931 |
6H05
K-Ras inhibitor |
Raf; Ras | GPCR/G Protein; MAPK |
6H05 (K-Ras inhibitor) 是致癌突变体 K-Ras(G12C) 的选择性变构抑制剂。 | |||
T7326 |
6H05 (TFA)
6H05 TFA,6H05 trifluoroacetate |
Ras | GPCR/G Protein; MAPK |
6H05 TFA (6H05 trifluoroacetate) 是一种选择性变构致癌突变体 K-Ras(G12C) 抑制剂。 | |||
TP2358 |
KRPEP-2D acetate
|
Raf | MAPK |
KRPEP-2D acetate 被鉴定为针对 K-Ras 的 G12D 突变体的 K-Ras(G12D) 选择性抑制肽,K-Ras 是 Ras 蛋白家族的关键成员和有吸引力的癌症治疗靶点。 | |||
T10375 |
ARS-1323
|
Ras | GPCR/G Protein; MAPK |
ARS-1323 是 ARS-1620 的消旋体。ARS-1323 是突变型K-Ras G12C 的新型抑制剂。 | |||
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。 | |||
T10376 |
ARS-1630
|
Ras | GPCR/G Protein; MAPK |
ARS-1630 是一种突变型 K-ras G12C 抑制剂。 它是 ARS-1620 的活性较低的对映异构体。 | |||
T8006 |
Oncrasin-1
1-(4-氯苄基)-1H-吲哚-3-甲醛 |
Apoptosis; Raf; Ras | Apoptosis; GPCR/G Protein; MAPK |
Oncrasin 1 是一种有效的抗癌抑制剂,可在低或亚微摩尔浓度下杀死具有 K-Ras 突变的各种人类肺癌细胞。 | |||
T7414 |
ARS-853
|
Apoptosis; Raf; Ras | Apoptosis; GPCR/G Protein; MAPK |
ARS-853 是一种选择性共价KRAS G12C 抑制剂,IC50为 2.5 μM。它通过与 GDP 结合的癌蛋白结合并阻止激活来抑制突变 KRAS 驱动的信号传导。 | |||
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。 | |||
T4470 |
Pyridostatin TFA
|
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Pyridostatin TFA 是一种 G-四链体稳定剂,靶向原癌基因 Src,降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。它通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。 | |||
T76215L |
KRpep-2d TFA
|
||
KRpep-2d (TFA) 是一种有效的K-Ras 抑制剂,抑制K-Ras 驱动的癌细胞增殖。KRpep-2d (TFA) 可用于癌症研究。 | |||
T76215 |
KRpep-2d
|
||
KRpep-2d 是一种有效的 K-Ras 抑制剂,抑制 K-Ras 驱动的癌细胞增殖。KRpep-2d 可用于癌症研究。 | |||
T63758 |
G12Si-1
|
||
G12Si-1 是选择性的、共价的 K-Ras(G12S) 抑制剂,能抑制 K-Ras(G12S) 致癌信号的传导。在突变的丝氨酸残基上,G12Si-1能够良好的结合 K-Ras(G12S)。G12Si-1 也可能够阻碍 Sos 催化的交换,并抑制 EDTA 促进的交换速率,进而影响 K-Ras 的核苷酸循环。 | |||
T18853 |
Tos-PEG4-THP
|
Others | Others |
Tos-PEG4-THP is a polyethylene glycol (PEG) derivative utilized as a linker in the synthesis of PROTAC K-Ras Degrader-1, a potential therapeutic compound for targeted degradation of K-Ras protein [1]. | |||
T69710 | LB42908 | ||
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. | |||
T70476 | SML-10-70-1 | ||
SML-10-70-1 is a Novel Active Site Inhibitor of Oncogenic K-Ras G12C. | |||
T71037 | BAY-438 | ||
BAY-438 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model. | |||
T62675 |
FTI-277
|
||
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。 | |||
T18847 | THP-PEG4-Pyrrolidine(N-Me)-CH2OH | Others | Others |
THP-PEG4-Pyrrolidine(N-Me)-CH2OH, a PEG-based PROTAC linker, facilitates the synthesis of PROTAC K-Ras Degrader-1[1]. | |||
T36391 | Spiro-Oxanthromicin A | ||
Spiro-oxanthromicin A is a polyketide that has been found inStreptomyces.1It induces mislocalization of K-RAS in MDCK cells (IC50= 26.7 μM). 1.Salim, A.A., Xiao, X., Cho, K.J., et al.Rare Streptomyces sp. polyketides as modulators of K-Ras localisationOrg. Biomol. Chem.12(27)4872-4878(2014) | |||
T15113 |
Diazepinomicin
TLN-4601,BU 4664L,ECO-4601 |
Others | Others |
Diazepinomicin is a secondary metabolite produced by Micromonospora sp. It inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. Diazepinomicin also is an anti-tumor agent for K-Ras mutant models. | |||
T70133 |
BAY-846
|
||
BAY-846 is an allosteric MEK inhibitor with long half-lives, high bioavailabilities, low brain penetration potential and high efficacy in a K-Ras-mutated A549 xenograft model. | |||
T41212 |
FTI 277
|
||
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. | |||
T72707 |
(Rac)-Lonafarnib
Sch66336 racemate |
||
(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。 | |||
T82108 | ICMT-IN-35 | ||
ICMT-IN-35(即compound 10n),作为FTPA-triazole类ICMT抑制剂(IC50=0.8 μM),能被哺乳动物细胞吸收并阻断K-Ras膜定位,进而诱导K-Ras错定位。ICMT-IN-35对ICMT+/+MEF细胞表现出选择性细胞毒性,对转移性胰腺癌细胞系展示低微摩尔级别活性(IC50=0.8 μM)。 | |||
T82136 |
ICMT-IN-1
|
||
ICMT-IN-1 (化合物75) 作为一种高效的ICMT抑制剂展现出显著活性(IC50=0.0013 μM),能够剂量依赖性地在HCT-116细胞中导致ICMT的胞质内积累,进而有效抑制携带K-Ras和N-Ras变异的多个癌细胞系的增殖。 | |||
T18846 |
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH
|
Others | Others |
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a polyethylene glycol (PEG) based PROteolysis TArgeting Chimera (PROTAC) linker, employed for the synthesis of PROTAC K-Ras Degrader-1, as documented in reference [1]. | |||
T82086 |
ICMT-IN-7
|
||
ICMT-IN-7(化合物74)是一种高效的ICMT抑制剂,其IC50值为0.015 μM。该化合物能剂量依赖性地在HCT-116细胞中诱导ICMT蛋白在胞质的积累,并能抑制表达K-Ras和N-Ras的多种癌细胞系的增殖。 | |||
T74973 | KRas G12R inhibitor 1 | ||
KRas G12R inhibitor 1 (compound 3) 是一种 KRas G12R 选择性共价抑制剂,可以利用突变半胱氨酸的强亲核性,在 K-Ras 的 Switch II 区域不可逆结合。KRas G12R inhibitor 1 可用于癌症研究。 | |||
T74920 | G12Si-2 | ||
G12Si-2,一种 G12Si-1 的类似物,可作为阴性对照。G12Si-2 不是 KRAS G12S 突变体的共价抑制剂。 | |||
T73822 | GGTI-286 TFA | ||
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。 | |||
T79464 |
RORγ antagonist 1
|
ROR | Metabolism |
RORγ antagonist1 (化合物22) 作为RORγ的有效拮抗剂 (KD=0.18 μM),在HPAF-II胰腺癌异种移植模型中显示出了抗增殖性能。该化合物通过抑制RAS/MAPK和AKT/mTORC1通路,并引发caspase依赖的细胞凋亡(apoptosis)机制,从而在胰腺癌细胞中发挥作用。 |