Ras

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抑制剂选择性比较

Ras产品

所有产品 Ras抑制剂(24) Ras调节剂(1)

目录号	产品描述	文献引用	实验数据
S1314	Zoledronic Acid Zoledronic acid (ZA), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。	Aging Cell, 2020, 29 Cancers (Basel), 2020, 31;12(1) pii: E104 Mol Cancer Ther, 2020, 19(1):39-51	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
S2797	Lonafarnib Lonafarnib是一种口服生物有效的FPTase抑制剂，作用于H-ras，K-ras-4B和N-ras，无细胞试验中IC50分别为1.9 nM， 5.2 nM和2.8 nM。Phase 3。	Aging Cell, 2020, 29 Dev Biol, 2020, 457(2):215-225 Nat Cell Biol, 2018, 20(7):800-810	Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 是致癌的K-Ras(G12C)的变构抑制剂。
S7684	Salirasib Salirasib是一种有效的竞争性_{prenylated protein methyltransferase (PPMTase)}抑制剂， K_i为2.6 μM，其抑制_Ras甲基化。Phase 2。	Mol Oncol, 2018, 12(2):224-238 Food Chem Toxicol, 2018, 119:464-478 Oncotarget, 2017, 8(30):49824-49838
S8830	AMG510 AMG-510是有效的KRAS G12C共价抑制剂，具有潜在的抗肿瘤活性。该AMG510是手性化合物。
S8916^New	BI-3406 BI-3406 (compound I-6) 是一种有效的、选择性和口服活性的抑制剂，可抑制 KRAS 和 Son of Sevenless 1 (SOS1) 之间的相互作用，其IC50值为6 nM。BI-3406 可减少 GTP-loaded KRAS 的形成，并抑制MAPK信号通路。BI-3406 具有抗肿瘤的活性。
S8959^New	BI-2852 BI-2852 is a potent KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
S0780^New	Oncrasin-1 Oncrasin-1 is a potent and effective inhibitor with anticancer activity. Oncrasin-1 kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. Oncrasin-1 drives abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.
S0023^New	K-Ras-IN-1 K-Ras-IN-1 可通过结合apo-Ras晶体结构中被Tyr-71占据的疏水口袋中的K-Ras来抑制 K-Ras。
S8955^New	AMG-510 racemate AMG-510 racemate 是AMG-510的外消旋体。AMG-510是一种有效的 KRAS G12C 共价抑制剂，具有潜在的抗肿瘤活性。
S8884^New	MRTX849 MRTX849是一种有效的，选择性的和共价的KRAS G12C抑制剂，具有良好的药物样特性，可选择性地修饰GDP结合的KRAS G12C中的突变半胱氨酸12并抑制KRAS依赖性信号传导。
S7224	Deltarasin Deltarasin是一种小分子抑制剂，抑制KRAS-PDEδ相互作用，其结合到纯PDEδ的K_d值为38 nM。	Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y Cell Death Differ, 2019, 26(11):2400-2415 Nat Commun, 2018, 9(1):672
S8826	BAY-293 BAY-293可选择性抑制KRAS-SOS1相互作用，IC50为21 nM。
S7330	6H05 6H05是一个致癌K-Ras(G12C)的选择性、变构抑制剂。
S7331	K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12是致癌K-Ras(G12C)的变构抑制剂。	Oncotarget, 2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
S8303	Kobe0065 Kobe0065是H-Ras-cRaf1相互作用的抑制剂，能有效抑制H-Ras·GTP与c-Raf-1 RBD的结合，Ki值为46±13 μM。	Acta Pharm Sin B, 2019, 9(2):294-303 Cell Death Differ, 2019, 10.1038/s41418-019-0416-4
S7333	K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 是一种变构的，选择性的致瘤性K-Ras(G12C)抑制剂。
S7607	BQU57 BQU57，RBC8的衍生物，是一种相对于GTPases Ras 和 RhoA的选择性GTPase Ral 抑制剂。	PLoS One, 2019, 14(4):e0214764
S8707	ARS-1620 ARS-1620是一种有效的、具有口服活性的KRAS^G12C共价抑制剂，在体内可产生迅速而持续地结合（占用）靶点，诱导肿瘤消退。	J Cell Sci, 2020, 22;jcs.244111 Clin Cancer Res, 2019, 10.1158/1078-0432 Cell Rep, 2019, 29(1):118-134
S6527	Kobe2602 Kobe2602是选择性Ras抑制剂，抑制H-Ras GTP与c-Raf-1结合，Ki值为149 μM。
S5279	Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
S8499	KRpep-2d KRpep-2d是选择性的K-Ras(G12D)抑制性环肽，相较于WT K-Ras和K-Ras(G12C)，对K-Ras(G12D)选择性更高，IC50为1.6 nM。
S8156	ARS-853 (ARS853) ARS-853 是一种具有选择性的KRAS(G12C)共价结合抑制剂，通过结合GDP-肿瘤蛋白并阻止其激活，抑制突变型KRAS所驱动的信号通路。ARS-853 还可诱导凋亡。	Mol Ther Oncolytics, 2019, 14:266-278
S5244	Zoledronic acid monohydrate Zoledronic acid，一种含氮的二磷酸盐，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。	Cancers (Basel), 2020, 31;12(1) pii: E104 J Cell Mol Med, 2020, 25
S0458^New	KY1220 KY1220 通过靶向 Wnt/β-catenin 通路，使得 β-catenin 和 Ras 的稳定性被破坏，其在HEK293 reporter细胞中的IC50值为2.1 μM。
S7444	Pyridostatin Trifluoroacetate Salt Pyridostatin Trifluoroacetate Salt是一种G-quadruplexe稳定剂，无细胞试验中K_d为490 nM，其以一系列原癌基因，包括c-kit，K-ras 和 Bcl-2为靶点。	Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8 Nat Commun, 2020, 27;11(1):2661 Autophagy, 2020, 18

目录号	产品描述	文献引用	实验数据
S1314	Zoledronic Acid Zoledronic acid (ZA), 破骨细胞抑制剂，通过抑制甲羟戊酸途径诱导破骨细胞凋亡，并防止小GTP结合蛋白，如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。	Aging Cell,2020, 29 Cancers (Basel),2020, 31;12(1) pii: E104 Mol Cancer Ther,2020, 19(1):39-51	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
S2797	Lonafarnib Lonafarnib是一种口服生物有效的FPTase抑制剂，作用于H-ras，K-ras-4B和N-ras，无细胞试验中IC50分别为1.9 nM， 5.2 nM和2.8 nM。Phase 3。	Aging Cell,2020, 29 Dev Biol,2020, 457(2):215-225 Nat Cell Biol,2018, 20(7):800-810	Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 是致癌的K-Ras(G12C)的变构抑制剂。
S7684	Salirasib Salirasib是一种有效的竞争性_{prenylated protein methyltransferase (PPMTase)}抑制剂， K_i为2.6 μM，其抑制_Ras甲基化。Phase 2。	Mol Oncol,2018, 12(2):224-238 Food Chem Toxicol,2018, 119:464-478 Oncotarget,2017, 8(30):49824-49838
S8830	AMG510 AMG-510是有效的KRAS G12C共价抑制剂，具有潜在的抗肿瘤活性。该AMG510是手性化合物。
S8916^New	BI-3406 BI-3406 (compound I-6) 是一种有效的、选择性和口服活性的抑制剂，可抑制 KRAS 和 Son of Sevenless 1 (SOS1) 之间的相互作用，其IC50值为6 nM。BI-3406 可减少 GTP-loaded KRAS 的形成，并抑制MAPK信号通路。BI-3406 具有抗肿瘤的活性。
S8959^New	BI-2852 BI-2852 is a potent KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
S0780^New	Oncrasin-1 Oncrasin-1 is a potent and effective inhibitor with anticancer activity. Oncrasin-1 kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. Oncrasin-1 drives abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.
S0023^New	K-Ras-IN-1 K-Ras-IN-1 可通过结合apo-Ras晶体结构中被Tyr-71占据的疏水口袋中的K-Ras来抑制 K-Ras。
S8955^New	AMG-510 racemate AMG-510 racemate 是AMG-510的外消旋体。AMG-510是一种有效的 KRAS G12C 共价抑制剂，具有潜在的抗肿瘤活性。
S8884^New	MRTX849 MRTX849是一种有效的，选择性的和共价的KRAS G12C抑制剂，具有良好的药物样特性，可选择性地修饰GDP结合的KRAS G12C中的突变半胱氨酸12并抑制KRAS依赖性信号传导。
S7224	Deltarasin Deltarasin是一种小分子抑制剂，抑制KRAS-PDEδ相互作用，其结合到纯PDEδ的K_d值为38 nM。	Acta Pharmacol Sin,2019, 10.1038/s41401-019-0268-y Cell Death Differ,2019, 26(11):2400-2415 Nat Commun,2018, 9(1):672
S8826	BAY-293 BAY-293可选择性抑制KRAS-SOS1相互作用，IC50为21 nM。
S7330	6H05 6H05是一个致癌K-Ras(G12C)的选择性、变构抑制剂。
S7331	K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12是致癌K-Ras(G12C)的变构抑制剂。	Oncotarget,2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
S8303	Kobe0065 Kobe0065是H-Ras-cRaf1相互作用的抑制剂，能有效抑制H-Ras·GTP与c-Raf-1 RBD的结合，Ki值为46±13 μM。	Acta Pharm Sin B,2019, 9(2):294-303 Cell Death Differ,2019, 10.1038/s41418-019-0416-4
S7333	K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 是一种变构的，选择性的致瘤性K-Ras(G12C)抑制剂。
S7607	BQU57 BQU57，RBC8的衍生物，是一种相对于GTPases Ras 和 RhoA的选择性GTPase Ral 抑制剂。	PLoS One,2019, 14(4):e0214764
S8707	ARS-1620 ARS-1620是一种有效的、具有口服活性的KRAS^G12C共价抑制剂，在体内可产生迅速而持续地结合（占用）靶点，诱导肿瘤消退。	J Cell Sci,2020, 22;jcs.244111 Clin Cancer Res,2019, 10.1158/1078-0432 Cell Rep,2019, 29(1):118-134
S6527	Kobe2602 Kobe2602是选择性Ras抑制剂，抑制H-Ras GTP与c-Raf-1结合，Ki值为149 μM。
S5279	Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
S8499	KRpep-2d KRpep-2d是选择性的K-Ras(G12D)抑制性环肽，相较于WT K-Ras和K-Ras(G12C)，对K-Ras(G12D)选择性更高，IC50为1.6 nM。
S8156	ARS-853 (ARS853) ARS-853 是一种具有选择性的KRAS(G12C)共价结合抑制剂，通过结合GDP-肿瘤蛋白并阻止其激活，抑制突变型KRAS所驱动的信号通路。ARS-853 还可诱导凋亡。	Mol Ther Oncolytics,2019, 14:266-278
S5244	Zoledronic acid monohydrate Zoledronic acid，一种含氮的二磷酸盐，是有效的破骨细胞抑制剂，可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。	Cancers (Basel),2020, 31;12(1) pii: E104 J Cell Mol Med,2020, 25

目录号	产品描述	文献引用	实验数据
S0458^New	KY1220 KY1220 通过靶向 Wnt/β-catenin 通路，使得 β-catenin 和 Ras 的稳定性被破坏，其在HEK293 reporter细胞中的IC50值为2.1 μM。

目录号

产品描述

文献引用

实验数据

S0458^New

KY1220

KY1220 通过靶向 Wnt/β-catenin 通路，使得 β-catenin 和 Ras 的稳定性被破坏，其在HEK293 reporter细胞中的IC50值为2.1 μM。

目录号	产品描述	文献引用	实验数据
S7444	Pyridostatin Trifluoroacetate Salt Pyridostatin Trifluoroacetate Salt是一种G-quadruplexe稳定剂，无细胞试验中K_d为490 nM，其以一系列原癌基因，包括c-kit，K-ras 和 Bcl-2为靶点。	Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8 Nat Commun, 2020, 27;11(1):2661 Autophagy, 2020, 18

目录号

产品描述

文献引用

实验数据

S7444