Ras(Ras蛋白)

Cat.No. 产品名称 Information

GC60533 6H05 (TFA) An allosteric inhibitor of oncogenic K-Ras(G12C)

GC39763 Z62954982

ZINC08010136

Z62954982 (ZINC08010136) 是一种强效的、选择性的、细胞渗透性强的 Rac1 (IC50=12 μM) 抑制剂，比 NSC23766 (IC50=50 μM) 有效性强 4 倍。Z62954982 干扰 Rac1/Tiam1 复合物，降低活性 Rac1 (GTP 结合的 Rac1) 的细胞质水平，而不影响其他 Rho GTPases (如，Cdc42 或 RhoA) 的活性。

GC50609 SAH-SOS1A SAH-SOS1A 是一种基于肽的 SOS1/KRAS 蛋白相互作用抑制剂。 SAH-SOS1A 以纳摩尔级亲和力 (EC50=106-175 nM) 与野生型和突变型 KRAS（G12D、G12V、G12C、G12S 和 Q61H）结合，直接且独立地阻断核苷酸结合，削弱 KRAS 驱动的癌细胞活力，并通过机制阻断 KRAS 下游的 ERK-MAPK 磷酸信号级联发挥其作用。

GC38942 PROTAC K-Ras Degrader-1 PROTAC K-Ras Degrader-1 是一种基于 PROTAC 技术的有效的 K-Ras 降解剂，在 SW1573 中对其降解率为 ≥70%。

GC38898 CCG-222740 CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression.

GC38400 MRTX849

(2S)-4-[7-(8-氯-1-萘)-5,6,7,8-四氢-2-[[((2S)-1-甲基-2-吡咯烷基]甲氧基]吡啶基[3,4-d]嘧啶-4-基]-1-(2-氟-1-氧代-2-丙烯-1-基)-2-哌嗪乙腈,MRTX849

A covalent inhibitor of K-Ras^G12C

GC37973 ZT-12-037-01 ZT-12-037-01 is a specific and ATP-competitive STK19 inhibitor with IC50s of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively. It displays extremely high kinase selectivity using KINOMEscan against a panel of 468 diverse kinases using an in vitro ATP-site competition binding assay at 1 μM.

GC36901 PHT-7.3 PHT-7.3 是一种选择性的 Ras 激酶抑制因子连接增强蛋白 1 (Cnk1) PH 结构域的抑制剂，抑制突变型 KRas，但不抑制野生型 KRas 癌细胞和肿瘤的生长和信号传导。

GC36599 Methylophiopogonanone B

甲基麦冬黄烷酮B

An isoflavone with diverse biological activities

GC36400 K-Ras G12C-IN-3 K-Ras G12C-IN-3是突变型K-Ras G12C不可逆小分子抑制剂。

GC36399 K-Ras G12C-IN-2 K-Ras G12C-IN-2 是一种不可逆的 K-Ras G12C 抑制剂。

GC36398 K-Ras G12C-IN-1 K-Ras G12C-IN-1是突变型K-Ras G12C不可逆小分子抑制剂。

GC36397 KRAS G12C inhibitor 13 KRAS G12C inhibitor 13 是一种有效的选择性 KRAS G12C 抑制剂，详细信息请参考专利文献 WO2018143315A1 中的化合物 30。

GC36134 GGTI298 A geranylgeranyltransferase I inhibitor

GC35859 Diazepinomicin

ECO-4601; TLN-4601; BU 4664L

Diazepinomicin (TLN-4601) 是Micromonospora sp 的次生代谢产物，可抑制EGF 诱导的 Ras-ERK MAPK 信号通路，可诱导凋亡。是一种可用于 K-Ras 突变型的抗肿瘤药物。

GC35513 BI-2852 BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.

GC35361 Antineoplaston A10

3-苯基乙酰氨基-2,6-哌啶二酮

Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.

GC19546 AMG-510 racemate

AMG-510(消旋体),AMG-510 racemate

A covalent inhibitor of K-Ras^G12C

GC19541 (rac)-Antineoplaston A10

3-苯基乙酰氨基-2,6-哌啶二酮

(rac)-Antineoplaston A10 是 Antineoplaston A10 的外消旋体。 Antineoplaston A10 是一种潜在的 Ras 抑制剂，可用于治疗神经胶质瘤、淋巴瘤、星形细胞瘤和乳腺癌。

GC34427 6H05 trifluoroacetate (K-Ras inhibitor) 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).

GC34198 KRas G12C inhibitor 1 KRasG12Cinhibitor1是KRasG12C的抑制剂，来自专利US20180072723A1。

GC34196 KRas G12C inhibitor 3 KRasG12Cinhibitor3是KRasG12C的抑制剂，来自专利US20180072723A1。

GC34192 KRas G12C inhibitor 4 KRasG12Cinhibitor1是KRasG12C的抑制剂，来自专利US20180072723A1。

GC34188 KRas G12C inhibitor 2 KRasG12Cinhibitor2是KRasG12C的抑制剂，来自专利US20180072723A1。

GC34162 KRAS G12C inhibitor 5 KRASG12Cinhibitor5是一种KRasG12C抑制剂，详细信息请参考专利文献WO2017201161A1中的化合物147。

GC34114 ARS-1323 ARS-1323是突变型K-RasG12C的新型抑制剂，来自专利WO2015054572A1。

GC34091 ARS-1630 ARS-1630是突变型K-RasG12C的新型抑制剂，来自专利WO2015054572A1。

GC34088 Y16 Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM).

GC34055 ARS-1620 A covalent inhibitor of K-RAS^G12C

GC33340 BDP9066 BDP9066是肌强直性肌营养不良相关Cdc-42结合激酶MRCK的选择性有效抑制剂，其在SCC12细胞中测得对MRCKβ的IC50值为64nM，对MRCKα/β的Ki值分别为0.0136nM和0.0233nM。BDP9066通过降低底物磷酸化来治疗皮肤癌。

GC33186 BAY-293

(R)-6,7-二甲氧基-2-甲基-N-(1-(4-(2-((甲基氨基)甲基)苯基)噻吩-2-基)乙基)喹唑啉-4-胺

An inhibitor of the K-Ras-SOS1 protein-protein interaction

GC33167 Rhosin An inhibitor of the Rho-GEF protein-protein interaction

GC33153 K-Ras-IN-1 K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.

GC32970 MBQ-167

MBQ-167是Ras相关的C3型肉毒素底物(Rac)和细胞分裂周期蛋白(Cdc42)的双抑制剂，其对Rac1/2/3的IC50值为103nM，对Cdc42的IC50值为78nM。

GC32770 1A-116 1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer, prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes.

GC32729 Rhosin hydrochloride

G04

An inhibitor of the Rho-GEF protein-protein interaction

GC32716 Pan-RAS-IN-1 Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.