Ras
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1314 | Zoledronic Acid | <1 mg/mL | 0.004 mg/mL | ''<1 mg/mL |
| S2797 | Lonafarnib | <1 mg/mL | 127 mg/mL | '127 mg/mL |
| S7332 | K-Ras(G12C) inhibitor 9 | <1 mg/mL | 53 mg/mL | '<1 mg/mL |
| S7684 | Salirasib | ' mg/mL | ||
| S8830 | AMG510 | <1 mg/mL | 100 mg/mL | ''100 mg/mL |
| S8916 | BI-3406 | <1 mg/mL | 92 mg/mL | ''''92 mg/mL |
| S8959 | BI-2852 | ' mg/mL | ||
| S0780 | Oncrasin-1 | ' mg/mL | ||
| S0023 | K-Ras-IN-1 | <1 mg/mL | 41 mg/mL | '''''41 mg/mL |
| S8955 | AMG-510 racemate | ' mg/mL | ||
| S8884 | MRTX849 | <1 mg/mL | 100 mg/mL | '50 mg/mL |
| S6527 | Kobe2602 | <1 mg/mL | 84 mg/mL | '40 mg/mL |
| S7224 | Deltarasin | <1 mg/mL | 100 mg/mL | '100 mg/mL |
| S8826 | BAY-293 | <1 mg/mL | 90 mg/mL | '90 mg/mL |
| S7330 | 6H05 | 100 mg/mL | 100 mg/mL | '100 mg/mL |
| S7331 | K-Ras(G12C) inhibitor 12 | <1 mg/mL | 27 mg/mL | '<1 mg/mL |
| S8303 | Kobe0065 | <1 mg/mL | 89 mg/mL | '13 mg/mL |
| S7333 | K-Ras(G12C) inhibitor 6 | <1 mg/mL | 81 mg/mL | '30 mg/mL |
| S7607 | BQU57 | <1 mg/mL | 66 mg/mL | '20 mg/mL |
| S8707 | ARS-1620 | <1 mg/mL | 86 mg/mL | '60 mg/mL |
| S5279 | Fendiline hydrochloride | -1 mg/mL | 70 mg/mL | '-1 mg/mL |
| S8499 | KRpep-2d | 100 mg/mL | -1 mg/mL | '-1 mg/mL |
| S8156 | ARS-853 (ARS853) | <1 mg/mL | 86 mg/mL | '''1 mg/mL |
| S5244 | Zoledronic acid monohydrate | <1 mg/mL | 0.01 mg/mL | ''<1 mg/mL |
| S0458 | KY1220 | <1 mg/mL | 63 mg/mL | ''''<1 mg/mL |
| S7444 | Pyridostatin Trifluoroacetate Salt | 100 mg/mL | 100 mg/mL | '30 mg/mL |
Ras製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1314 |
Zoledronic AcidZoledronic acid (ZA), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. |
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 |
LonafarnibLonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3. |
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 9K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
||
| S7684 |
SalirasibSalirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Phase 2. |
||
| S8830 |
AMG510AMG-510 is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. |
||
| S8916新 |
BI-3406BI-3406 is a potent, orally active and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling with anticancer activities. |
||
| S8959新 |
BI-2852BI-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新 |
Oncrasin-1Oncrasin-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新 |
K-Ras-IN-1K-Ras-IN-1 inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. |
||
| S8955新 |
AMG-510 racemateAMG-510 racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. |
||
| S8884新 |
MRTX849MRTX849 is a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C and inhibits KRAS-dependent signaling. |
||
| S6527新 |
Kobe2602Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM). |
||
| S7224 |
DeltarasinDeltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
||
| S8826 |
BAY-293BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM. |
||
| S7330 |
6H056H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C). |
||
| S7331 |
K-Ras(G12C) inhibitor 12K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
-inhibitor-12-S733101W0420171213.gif)
-inhibitor-12-S733101W0420171213.gif)
(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 |
Kobe0065Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. |
||
| S7333 |
K-Ras(G12C) inhibitor 6K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). |
||
| S7607 |
BQU57BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA. |
||
| S8707 |
ARS-1620ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression. |
||
| S5279 |
Fendiline hydrochlorideFendiline 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-2dKRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM. |
||
| S8156 |
ARS-853 (ARS853)ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis. |
||
| S5244 |
Zoledronic acid monohydrateZoledronic acid, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. |
||
| S0458新 |
KY1220KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells. |
||
| S7444 |
Pyridostatin Trifluoroacetate SaltPyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes including c-kit, K-ras and Bcl-2. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1314 |
Zoledronic AcidZoledronic acid (ZA), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. |
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 |
LonafarnibLonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3. |
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 9K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
||
| S7684 |
SalirasibSalirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Phase 2. |
||
| S8830 |
AMG510AMG-510 is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. |
||
| S8916新 |
BI-3406BI-3406 is a potent, orally active and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling with anticancer activities. |
||
| S8959新 |
BI-2852BI-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新 |
Oncrasin-1Oncrasin-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新 |
K-Ras-IN-1K-Ras-IN-1 inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. |
||
| S8955新 |
AMG-510 racemateAMG-510 racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. |
||
| S8884新 |
MRTX849MRTX849 is a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C and inhibits KRAS-dependent signaling. |
||
| S6527新 |
Kobe2602Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM). |
||
| S7224 |
DeltarasinDeltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
||
| S8826 |
BAY-293BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM. |
||
| S7330 |
6H056H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C). |
||
| S7331 |
K-Ras(G12C) inhibitor 12K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
-inhibitor-12-S733101W0420171213.gif)
-inhibitor-12-S733101W0420171213.gif)
(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 |
Kobe0065Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. |
||
| S7333 |
K-Ras(G12C) inhibitor 6K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). |
||
| S7607 |
BQU57BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA. |
||
| S8707 |
ARS-1620ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression. |
||
| S5279 |
Fendiline hydrochlorideFendiline 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-2dKRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM. |
||
| S8156 |
ARS-853 (ARS853)ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis. |
||
| S5244 |
Zoledronic acid monohydrateZoledronic acid, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S0458新 |
KY1220KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S7444 |
Pyridostatin Trifluoroacetate SaltPyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes including c-kit, K-ras and Bcl-2. |
2020, 22 pii: S1097-2765(20)30231-8 2020, 27;11(1):2661 2020, 18 |
