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Cat. No. | Product Name | Form | Specificity Of Inhibition |
---|---|---|---|
CL0109 |
Ras inhibitor kit
Ras inhibitor kit |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T41003 |
KG5
|
Raf; FLT; PDGFR; c-Kit | Angiogenesis; MAPK; Tyrosine Kinase/Adaptors |
KG5 是 PDGFRβ 和 B-Raf 的双重变构抑制剂,对 PDGFRβ 和 PDGFRα 的 Kd 分别为 520 nM 和 300 nM。 KG5 抑制 FLT3、KIT 和 c-Raf,具有抗癌和抗血管生成活性。 | |||
T1792 |
Regorafenib
BAY 73-4506,瑞戈非尼,Fluoro-Sorafenib,瑞格非尼 |
Raf; VEGFR; c-RET; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Regorafenib (BAY 73-4506) 是一种多靶点受体酪氨酸激酶抑制剂,抑制 RET、C-RAF、VEGFR2、c-Kit、VEGFR1 和 PDGFRβ (IC50=1.5/2.5/4.2/7/13/22 nM),具有口服活性。Regorafenib 具有抗肿瘤和抗血管生成活性。 | |||
T72605 |
C-RAF kinase-IN-1
|
||
C-RAFkinase-IN-1 是一种有效的C-RAF 激酶抑制剂,IC50为 0.193 μM。C-RAFkinase-IN-1 是一种喹啉衍生物。C-RAFkinase-IN-1 具有研究癌症疾病的潜力。 | |||
T1845 |
B-Raf IN 1
|
Raf | MAPK |
B-Raf IN 1 是选择性B-Raf 抑制剂, IC50为 24 nM。 | |||
T1851 |
ZM 336372
Zinc00581684 |
Apoptosis; Raf | Apoptosis; MAPK |
ZM 336372 是一种选择性蛋白激酶 c-Raf 抑制剂。 | |||
T5634 |
Belvarafenib
|
Raf | MAPK |
Belvarafenib 是一种有效的泛 RAF 抑制剂,具有抗肿瘤活性,对 B-RAF、B-RAFv600E 和 C-RAF 的 IC50值分别为 56、7 和 5 nM。 | |||
T3711 |
RAF709
|
Raf | MAPK |
RAF709 是RAF 抑制剂,抑制BRAF 和CRAF,IC50分别为 0.4 和 0.5 nM,具有抗肿瘤活性。 | |||
T6882 |
LY3009120
DP-4978 |
Raf; Autophagy | Autophagy; MAPK |
LY3009120 (DP-4978) 是一种泛RAF 抑制剂,其抑制BRAFV600E、BRAFWT 和CRAFWT 的IC50分别为 5.8、9.1和15 nM。 | |||
T1903 |
Dabrafenib
GSK2118436A,GSK2118436,达拉非尼 |
Raf | MAPK |
Dabrafenib (GSK2118436A) 是一种 Raf 抑制剂,抑制 C-Raf 和 B-RafV600E (IC50=5/0.6 nM),具有 ATP 竞争性。Dabrafenib 具有抗肿瘤活性,可用于治疗 B-RafV600E 突变的黑色素瘤。 | |||
T2473 |
PLX-4720
PLX4720 |
Raf | MAPK |
PLX-4720 是一种有效且选择性的 B-Raf (V600E) 抑制剂,IC50为 13 nM,与 c-Raf-1(Y340D 和 Y341D 突变)同样有效。 | |||
T6318 |
AZ 628
|
Apoptosis; Raf | Apoptosis; MAPK |
AZ 628 是一种泛Raf 激酶抑制剂,抑制B-Raf、B-RafV600E 和c-Raf-1,IC50分别为 105、34和 29 nM。 | |||
T6296 |
RAF265
CHIR-265 |
Apoptosis; Raf; VEGFR; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
RAF265 (CHIR-265) 是一种 RAF/VEGFR2抑制剂。 | |||
T6348 |
NVP-BHG712
|
Raf; Bcr-Abl; Src; Ephrin Receptor | Angiogenesis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
NVP-BHG712 是一种特异性的 EphB4 抑制剂,ED50=25 nM,可区分 VEGFR 和 EphB4 抑制。它还显示对 c-Raf (IC50:0.395 μM)、c-Src (IC50:1.266 μM) 和 c-Abl (IC50:1.667 μM) 的活性。 | |||
T4167 |
Raf inhibitor 1 dihydrochloride
B-Raf inhibitor 1 dihydrochloride |
Raf | MAPK |
Raf inhibitor 1 dihydrochloride (B-Raf inhibitor 1 dihydrochloride) 是 Raf 激酶抑制剂,对 B-RafWT、B-RafV600E 和 C-Raf 的Ki 分别为 1、1 和 0.3 nM。 | |||
T6525 |
GW 5074
GW5074,3-(3,5-二溴-4-羟基苯亚甲基)-5-碘-1,3-二氢吲哚-2-酮,Raf1 Kinase Inhibitor I |
Apoptosis; Raf | Apoptosis; MAPK |
GW 5074 (Raf1 Kinase Inhibitor I) 是一种有效且特异性的 c-Raf 抑制剂,IC50值为 9 nM。 它对 JNK1/2/3、MEK1、MKK6/7、CDK1/2、c-Src、p38 MAP、VEGFR2 或 c-Fms 的活性没有影响。 | |||
T2074 |
Raf inhibitor 1
B-Raf inhibitor 1 |
Raf | MAPK |
Raf inhibitor 1 (B-Raf inhibitor 1)是Raf 激酶抑制剂,对B-RafWT、B-RafV600E 和 C-Raf 的Ki 分别为 1、1 和 0.3 nM。 | |||
T2382 |
Vemurafenib
RO5185426,RG7204,维罗非尼,PLX4032 |
Raf; MAPK; ACK; Src; Autophagy | Angiogenesis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Vemurafenib (RG7204) 是一种 B-RAF 抑制剂,可以抑制 RAFV600E 和 c-RAF-1 (IC50=31/48 nM),具有选择性和有效性。Vemurafenib 具有抗肿瘤活性,用于 BRAF V600E 突变阳性的黑色素瘤治疗。 | |||
T11898 |
LXH254
|
Raf | MAPK |
LXH254 是B/C RAF 抑制剂。 | |||
T2295 |
SB-590885
|
Raf | MAPK |
SB590885 是一种 B-Raf 抑制剂,Ki 值为 0.16 nM,对其选择性是对 c-Raf 的 11 倍多。 | |||
T8474 |
Dabrafenib Mesylate
达帕菲尼甲磺酸盐,甲磺酸达拉非尼,GSK 2118436B,GSK2118436 Mesylate |
Raf | MAPK |
Dabrafenib Mesylate (GSK2118436 Mesylate) 是一种ATP 竞争型Raf 抑制剂,抑制C-Raf 和B-RafV600E 的IC50分别为 5 和 0.6 nM。 | |||
T6320 |
GDC-0879
GDC 0879,AR-00341677,GDC0879 |
Raf | MAPK |
GDC-0879 (AR-00341677) 是一种选择性B-Raf 抑制剂,IC50为 0.13 nM。 | |||
T0093L |
Sorafenib
索拉非尼,Bay 43-9006 |
Apoptosis; Raf; VEGFR; FLT; Ferroptosis; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Sorafenib (Bay 43-9006) 是一种多激酶抑制剂,抑制 Raf-1、B-Raf、VEGFR2、VEGFR3、VEGFR4、PDGFRβ、FLT3、c-Kit 等 (IC50=6/22/90/15/20/20/57/58 nM),具有口服活性。Sorafenib 具有抗肿瘤活性,可以诱导细胞自噬和凋亡,也可以激动铁死亡。 | |||
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。 | |||
T0093 |
Sorafenib tosylate
甲苯磺酸索拉非尼,Bay 43-9006 |
Apoptosis; Raf; VEGFR; FLT; Ferroptosis; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Sorafenib tosylate (Bay 43-9006) 是一种口服活性Raf 抑制剂,也是铁死亡激动剂。它是多激酶抑制剂,对VEGFR2,VEGFR3,PDGFRβ,FLT3和c-Kit 的IC50分别为 90 nM,15 nM,20 nM,57 nM 和 58 nM。它诱导细胞自噬和凋亡,有抗肿瘤活性。 | |||
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。 | |||
T2293 |
SGX-523
|
Raf; p38 MAPK; c-Met/HGFR; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
SGX523 是选择性的和 ATP 竞争性的MET 抑制剂 (IC50:4 nM)。它对 MET 的选择性其它他蛋白激酶高 1000 倍。它具有抗肿瘤特性。 | |||
T6277 |
Doramapimod
BIRB 796,达马莫德,度马莫德 |
Raf; p38 MAPK; Autophagy | Autophagy; MAPK |
Doramapimod (BIRB 796) 是一种具有口服活性的p38 MAPK 抑制剂,Kd 值为0.1nM。它也抑制B-Raf 和 Abl,IC50分别为 83 nM 和 14.6 μM。 | |||
T2617 |
SNS-314 Mesylate
SNS-314 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
SNS-314 Mesylate (SNS-314) 是一种有效且特异性的极光激酶抑制剂,对极光激酶 A、B、C 的 IC50值分别为 9,31 和 3 nM。 | |||
T2624 |
OSI-930
OSI 930,噻尔非尼 |
Apoptosis; c-Fms; Raf; VEGFR; FLT; CSF-1R; Src; c-Kit | Angiogenesis; Apoptosis; MAPK; Tyrosine Kinase/Adaptors |
OSI-930 是 Kit,KDR 和 CSF-1R (c-Fms)的口服选择性抑制剂,IC50分别为 80 nM,9 nM 和 15 nM。它具有抗肿瘤活性,靶向肿瘤中的癌细胞增殖和血管生成。它还适度抑制 Flt-1,c-Raf 和 Lck,并且对 PDGFRα/β,Flt-3和 Abl 具有较弱的抑制活性。 | |||
TQ0048 |
BI-882370
|
Raf | MAPK |
BI-882370 是高选择性的RAF 激酶抑制剂,其结合位于 BRAF 激酶的 DFG-out 无活性构象处 (ATP 结合位点)。 它抑制 SRC 家族激酶,也抑制 BRAFV600E-mutant、WT BRAF 和 CRAF 激酶,IC50值分别为 0.4、0.8 和 0.6 nM。 | |||
T12685 |
RAF mutant-IN-1
|
Others | Others |
RAF mutant-IN-1 is an inhibitor of RAF kinase(IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAFV600E and B-RAFWT, respectively). | |||
T1886 |
TAK-632
|
Raf; FGFR; PDGFR; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; Tyrosine Kinase/Adaptors |
TAK632 是一种有效的pan-RAF 抑制剂,对CRAF、BRAFV600E 和BRAFWT 的IC50分别为 1.4、2.4 和 8.3 nM。 | |||
T79813 |
Raf inhibitor 3
|
Raf | MAPK |
Raf inhibitor3 (Example 30) 作为一种Raf抑制剂,对B-Raf和C-Raf展现出高效抑制作用,其IC50值均小于15 nM,主要应用于癌症研究领域。 | |||
T64194 | Belvarafenib TFA | ||
Belvarafenib TFA (HM95573 TFA) 是一种有效的、广泛的迅速加速纤维肉瘤激酶(RAF)的抑制剂,能够作用于 B-RAF (IC50: 56 nM)、B-RAFv600E (IC50: 7 nM) 和 C-RAF (IC50: 5 nM)。 | |||
T3641 |
NVP-BAW2881
BAW2881 |
Raf; VEGFR; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; MAPK; Tyrosine Kinase/Adaptors |
NVP-BAW2881 (BAW2881) 是一种选择性的 VEGFR2抑制剂,其 IC50=9 nM。 | |||
T5172 |
AZ304
|
c-Fms; Raf; p38 MAPK; Autophagy | Autophagy; MAPK; Tyrosine Kinase/Adaptors |
AZ304 是一种 ATP 竞争性双 BRAF 激酶抑制剂,有效抑制 BRAF (WT)、BRAF (V600E) 和野生型 CRAF,IC50值分别为79、38和68 nM。具有抗肿瘤活性。它对 p38 和 CSF1R 也有抑制作用,IC50值分别为 6 nM 和 35 nM。 | |||
T79572 |
MAPK-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MAPK-IN-2 (化合物3h)是一种携带抗肿瘤活性的高效MAPK抑制剂。它在多个癌细胞系中有效抑制了细胞增殖,并对MAPK途径表现出强大的抑制效果(EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, CDK4/6 IC50=95和184 nM),对突变型EGFR和B-RAF亦展现出高效力(EGFRT790M IC50=69 nM, B-RAFV600E IC50=83 nM)。 | |||
T10157 |
Regorafénib N-oxyde (M2)
瑞戈非尼杂质 13 |
Raf; VEGFR; c-RET; PDGFR; c-Kit; Drug Metabolite | Angiogenesis; Apoptosis; MAPK; Metabolism; Tyrosine Kinase/Adaptors |
Regorafénib N-oxyde M2 是 Regorafenib 的活性代谢物。Regorafenib 是多靶点抑制剂,包括VEGFR1/2/3,PDGFRβ,Kit,RET 和 Raf-1 , IC50分别是 13/4.2/46,22,7,1.5 和 2.5 nM。 | |||
T35578 |
Phosphatidylserines (sodium salt)
Phosphatidylserines (sodium salt),L-α-Phosphatidylserine |
||
Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum (ER) and can be reversibly converted back by the same enzymes. It can also be irre... | |||
T14928 |
Agerafenib hydrochloride
RXDX-105 hydrochloride,CEP-32496 (hydrochloride) |
c-RET; c-Kit | Apoptosis; Tyrosine Kinase/Adaptors |
Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM). |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T35577 |
Phosphatidylserines (bovine)
|
||
Phosphatidylserine is a naturally occurring phospholipid that comprises 2-10% of total phospholipids in mammals and is enriched in the central nervous system, particularly the retina. It is anionic and found mainly on the inner leaflet of the cell membrane. It is biosynthesized from phosphatidylcholine or phosphatidylethanolamine by phosphatidyl synthase 1 (PSS1) or PSS2, respectively, in the endoplasmic reticulum and can be reversibly converted back by the same enzymes. It can also be irreversi... |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-05095 |
RAF1 Protein, Human, Recombinant (His & GST)
Raf-1 proto-oncogene, serine/threonine kin... |
Human | Baculovirus Insect Cells |
RAF1 gene is the cellular homolog of viral raf gene (v-raf). The encoded protein is a MAP kinase kinase kinase (MAP3K), which functions downstream of the Ras family of membrane associated GTPases to which it binds directly. Once activated, the cellular RAF1 protein can phosphorylate to activate the dual specificity protein kinases MEK1 and MEK2, which in turn phosphorylate to activate the serine/threonine specific protein kinases, ERK1 and ERK2. Activated ERKs are pleiotropic effectors of cell p... | |||
TMPY-04411 |
YES1 Protein, Human, Recombinant (His & GST)
HsT441,c-yes,YES proto-oncogene 1, Src... |
Human | Baculovirus Insect Cells |
Proto-oncogene tyrosine-protein kinase Yes, also known as Proto-oncogene c-Yes, p61-Yes and YES1, is a cytoplasm protein that belongs to the protein kinase superfamily, Tyr protein kinase family and SRC subfamily. YES1 / c-Yes contains one protein kinase domain, one SH2 domain and one SH3 domain. It is thought that the subcellular distribution of Src-family tyrosine kinases, including c-Yes binding to the cellular membrane, is membranous and/or cytoplasmic. YES1 / c-Yes protein tyrosine kinase i... | |||
TMPK-01450 |
HLA-C*03:04&B2M&KRAS G12D (GADGVGKSAL) Monomer Protein, Human, MHC (His & Avi), Biotinylated
KRAS1,MHC,K-RAS4B,KRAS,CFC2,K-RAS... |
Human | HEK293 Cells |
Kirsten rat sarcoma 2 viral oncogene homolog (KRAS) is the most commonly mutated oncogene in human cancer. The developments of many cancers depend on sustained expression and signaling of KRAS, which makes KRAS a high-priority therapeutic target. The virtual screening approach to discover novel KRAS inhibitors and synthetic lethality interactors of KRAS are discussed in detail. | |||
TMPK-01456 |
HLA-C*03:04&B2M&KRAS G12D (GADGVGKSAL) Tetramer Protein, Human, MHC (His & Avi)
KRAS2,NS,MHC,C-K-RAS,KRAS1,K-RAS2A,K-RAS2B... |
Human | HEK293 Cells |
Kirsten rat sarcoma 2 viral oncogene homolog (KRAS) is the most commonly mutated oncogene in human cancer. The developments of many cancers depend on sustained expression and signaling of KRAS, which makes KRAS a high-priority therapeutic target. The virtual screening approach to discover novel KRAS inhibitors and synthetic lethality interactors of KRAS are discussed in detail. | |||
TMPK-01451 |
HLA-C 03:04&B2M&KRAS G12D (GADGVGKSAL) Monomer Protein, Human, MHC (His & Avi)
NS3,K-RAS4A,K-Ras 2,NS,KRAS1,RASK2,MHC,KI-RAS,KRAS,... |
Human | HEK293 Cells |
Kirsten rat sarcoma 2 viral oncogene homolog (KRAS) is the most commonly mutated oncogene in human cancer. The developments of many cancers depend on sustained expression and signaling of KRAS, which makes KRAS a high-priority therapeutic target. The virtual screening approach to discover novel KRAS inhibitors and synthetic lethality interactors of KRAS are discussed in detail. |