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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T63365 RAF-IN-1

RAF-IN-1 是 b/cRAF 的有效抑制剂,能够作用于 cRAF (IC50: 3.8 nM)、bRAFwt (IC50: 36 nM),bRAFV600E (IC50: 29.4 nM),能够抑制携带 bRAFV600E 突变的 A375 和 H358 细胞系,其 GI50分别为 3.4 和 2.9 nM。
T1845 B-Raf IN 1

Raf MAPK
B-Raf IN 1 是选择性B-Raf 抑制剂, IC50为 24 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).
T11224 Rineterkib

ERK-IN-1

ERK; Raf MAPK
Rineterkib (ERK-IN-1) 是口服有效的RAF 和ERK1/2的抑制剂,与 KRAS-突变型非小细胞肺癌、BRAF-突变型非小细胞肺癌、KRAS-突变型胰腺癌、KRAS -突变型结肠癌和 KRAS-突变型卵巢癌尤为相关。
T36642 RAS/RAS-RAF-IN-1

RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity[1]. RAS/RAS-RAF-IN-1 (compound 89; for 4 hours) has an EC50 of 0.5 μμ-5.0 μμ for BRAF-GTP-KRAS-G12C disruption and has an IC50 of 1.0 μμ-10 μμ for pERK inhibition in H358 cells[1]. [1]. Meizhong Jin, et al. Compounds that participate in cooperative binding and uses thereof. WO2020132597A1.
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。
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、9.115 nM。
T24437 MCP110

MCP-110,MCP 110

Raf; Ras GPCR/G Protein; MAPK
MCP110 是 Ras 与 Raf-1 相互作用的抑制剂,可用于治疗人类肿瘤的研究。
T13037 Sulindac sulfide

cis-Sulindac sulfide

Raf; Others; AChR MAPK; Neuroscience; Others
Sulindac sulfide (cis-Sulindac sulfide) 是一种非甾体抗炎化合物,对COX-1具有很高的亲和力,是Ras 激活Raf-1的抑制剂。Sulindac sulfide 是 γ-secretase 的一个非竞争性抑制剂, IC50 为 20.2 μM。它是舒林酸的活性代谢物。
T22341 GSK-114

Others Others
GSK 114 是口服有活性的、高选择性的TNNI3K 抑制剂 (IC50= 25 nM)。其中TNNI3K (又称 CARK) 是酪氨酸样激酶家族的成员,选择性在心脏组织中表达。它对 TNNI3K 的选择性是 B-Raf 激酶的 40 倍 (IC50= 1 µM)。
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。
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。
T60933 B-Raf IN 7

B-Raf IN 7 (compound 6a) 是 B-Raf 的有效抑制剂,IC50值为 110.23 nM。B-Raf IN 7 对结肠癌细胞(HCT-116)、乳腺癌细胞 (MCF-7)、肝癌细胞 (HEPG-2)、人宫颈癌细胞 (Hela) 和人前列腺癌细胞 (PC-3) 具有抗肿瘤活性。其 IC50值分别为 7.50、9.87、10.57、11.63 和 12.83 μM。
T60475 RRD-251

RRD-251 是一种(Rb)-Raf-1相互作用抑制剂,可诱导转移性黑色素瘤细胞凋亡并能与达卡巴嗪协同作用,具有抗增殖、抗血管生成和抗肿瘤活性。
T75110 Trametiglue

Trametiglue 是 Trametinib 的衍生物,通过独特的界面结合相互作用,以前所未有的效力和选择性靶向 KSR-MEK 和 RAF-MEK。
T60727 B-Raf IN 8

B-Raf IN 8 (compound 7g) 是 B-Raf 的有效抑制剂 (IC50 = 70.65 nM)。B-Raf IN 8 显示出抗肿瘤活性,其对肝细胞癌 (HEPG-2)、结肠癌 (HCT-116),乳腺癌 (MCF-7) 和人前列腺癌 (PC-3) 细胞的 IC50值分别为9.78、13.78、18.52 和 29.85 μM。
T36676 Rineterkib hydrochloride

Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1]. ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the C...
T36681 Sorafenib N-oxide

Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibi...
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)。
T35594 Cuspin-1

The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 μM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Ra...
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...

化合物

RAF-IN-1
Cat.No: T63365
Synonym:
Target:
B-Raf IN 1
Cat.No: T1845
Synonym:
Target: Raf
RAF mutant-IN-1
Cat.No: T12685
Synonym:
Target: Others
Rineterkib
Cat.No: T11224
Synonym: ERK-IN-1
Target: ERK, Raf
RAS/RAS-RAF-IN-1
Cat.No: T36642
Synonym:
Target:
C-RAF kinase-IN-1
Cat.No: T72605
Synonym:
Target:
LY3009120
Cat.No: T6882
Synonym: DP-4978
Target: Raf, Autophagy
MCP110
Cat.No: T24437
Synonym: MCP-110,MCP 110
Target: Raf, Ras
Sulindac sulfide
Cat.No: T13037
Synonym: cis-Sulindac sulfide
Target: Raf, Others, AChR
GSK-114
Cat.No: T22341
Synonym:
Target: Others
OSI-930
Cat.No: T2624
Synonym: OSI 930,噻尔非尼
Target: Apoptosis, c-Fms, Raf, VEGFR, FLT, CSF-1R, Src, c-Kit
Raf inhibitor 3
Cat.No: T79813
Synonym:
Target: Raf
B-Raf IN 7
Cat.No: T60933
Synonym:
Target:
RRD-251
Cat.No: T60475
Synonym:
Target:
Trametiglue
Cat.No: T75110
Synonym:
Target:
B-Raf IN 8
Cat.No: T60727
Synonym:
Target:
Rineterkib hydrochloride
Cat.No: T36676
Synonym:
Target:
Sorafenib N-oxide
Cat.No: T36681
Synonym:
Target:
MAPK-IN-2
Cat.No: T79572
Synonym:
Target: EGFR
Cuspin-1
Cat.No: T35594
Synonym:
Target:
Phosphatidylserines (sodium salt)
Cat.No: T35578
Synonym: Phosphatidylserines (sodium salt),L-α-Phosphatidylserine
Target:
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...

天然产物

Phosphatidylserines (bovine)
Cat.No: T35577
Synonym:
Target:
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