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Cytoskeleton——Integrin

Integrins, a family of heterodimeric adhesion receptors for diverse extracellular matrices, have consistently been implicated as crucial drivers of ovarian cancer development and progression. A number of the RGD-based members of the integrin family, including α5β1, and αvβ3 or αvβ5 integrins, are markedly elevated in aggressive ovarian tumors. These adhesion receptors appear to promote cell adhesion, survival, motility and invasion during ovarian tumor growth or metastatic progression. Importantly, the functions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signaling, including the PI3K/Akt- and Ras/MAPK-dependent pathways.

Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion. Modulation of these molecules, particularly αv integrin family, has exhibited profound effects on fibrosis in multiple organ and disease state. Based on the several studies, the integrins αvβ3, αvβ5, αvβ6, and αvβ8 have been known to modulate the fibrotic process via activation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis.

Each integrin is typically formed by the non-covalent pairing of one α subunit, of which, 18 types are known to exist, and one β subunit, of which 8 types are known to exist. Together, 24 distinct heterodimers have been identified to date. The αv subunit can form heterodimers with the β1, β3, β5, β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11, and αv, indicating that not all theoretically possible α and subunit pairs form. Interestingly, the activation of TGF-β appears to be a common function of multiple αv integrins.

Cytoskeleton——Integrin(66)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM3268 A-205804

A-205804 是抑制 E-selectinICAM-1 表达的口服有效的,高效、选择性的先导抑制剂,对 E-selectin 和 ICAM-1 作用的 IC50 分别为 20 nM 和 25 nM。A-205804 可用于慢性炎症疾病的研究。

251992-66-2 98%
KM9452 A-286982

A-286982 是一种有效的变构 LFA-1/ICAM-1 相互作用抑制剂,在 LFA-1/ICAM-1 结合和 LFA-1 介导的细胞粘附试验中,IC50 分别为 44 nM 和 35 nM。

280749-17-9 99%
KM7363 Arg-Gly-Asp-Ser

Arg-Gly-Asp-Ser 是整联蛋白结合序列,抑制整联蛋白受体 (integrin receptor) 功能。Arg-Gly-Asp-Ser 直接并特异性地结合 pro-caspase-8,pro-caspase-9 和 pro-caspase-3,但不与 pro-caspase-1 结合。

91037-65-9 99%
KM4125 ATN-161 trifluoroacetate salt

ATN-161 trifluoroacetate salt 是一种新型 integrin α5β1 拮抗剂,在肝转移模型小鼠模型中,抑制血管生成。

904763-27-5 ≥95%
KE9797 Bimosiamose disodium 187269-60-9 ≥95%
KM8700 BIO-1211

BIO-1211 是高度选择性的、具有口服活性的 α4β1 (VLA-4) 抑制剂,其对 α4β1 和 α4β7 的 IC50 值分别为 4 nM 和 2 μM。

187735-94-0 99%
KM9427 BIO5192 hydrate

BIO5192 hydrate 是一种选择性强的整合素 α4β1 (VLA-4) 抑制剂 (Kd<10 pM)。BIO5192 hydrate 选择性地与 α4β1 (IC50=1.8 nM) 结合,选择性高过其他一系列整合素。BIO5192 hydrate 导致小鼠造血干细胞和祖细胞 (HSPCs) 的动员比基础水平增加 30 倍。

≥98%
KM8579 BMS-587101

BMS-587101 是一种有效的具有口服活性的 leukocyte function associated antigen-1 (LFA-1) 拮抗剂。BMS-587101 具有抗炎作用,可用于类风湿关节炎的研究。

509083-77-6 98%
KM6799 BMS-688521

BMS-688521 是一种高效、具有口服活性的 LFA-1/ICAM 相互作用抑制剂,在粘附试验中 IC50 为 2.5 nM,在 MLR 试验中 IC50 为 60 nM。BMS-688521 对小鼠变应性嗜酸性肺炎模型有较好的研究作用。

893397-44-9 98%
KM8674 c(phg-isoDGR-(NMe)k)

c(phg-isoDGR-(NMe)k) 是有效选择性的 α5β1 整合素 配体,IC50 为 2.9 nM。

1844830-65-4
KM6511 c(phg-isoDGR-(NMe)k) TFA

c(phg-isoDGR-(NMe)k) TFA 是有效选择性的 α5β1 整合素配体,IC50 为 2.9 nM。

KM7879 Carotegrast

Carotegrast是一种口服的 α4整合素受体抑制剂,具有抗炎活性。

401904-75-4 98%
KM7687 Carotegrast methyl

Carotegrast methyl (AJM300) 是一种口服有效和选择性 α4 整联蛋白 (α4 integrin) 拮抗剂。HCA2969 是 Carotegrast methyl 的活性代谢产物,是一种特异的双重 α4β1/α4β7 整联蛋白拮抗剂。Carotegrast methyl 可预防小鼠结肠炎。

401905-67-7 99%
KM11580 Cilengitide

Cilengitide (EMD 121974) 是一种有效的选择性整合素 ανβ3ανβ5 抑制剂。Cilengitide 抑制 ανβ3 和 ανβ5 与玻连蛋白结合,IC50 值分别为 4 和 79 nM。

188968-51-6 99%
KM9816 Cilengitide TFA

Cilengitide 是有效的,选择性的 αvβ3 和 αvβ5 受体整合素抑制剂,IC50 分别为 4 nM 和 79 nM。

199807-35-7 98%
KM14686 Cucurbitacin B

葫芦素B (Cucurbitacin B)是一具有抗癌活性的天然化合物。

6199-67-3 99%
KM18191 CWHM-12

CWHM-12是αV整联蛋白的有效抑制剂,抑制αvβ8αvβ3αvβ6αvβ1IC50 值分别为0.2,0.8,1.5,1.8 nM。

1564286-55-0 98%
KM12974 Cyclo(-RGDfK)

Cyclo(-RGDfK) 是有效,选择性的整合素 αvβ3 抑制剂,其 IC50 值为 0.94 nM。Cyclo(-RGDfK) TFA 通过与细胞表面的 αvβ3 整合素结合,特异性靶向肿瘤微血管和癌细胞。

161552-03-0 ≥98%
KM14032 Cyclo(-RGDfK) TFA

Cyclo(-RGDfK) TFA 是有效,选择性的整合素 αvβ3 抑制剂,其 IC50 值为 0.94 nM。Cyclo(-RGDfK) TFA 通过与细胞表面的 αvβ3 整合素结合,特异性靶向肿瘤微血管和癌细胞。

500577-51-5 99%
KM17952 Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA

Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) 是整合蛋白 αvβ3 的抑制剂,具有抗肿瘤活性。

199807-33-5 99%
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