製品説明

ターゲット

がんの血管新生

がん細胞は一定のサイズになると局所的に低い酸素濃度の環境が生じます。そこでがん細胞は、自身に酸素が届くよう、血管新生因子を分泌します。これらの因子が血管内皮細胞に発現する受容体に結合することで、血管の基底膜の分解を誘導し、そこから新たな血管が形成され、がん細胞まで伸びていき、酸素・栄養を供給します。

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主要なターゲット例

HIF-1 作用対象：がん細胞

がん細胞が低酸素状態に陥るとHIF-1が活性化し、血管新生因子の分泌を促すことから、がん治療のターゲットとなっています。

VEGFR-2 作用対象：血管内皮細胞

血管内皮細胞には複数の受容体が発現している中、VEGFR-2 は血管新生制御機構で中心的な役割を果たすことが知られており、がん治療のターゲットとなっています。

PDGFR-β 作用対象：ペリサイト

血管内皮細胞から分泌され、PDGFR-β を発現するペリサイトを血管周囲に誘引します。これにより、血管の安定化が促進され、がんの成長にも関わるため治療のターゲットとなっています。

製品ラインアップ

各製品の容量は、オンラインカタログでご確認いただけます。

転写因子

カテゴリー	製品名	作用	メーカー 製品番号	オンライン カタログへ
Hypoxia Inducible Factor (HIF-1)	DMOG	Prolyl hydroxylase inhibitor	4408
	Echinomycin	Highly potent and selective HIF-1α inhibitor	5520
	GN 44028	Potent HIF-1α inhibitor	5655
	KC7F2	HIF-1α inhibitor; down-regulates HIF-1α protein synthesis	4324
	PX 12	Thioredoxin-1 inhibitor	2954
	TC-S 7009	High affinity and selective HIF-2α inhibitor	5243
	Chetomin	Blocks interaction of HIF-1α, HIF-2α and STAT2 with CBP/p300	4705
	Pimonidazole	Hypoxia detection reagent	6182
	SAG	Potent Smoothened receptor agonist; activates the Hedgehog signaling pathway	4366
	Thalidomide	Binds cereblon; also TNF-α synthesis inhibitor	0652
	Lenalidomide	Cereblon binder; induces ubiquitination and degradation of CK1α by E3 ubiquitin ligase	6305
NF-κB	Anacardic acid	Noncompetitive PCAF/p300 inhibitor	3084
	Piceatannol	Inhibits TNF-induced NF-κB activation	1554
	SP 100030	NF-κB and AP-1 dual inhibitor	5309

成長因子

カテゴリー	製品名	作用	メーカー 製品番号	オンライン カタログへ
EGFR	Erlotinib Hydrochloride	Potent, reversible EGFR tyrosine kinase inhibitor	7194
	Iress	Orally active, selective EGFR inhibitor	3000
	Gefitinib-based PROTAC 3	Potent EGFR PROTAC	7258
	MS 39	Potent and selective VHL-recruiting Degrader (PROTAC) of mutant EGFR	7397
	SJF 1521	Selective EGFR PROTAC	7261
FGFR	AZD 4547	Potent and selective FGFR inhibitor	7823
	FIIN 1 hydrochloride	Potent, irreversible FGFR inhibitor	4002
	PD 173074	FGFR1 and -3 inhibitor	3044
	SU 5402	Potent FGFR and VEGFR inhibitor	3300
PDGFR	JNJ 10198409	Potent PDGFα and PDGFRβ inhibitor; also inhibits c-Abl, Lck, c-Src and Fyn kinases	6976
	Linifanib	Potent inhibitor of PDGFRβ, KDR, FLT3 and CSF-1R	7743
	SU 16f	Potent and selective PDGFRβ inhibitor	3304
	SU 6668	PDGFR, VEGFR and FGFR inhibitor	3335
TGF-β	Galunisertib	ALK4 and ALK5 (TGFβRI) inhibitor	6956
	LY 2109761	Selective TGF-β kinase inhibitor	7864
VEGFR	Axitinib	Potent VEGFR-1, -2 and -3 inhibitor	4350
	Cediranib	Potent inhibitor of VEGFR, PDGFR and FGFR	7454
	Ki 8751	Potent, selective VEGFR-2 inhibitor	2542
	Nintedanib	Potent VEGFR, PDGFR and FGFR inhibitor	7049
	SU 5416	VEGFR inhibitor; also inhibits KIT, RET, MET and FLT3	3037
	Sunitinib malate	Potent VEGFR, PDGFRβ and KIT inhibitor	3768
	Tiplaxtinin	Plasminogen activator inhibitor-1 (PAI-1) inhibitor	5565
	Vandetanib	Potent VEGFR-2 inhibitor, also inhibits EGFR and RET oncoproteins activity	7497
	XL 184	Potent VEGFR inhibitor; also inhibits other RTKs	5422

接着 / 細胞外マトリックスリモデリング

カテゴリー	製品名	作用	メーカー 製品番号	オンライン カタログへ
Cell Adhesion Molecule	RGD peptide	Minimal recognition sequence for integrin binding; potent integrin inhibitor	7723
	C26-A6	Disrupts MTDH and SND1 interaction; enhances immune surveillance	7692
	Surfen	Heparin sulfate antagonist	6634
Chemokine CXC Receptor	ATI 2341	CXCR4 allosteric agonist	5795
	SB 332235	Potent CXCR2 antagonist	5671
	AZ 10397767	Potent CXCR2 antagonist	5872
Ephrin	KYL	EphA4 receptor tyrosine kinase inhibitor	5290
Focal Adhesion Kinase	Defactinib	Potent and selective FAK and Pyk2 inhibitor	7305
	PF 573228	Potent and selective FAK inhibitor	3239
	FC 11	Highly potent focal adhesion kinase (FAK) Degrader (PROTAC)	7306
	GSK 215	Potent and selective focal adhesion kinase (FAK) Degrader (PROTAC)	7818
Integrin	BIO 1211	Selective α4β1 (VLA-4) inhibitor	3910
	BIO 5192	Highly potent and selective inhibitor of integrin α4β1 (VLA-4)	5051
	BMS 688521	Potent inhibitor of the LFA-1/ICAM interaction	4970
	BOP	Dual α9β1/α4β1 integrin inhibitor; preferentially mobilizes HSCs	6047
	Cilengitide	Potent and selective inhibitor of integrins αvβ3 and αvβ5	5870
	E 7820	α2 integrin inhibitor; anti-angiogenic	6785
	Echistatin, α1 isoform	αvβ3 and glycoprotein IIb/IIIa (integrin αIIbβ3) inhibitor	3202
	K34c	Potent and selective α5β1 integrin inhibitor	5114
	Obtustatin	Potent and selective α1β1 inhibitor	4664
	ATN 161	α5β1 integrin receptor antagonist	6058
	BOP-JF549	Yellow fluorescent dual α9β1/α4β1 integrin inhibitor comprising BOP conjugated to Janelia Fluor 549; fluorogenic; photostable	6996
	BOP-JF646	Red fluorescent dual α9β1/α4β1 integrin inhibitor comprising BOP conjugated to Janelia Fluor 646; fluorogenic; photostable	6997
	LDV	α4β1 (VLA-4) ligand	7020
	LDV FITC	Fluorescent ligand for α4β1 (VLA-4)	4577
	TCS 2314	α4β1 (VLA-4) antagonist	3900
Matrix Metalloprotease	ARP 101	Inhibitor of MMP-2	2622
	Batimastat	Potent, broad spectrum MMP inhibitor	2961
	CL 82198 hydrochloride	Selective inhibitor of MMP-13	2632
	Doxycycline hyclate	Broad-spectrum MMP inhibitor; tetracycline derivative	4090
	GI 254023X	Selective ADAM10 metalloprotease inhibitor	3995
	GM 6001	Broad spectrum MMP inhibitor	2983
	JNJ 0966	Pro-MMP9 activation inhibitor	6439
	Marimastat	Broad spectrum MMP inhibitor	2631
	UK 383367	Potent and selective BMP-1 (PCP) inhibitor	4188
	WAY 170523	Potent and selective inhibitor of MMP-13	2633

シグナル伝達経路

カテゴリー	製品名	作用	メーカー 製品番号	オンライン カタログへ
Akt (Protein Kinase B)	Akti-1/2	Potent and selective dual Akt1 and 2 inhibitor	5773
	Ceritinib	Highly potent ALK inhibitor; also potently inhibits IR, IGF1R, STK22D and FLT3	6905
	GSK 690693	Akt kinase inhibitor; anti-tumor	4144
	MK 2206 dihydrochloride	Potent and selective allosteric Akt1, Akt2 and Akt3 inhibitor	7850
	Urolithin A	PI 3-K/Akt/mTOR signaling inhibitor; blocks phosphorylation of Akt and p70S6K in vitro	6762
	SC 79	Akt activator	4635
Hedgehog Signaling	AY 9944 dihydrochloride	Inhibitor of Hedgehog (Hh) signaling; inhibits Δ7-dehydrocholesterol reductase	1639
	Cyclopamine	Inhibitor of Hedgehog (Hh) signaling	1623
	GANT 61	GLI antagonist; inhibits Hedgehog (Hh) signaling	3191
	SANT-1	Inhibitor of hedgehog (Hh) signaling; antagonizes smoothened activity	1974
MAP Kinase	AX 15836	Potent and selective ERK5 inhibitor	5843
	Cercosporamide	Potent Mnk2 inhibitor	4500
	FR 180204	Selective ERK inhibitor	3706
	Sorafenib	Potent Raf-1 inhibitor; also inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and cKIT	6814
	TCS ERK 11e	Potent and selective ERK2 inhibitor	4465
MEK	PD 0325901	Potent inhibitor of MEK1/2	4192
	PD 184352	Selective MEK inhibitor	4237
mTOR	Everolimus	mTOR inhibitor; immunosuppressant	6188
	Rapamycin	mTOR inhibitor; immunosuppressant	1292
Other Kinase	CGP 57380	Selective inhibitor of Mnk1	2731
	SGX 523	Selective and potent c-MET kinase inhibitor	5356
Wnt Signaling	DAPT	γ-secretase inhibitor; induces neuronal differentiation; blocks Notch signaling	2634
	endo-IWR 1	Wnt/β-catenin signaling inhibitor; axin stabilizer	3532
	ICG 001	Inhibits TCF/β-catenin-mediated transcription	4505
	iCRT 14	Inhibits β-catenin-responsive transcription (CRT)	4299
	IWP 2	PORCN inhibitor; inhibits Wnt processing and secretion	3533

その他

カテゴリー	製品名	作用	メーカー 製品番号	オンライン カタログへ
Anti-angiogenic	OGT 2115	Anti-angiogenic; heparanase inhibitor	2710
	Tranilast	Antiallergic; inhibits inflammatory mediator release from mast cells	1098

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