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抑制剂 & 化合物

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T10520	BET-IN-2	Epigenetic Reader Domain	Chromatin/Epigenetic
	BET-IN-2 is a BET inhibitor (IC50: 52 nM for BRD4-BD1).
T3504	AZD5153 6-Hydroxy-2-naphthoic acid AZD5153,AZD5153结晶体(API形式),AZD-5153 HNT salt	Epigenetic Reader Domain	Chromatin/Epigenetic
	AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) 是 AZD5153的6-羟基-2-萘甲酸盐形式。AZD5153是一种有口服活性的选择性 BET/BRD4溴结构域抑制剂，对BRD4的IC50值为1.7nM。
T13671	(S,R,S)-AHPC-Me hydrochloride VHL ligand 2 hydrochloride,E3 ligase Ligand 1	Others; Ligand for E3 Ligase	Others; PROTAC
	(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is a chemical compound utilized in the synthesis of ARV-771, an exceptionally potent BET protein degrader. This compound selectively degrades BET protein in cells resistant to castration, exhibiting a remarkable DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, (S,R,S)-AHPC-Me hydrochloride serves as the VHL ligand derived from (S,R,S)-AHPC for the recruitment of von Hippel-Lindau (VHL) protein.
T19618	(R)-(-)-JQ1 Enantiomer (R)-(-)2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂环庚烷-6-基)乙酸叔丁酯	Epigenetic Reader Domain	Chromatin/Epigenetic
	(R)-(-)-JQ1 Enantiomer 是 (+)-JQ1 的立体异构体。 (+)-JQ1 是一种 BET 溴结构域抑制剂，对BRD4(1/2)的IC50 为 77 和 33 nM。
T10773	CF53	Epigenetic Reader Domain; CDK	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	CF53 是一种高效、选择性、可口服的 BET 抑制剂，对 BRD4 BD1 的 Ki 值为 <1 nM，Kd 值为 2.2 nM，IC50 值为 2 nM；CF53 对 BRD2，BRD3，BRD4 和 BRDT BET 蛋白的 BD1 和 BD2 两个结构域都有高亲和性，对其选择性远高于非含溴结构域 BET 蛋白。CF53 在体外和体内都具有显著的抗肿瘤活性。
T7752	(S,R,S)-AHPC-Me VHL ligand 2,E3 ligase Ligand 1A	Ligand for E3 Ligase	PROTAC
	(S,R,S)-AHPC-Me (E3 ligase Ligand 1A) 是基于 (S,R,S)-AHPC 的的 VHL 配体，可用于募集 von Hippel-Lindau (VHL) 蛋白。它可有效降解去势抵抗性前列腺癌细胞中的 BET 蛋白，DC50<1 nM。它可用于合成 ARV-771。
T74753	JQ1-TCO
	JQ1-TCO (JQ1-trans-cycloctene) 是一种 BET 抑制剂 JQ1 的衍生物。JQ1-TCO 适用于点击化学，可作为体外和体内的分子探针。
T13671L	(S,R,S)-AHPC-Me dihydrochloride VHL ligand 2 dihydrochloride,E3 ligase Ligand 1 dihydrochloride,(S,R,S)-AHPC-Me dihydrochloride (1948273-02-6 free base)	Others	Others
	(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound utilized in the synthesis of ARV-771. ARV-771, a BET PROTAC degrader relying on von Hippel-Landau (VHL) E3 ligase, demonstrates potent degradation of BET protein in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound serves as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, that facilitates the recruitment of von Hippel-Lindau (VHL) prote...
T36103	TW9 TW9
	TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistica...

化合物

BET-IN-2

Cat.No: T10520

Synonym:

Target: Epigenetic Reader Domain

AZD5153 6-Hydroxy-2-naphthoic acid

Cat.No: T3504

Synonym: AZD5153,AZD5153结晶体(API形式),AZD-5153 HNT salt

Target: Epigenetic Reader Domain

(S,R,S)-AHPC-Me hydrochloride

Cat.No: T13671

Synonym: VHL ligand 2 hydrochloride,E3 ligase Ligand 1

Target: Others, Ligand for E3 Ligase

(R)-(-)-JQ1 Enantiomer

Cat.No: T19618

Synonym: (R)-(-)2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂环庚烷-6-基)乙酸叔丁酯

Target: Epigenetic Reader Domain

CF53

Cat.No: T10773

Synonym:

Target: Epigenetic Reader Domain, CDK

(S,R,S)-AHPC-Me

Cat.No: T7752

Synonym: VHL ligand 2,E3 ligase Ligand 1A

Target: Ligand for E3 Ligase

(S,R,S)-AHPC-Me dihydrochloride

Cat.No: T13671L

Synonym: VHL ligand 2 dihydrochloride,E3 ligase Ligand 1 dihydrochloride,(S,R,S)-AHPC-Me dihydrochloride (1948273-02-6 free base)

Cat. No.	Product Name	Target	Signaling Pathways
T5681	ETHYL CAFFEATE 咖啡酸乙酯,ETHYL 3,4-DIHYDROXYCINNAMATE	NF-κB; COX; PGE Synthase; NO Synthase	Immunology/Inflammation; Neuroscience; NF-κB
	Ethyl Caffeate (ETHYL 3,4-DIHYDROXYCINNAMATE) 是从鬼针草分离的一种酚类天然产物，在体外或在小鼠皮肤中抑制NF-κB 活化及其下游炎症介质的诱导型一氧化氮合酶、环氧合酶 2 和前列腺素 E2。
T3824	Jaceosidin	Apoptosis; BCL; COX; UGT	Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience
	Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物，可激活Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。它能够降低炎性因子水平，激活 NF-κB，抑制COX-2的表达，具有抗癌和抗炎作用。

天然产物

ETHYL CAFFEATE

Cat.No: T5681

Synonym: 咖啡酸乙酯,ETHYL 3,4-DIHYDROXYCINNAMATE

Target: NF-κB, COX, PGE Synthase, NO Synthase

Jaceosidin

Cat.No: T3824

Synonym:

Target: Apoptosis, BCL, COX, UGT

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