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Search Results for " covalently "

91

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13858	RA190	Proteasome	Proteases/Proteasome; Ubiquitination
	RA190 能够与泛素受体 RPN13 的半胱氨酸 88 共价结合，并抑制蛋白酶体功能。
T18889	5-Aminofluorescein 5-氨基荧光素,5-AF	Others	Others
	5-Aminofluorescein (5-AF) (5-AF) is a covalently-bound fluorescence marker conjugated with human serum albumin. It exhibits an excitation wavelength of 490 nm and an emission wavelength of 515 nm.
T19947	EDC hydrochloride EDC-HCl Crosslinker,1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride	Others	Others
	EDC hydrochloride (EDC-HCl Crosslinker) 是一种零长度交联剂。 EDC hydrochloride 非常适合将蛋白质或肽共价结合到含羧基的珠子、树脂或其他纳米颗粒上。
T16732	Reproxalap NS-2,ADX-102	Others	Others
	Reproxalap (NS-2) 是一种活性醛类隔离剂，可用于干眼症的研究。它能够与醛 (包括丙二醛和 4-羟基壬醛) 共价结合。
T7541	PTP inhibitor 1 PTP Inhibitor II,alpha-溴-4-甲氧基苯乙酮	Phosphatase	Metabolism
	PTP inhibitor 1 是蛋白酪氨酸磷酸酶 (PTP) 抑制剂，具有抗血管生成作用。
T13586L	BPK-29 hydrochloride	Others	Others
	BPK-29 hydrochloride 是特殊配体，能够共价修饰 C274 ，破坏非典型孤核受体NR0B1与RBM45、SNW1蛋白质的相互作用。它能够损害KEAP1突变癌细胞的锚定独立生长。
T38960	QL-X-138	Virus Protease; MNK; BTK	Angiogenesis; MAPK; Microbiology/Virology; Tyrosine Kinase/Adaptors
	QL-X-138 是一种强效的选择性 BTK和 MNK 双激酶抑制剂，与 BTK 具有共价结合，与 MNK 具有非共价结合。QL-X-138 对 BTK、MNK1 和 MNK2 激酶的 IC 50 s 分别为 9.4 nM、107.4 nM 和 26 nM。QL-X-138 对登革病毒 2 具有抑制作用，其 IC 50 为 3.5 μM。QL-X-138 可用于 B 细胞恶性肿瘤的研究。
T10460	Batabulin 巴他布林,T138067	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Batabulin (T138067) 是一种抗肿瘤剂，可与 β-微管蛋白同种型的子集共价且选择性地结合，从而破坏微管聚合。它影响细胞形态并导致细胞周期停滞，最终诱导细胞凋亡。
T77762	ROS-generating agent 1	Apoptosis; Ferroptosis; ROS Kinase	Apoptosis; Tyrosine Kinase/Adaptors
	ROS-generating agent 1 具有抗癌活性,通过共价修饰 TrxR 的 Sec-498 残基以生成 ROS。ROS-generating agent 1 降低细胞内 TrxR 蛋白水平，促进 NCI-H460 细胞中 ROS 依赖的性细胞凋亡 (apoptosis) 和铁死亡 (ferroptosis)。
T5674	H-151	STING	Immunology/Inflammation
	H-151 是一种 STING 拮抗剂，具有高效性和选择性。H-151 与 STING 的 Cys91 共价结合，抑制 Cys91 的棕榈酰化，从而抑制 STING 的活性。H-151 可用于体内外自身炎症性疾病的研究。
T3215	JNJ-42165279 JNJ42165279	FAAH; Autophagy	Autophagy; Metabolism; Neuroscience
	JNJ-42165279 是一种 FAAH 抑制剂，抑制 hFAAH 和 rFAAH，IC50分别为70 ± 8 nM 和 313 ± 28 nM。它对其他酶、离子通道、转运蛋白和受体具有高度选择性。
T7084	2-Bromo-4'-hydroxyacetophenone SHP-1 Inhibitor II,PTP Inhibitor I,α-Bromo-4-hydroxyacetophenone,4-Hydroxyphenacyl bromide,2-溴-4'-羟基苯乙酮	Phosphatase	Metabolism
	2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) 是一种PTP1B 的有效抑制剂，其Ki=42 μM。
TQ0236	Tirabrutinib ONO-4059,GS-4059,Velexbru	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	Tirabrutinib (GS-4059) (ONO-4059) 是一种口服有效的高选择性 Bruton’s Tyrosine Kinase (BTK) 抑制剂 (能透过血脑屏障)，其 IC50 值为 6.8 nM。Tirabrutinib 不可逆共价结合 BTK 并抑制异常 B 细胞受体信号传导。Tirabrutinib 可用于自身免疫性疾病和血液学恶性肿瘤的研究。
T6446	Clevudine L-FMAU,克拉夫定,Levovir	HBV; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	Clevudine (Levovir) 是一种非自然 L-构型的核苷类似物，是一种与聚合酶结合的非竞争性抑制剂，具有较强的抗 HBV 活性，半衰期长，毒性低的特点。
T0668	1-Aminohydantoin hydrochloride	Others	Others
	1-Aminohydantoin hydrochloride 是一种呋喃妥因在动物组织中的主要代谢物。它与组织蛋白共价结合，在微酸性条件下从组织中释放出来，与 2-硝基苯甲醛衍生形成 AHD 的硝基苯基衍生物可被检测。它可作为测定肉、奶等兽药残留的测定指标。
T21320	Methoxyamine HCl 甲氧基胺盐酸盐,TRC102,TRC 102,Methoxyamine,TRC-102	Others	Others
	Methoxyamine HCl (Methoxyamine) 与脱嘌呤/脱嘧啶 (AP) DNA 损伤位点共价结合并抑制碱基切除修复 (BER)，这可能导致 DNA 链断裂和细胞凋亡增加。 Methoxyamine 是一种具有潜在佐剂活性的口服生物可利用的小分子抑制剂。该药剂可增强烷化剂的抗肿瘤活性。
T36256	LC-2 LC 2,PROTAC KRASG12C Degrader-LC-2,LC2	PROTACs	PROTAC
	LC-2 (PROTAC KRASG12C Degrader-LC-2) 是一种新型基于von Hippel-Lindau的内源性 KRAS G12C 的 PROTAC 降解剂，DC50 在 0.25 和 0.76 μM 之间。LC-2 是一种与 MRTX849 共价结合 KRAS G12C 并招募 E3 连接酶 VH的 PROTAC，诱导 KRAS G12C 快速持续降解。LC-2 对纯合和杂合子 KRAS G12C 细胞系 MAPK 信号有抑制作用。
T21687	Conoidin A	Parasite	Microbiology/Virology
	Conoidin A 是刚地弓形虫过氧化物酶 II 的细胞通透性抑制剂，有杀线虫特性。它共价结合 TgPrxII 的过氧化物催化位点 Cys47，不可逆地抑制其过氧化物活性，IC50为 23 µM。它也抑制哺乳动物 PrxI 和 PrxII 的氧化。它具有抗氧化、神经保护作用，可研究缺血性心脏病。
T11191	EN6	Proton pump; Autophagy	Autophagy; Membrane transporter/Ion channel
	EN6 是一种小分子体内自噬激活剂，其共价靶向溶酶体v-ATP 酶的 ATP6V1A 亚基中的半胱氨酸 277。它以溶酶体依赖性方式清除 TDP-43 聚集体，这是额颞叶痴呆的病原体。它介导的 ATP6V1A 修饰使 v-ATP 酶与 Rags 分离，从而抑制 mTORC1 信号传导、增加溶酶体酸化和激活自噬。
T38960L	QL-X-138 HCl QL-X-138 HCl（1469988-63-3 Free base）	MNK; BTK	Angiogenesis; MAPK; Tyrosine Kinase/Adaptors
	QL-X-138 HCl 是一种新型具有选择性和高效性的 BTK/MNK 双激酶抑制剂，具有抗癌活性，可与 BTK 共价结合，与 MNK 非共价结合。QL-X-138 HCl 对 BTK、MNK1 和 MNK2 激酶有抑制作用。QL-X-138 HCl 具有抗登革热病毒 2 活性，在急性髓系白血病细胞中显示抗增殖活性。QL-X-138 HCl 可用于研究淋巴瘤和白血病。
T3024	Avitinib AC0010,艾维替尼	EGFR; JAK; BTK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Avitinib (AC0010) 是一种不可逆的、突变体选择性的EGFR 抑制剂，可有效抑制非小细胞肺癌中EGFR T790M 耐药突变。阿比替尼也是一种新型BTK 抑制剂。
T27391	FSBA
	FSBA inhibits covalently anthrax edema factor.
T35061	Vinthionine L-Vinthionine,S-Ethenyl-L-homocysteine
	Vinthionine binds covalently to rat liver DNA, RNA, and protein in vivo, but not in vitro.
T29596	Acetylaminofluorene-dG dG-8-AAF,8-AAF dG,8 AAF-dG,8-AAF-dG
	Acetylaminofluorene-dG is a carcinogenic adduct which covalently binds DNA bases and promotes mutagenesis near the adduct site.
T15626	JPM-OEt	Others	Others
	JPM-OEt is a broad spectrum cysteine cathepsin inhibitor with antitumor activity. JPM-OEt binds covalently in the active site and irreversibly inhibits the cysteine cathepsin family.
T27766	Hymeglusin L659,699,L 659,699,L-659,699
	L-659,699, also known as hymeglusin, is a fungal β-lactone antibiotic that inhibits HMG-CoA synthase (IC50 = 0.12 μM) by covalently modifying the active Cys129 residue of the enzyme.
T28389	PF-6422899 PF6422899,PF 6422899
	PF-6422899 irreversibly inhibits EGFR kinase activity by binding covalently to active-site cysteine residues in the ATP binding pocket of EGFR.
T11956L	MBC-11	Others	Others
	MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). It also has the potential to treat tumor-induced bone disease (TIBD).
TP2303	ZIP, Biotinylated	Others	Others
	ZIP with a biotin moiety covalently attached
T13586	BPK-29	Others	Others
	BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein interactions by covalently modifying C274. It impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
T17060	Tetramethylrhodamine-5-iodoacetamide 5-TMRIA	Others	Others
	Tetramethylrhodamine-5-iodoacetamide (5-TMRIA) is a thiol-selective reactive dye that is used to non-specifically label proteins via the cysteine residues and covalently label DNA fragments[1].
T33957	PF-Alkyne PF Alkyne
	PF-Alkyne is a fluorophosphonate-based probe which specifically and covalently reacts with the tyrosine-111 residue of the Schistosoma japonicum GST (sjGST) tag. PF-Alkyne rapidly and site-selectively immobilizes sjGST fusion proteins.
T21318	Efaproxiral RSR13,Efaproxyn,RSR 13,RSR-13
	Efaproxiral is a synthetic small molecule with radiosensitizing activity. Efaproxiral increases oxygen levels in hypoxic tumor tissues by binding non-covalently to the hemoglobin tetramer and decreasing hemoglobin-oxygen binding affinity, increasing tumor
T41056	Phalloidin-TRITC
	Phalloidin-TRITC is a TRITC labeled, red fluorescence probe for F-actin . Phalloidin, bound to actin filaments, reacts covalently with amino acids Glu-llT, Met-ll9, and Met355, which are very close to the nucleotide binding site.
T30461	BI-RJ 70 BI RJ 70,BIRJ70,BI-RJ-70
	BI-RJ 70 is a tritiated photoaffinity azide analog of nevirapine, which can be used to study the binding of nevirapine to HIV-1 transcriptase through covalently labeled enzymes and amino acid residues.
T73006	cis-ccc_R08
	cis-ccc_R08（化合物1）为黄酮衍生物，适用于乙型肝炎病毒（HBV）感染研究，作为cccDNA（共价封闭环状DNA）的抑制剂。
T27200	DOX−NOP1 HCl doxorubicin-NOP1 conjugate,doxorubicin-NOP1 HCl,DOX−NOP1 Hydrochloride
	DOX−NOP1 is a molecular hybrid covalently joining doxorubicin (DOX) and NOP1. DOX−NOP1 showed similar increased toxicity toward resistant cancer cells and, in addition, lower cardiotoxicity than DOX.
T16568	PR-924	Proteasome	Proteases/Proteasome; Ubiquitination
	PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.
T16327	Nitracrine	Others	Others
	Nitracrine is a 1-nitroacridine derivative and is an effective hypoxia-selective agent in vitro and antitumor drugs. Nitracrine suppresses RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine h
T11956	MBC-11 triethylamine	Others	Others
	MBC-11 triethylamine has potential to treat tumor-induced bone disease (TIBD), is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC).
T11957	MBC-11 trisodium	Others	Others
	MBC-11 trisodium has potential to treat tumor-induced bone disease (TIBD).It is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C.
T70403	VUF14480
	VUF14480 is a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor. VUF14480 was shown to be a partial agonist of hH4 receptor-mediated G protein signalling and β-arrestin2 recruitment. VUF14480 bound covalently to the hH₄ receptor with submicromolar affinity. Serine substitution of C98(3.36) prevented this covalent interaction.
T75139	TMX1
	TMX1 是一种 BRD4共价分子胶降解剂。TMX1 选择性地将 DCAF16 招募到 BRD4BD2 上，导致 BRD4的降解。
T62534	POP-IN-2
	POP-IN-2 (Compound 7k) 是一种有效的、共价结合的 prolyl oligopeptidase (POP) 抑制剂 (Ki: 6 nM)。POP-IN-2 能够用于神经退行性疾病和癌症的研究。
T73282	HBV-IN-31
	HBV-IN-31 是一种有效的共价闭合环状 DNA (cccDNA) 抑制剂。HBV-IN-31 具有抗HBV 活性，对 HBsAg 的 IC50值为 0.13 µM。HBV-IN-31 抑制细胞生长。
T63704	FGFR4-IN-11
	FGFR4-IN-11 是选择性的、有效的、共价结合的 FGFR4 抑制剂 (IC50: 2.1 nM)。FGFR4-IN-11 能够明显抑制 FGF19/FGFR4 信号通路，表现出抗癌效果。
TP1837	Acyl Carrier Protein (ACP) (65-74) Acyl Carrier Protein (ACP) 65-74
	Acyl Carrier Protein (ACP) (65-74) is an active acyl carrier protein (ACP) fragment.Acyl Carrier Protein (ACP) is a component of plastid-located plant fatty acid synthetase. It binds acyl groups covalently via the prosthetic group, 4-phosphopantetheine, d
T72328	Cyclopropenone probe 1
	Cyclopropenone probe 1 可以通过在催化活性位点共价结合，特异且有效地修饰三阴性乳腺癌驱动因子 GSTP1。
T74026	AUTAC2
	AUTAC2 是一种 FKBP12靶向自噬介导降解体 (AUTAC)。AUTAC2 包含一个 FBnG 和 SLF 部分，其中 SLF 与 FKBP12 非共价结合。
T63340	CCG-273220
	CCG-273220 是 G 蛋白偶联受体 (GPCR) 激酶 5 (GRK5) 共价抑制剂 (IC50: 220 nM)。CCG-273220 可以共价结合GRK5亚家族特异性残基 Cys474 ，而对GRK5的选择性比 GRK2 高。

化合物

Cat.No: T13858

Target: Proteasome

5-Aminofluorescein

Cat.No: T18889

Synonym: 5-氨基荧光素,5-AF

Target: Others

EDC hydrochloride

Cat.No: T19947

Synonym: EDC-HCl Crosslinker,1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride

Target: Others

Cat.No: T16732

Synonym: NS-2,ADX-102

Target: Others

PTP inhibitor 1

Cat.No: T7541

Synonym: PTP Inhibitor II,alpha-溴-4-甲氧基苯乙酮

Target: Phosphatase

BPK-29 hydrochloride

Cat.No: T13586L

Target: Others

Cat.No: T38960

Target: Virus Protease, MNK, BTK

Cat.No: T10460

Synonym: 巴他布林,T138067

Target: Apoptosis, Microtubule Associated

ROS-generating agent 1

Cat.No: T77762

Target: Apoptosis, Ferroptosis, ROS Kinase

Cat.No: T5674

Target: STING

Cat.No: T3215

Synonym: JNJ42165279

Target: FAAH, Autophagy

2-Bromo-4'-hydroxyacetophenone

Cat.No: T7084

Synonym: SHP-1 Inhibitor II,PTP Inhibitor I,α-Bromo-4-hydroxyacetophenone,4-Hydroxyphenacyl bromide,2-溴-4'-羟基苯乙酮

Target: Phosphatase

Cat.No: TQ0236

Synonym: ONO-4059,GS-4059,Velexbru

Target: BTK

Cat.No: T6446

Synonym: L-FMAU,克拉夫定,Levovir

Target: HBV, DNA/RNA Synthesis

1-Aminohydantoin hydrochloride

Cat.No: T0668

Target: Others

Methoxyamine HCl

Cat.No: T21320

Synonym: 甲氧基胺盐酸盐,TRC102,TRC 102,Methoxyamine,TRC-102

Target: Others

Cat.No: T36256

Synonym: LC 2,PROTAC KRASG12C Degrader-LC-2,LC2

Target: PROTACs

Cat.No: T21687

Target: Parasite

Cat.No: T11191

Target: Proton pump, Autophagy

Cat.No: T38960L

Synonym: QL-X-138 HCl（1469988-63-3 Free base）

Target: MNK, BTK

Cat.No: T3024

Synonym: AC0010,艾维替尼

Target: EGFR, JAK, BTK

Cat.No: T27391

Cat.No: T35061

Synonym: L-Vinthionine,S-Ethenyl-L-homocysteine

Acetylaminofluorene-dG

Cat.No: T29596

Synonym: dG-8-AAF,8-AAF dG,8 AAF-dG,8-AAF-dG

Cat.No: T15626

Target: Others

Cat.No: T27766

Synonym: L659,699,L 659,699,L-659,699

Cat.No: T28389

Synonym: PF6422899,PF 6422899

Cat.No: T11956L

Target: Others

ZIP, Biotinylated

Cat.No: TP2303

Target: Others

Cat.No: T13586

Target: Others

Tetramethylrhodamine-5-iodoacetamide

Cat.No: T17060

Synonym: 5-TMRIA

Target: Others

Cat.No: T33957

Synonym: PF Alkyne

Cat.No: T21318

Synonym: RSR13,Efaproxyn,RSR 13,RSR-13

Phalloidin-TRITC

Cat.No: T41056

Cat.No: T30461

Synonym: BI RJ 70,BIRJ70,BI-RJ-70

Cat.No: T73006

Cat.No: T27200

Synonym: doxorubicin-NOP1 conjugate,doxorubicin-NOP1 HCl,DOX−NOP1 Hydrochloride

Cat.No: T16568

Target: Proteasome

Cat.No: T16327

Target: Others

MBC-11 triethylamine

Cat.No: T11956

Target: Others

MBC-11 trisodium

Cat.No: T11957

Target: Others

Cat.No: T70403

Cat.No: T75139

Cat.No: T62534

Cat.No: T73282

Cat.No: T63704

Acyl Carrier Protein (ACP) (65-74)

Cat.No: TP1837

Synonym: Acyl Carrier Protein (ACP) 65-74

Cyclopropenone probe 1

Cat.No: T72328

Cat.No: T74026

Cat.No: T63340

Cat. No.	Product Name	Target	Signaling Pathways
T6830	Epoxomicin BU-4061T,BU-4061T,Aids010837,环氧酶素	Apoptosis; Proteasome	Apoptosis; Proteases/Proteasome; Ubiquitination
	Epoxomicin (BU-4061T,Aids010837) 是一种含环氧酮的天然产物，可穿越血脑屏障，并具有很强的抗肿瘤和抗炎活性。它是一种选择性不可逆的蛋白酶体抑制剂，抑制类胰凝乳蛋白酶的活性。
T3949	Myristic acid 肉豆蔻酸,Crodacid,Tetradecanoic acid,n-Tetradecanoic acid	Others; Endogenous Metabolite	Metabolism; Others
	Myristic acid (Crodacid) 是饱和的 14 碳脂肪酸，存在于大多数动物、植物的脂肪中，特别是乳脂，椰子油，棕榈油和肉豆蔻油。
T40810	Rachelmycin 拉奇霉素,NSC298223,CC-1065
	Rachelmycin (CC-1065; NSC 298223) is a potent naturally antibiotic isolated from Streptomyces zelensis . Rachelmycin binds non-covalently and covalently (N-3 adenine adduct) in the minor groove of B-form DNA. Rachelmycin has exceptionally potent antitumor activity.
T38673	Sibiromycin
	Sibiromycin, a glycosylated pyrrolobenzodiazepines (PBDs) compound, is a naturally occurring and potent antitumor antibiotic. It exerts its activity by covalently binding to DNA in the minor groove at the NH2 of guanine.

天然产物

Cat.No: T6830

Synonym: BU-4061T,BU-4061T,Aids010837,环氧酶素

Target: Apoptosis, Proteasome

Cat.No: T3949

Synonym: 肉豆蔻酸,Crodacid,Tetradecanoic acid,n-Tetradecanoic acid

Target: Others, Endogenous Metabolite

Cat.No: T40810

Synonym: 拉奇霉素,NSC298223,CC-1065

Cat.No: T38673

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