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93

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9072	Tuxobertinib BDTX-189	EGFR; HER; BTK; RIP kinase	Angiogenesis; Apoptosis; JAK/STAT signaling; NF-κB; Tyrosine Kinase/Adaptors
	Tuxobertinib (BDTX-189) 是一种高效可口服的选择性 EGFR 和 HER2变构突变抑制剂，具有抗癌活性。它对 EGFR、HER2、BLK 和 RIPK2 的 KD 值分别为 0.2、0.76、13 和 1.2 nM。
TQ0092	Naquotinib ASP8273	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Naquotinib (ASP8273) 是一种口服的、突变体选择性和不可逆的 EGFR 抑制剂，对EGFR 突变体和EGFR 的IC50值分别为8-33和230 nM。
T24943	VPC-14228 VPC 14228,VPC14228	Androgen Receptor	Endocrinology/Hormones
	VPC-14228 是一种特异性 AR-DBD 抑制剂，通过抑制 Y594A 和 Q592A 突变体起作用。
T31014	Corrector C4 Corr 4a,Corrector C-4,Corr4a,Corrector C 4,Corr-4a	Others	Others
	Corrector C4 是一种常用于研究囊性纤维化突变体的校正子，通过减轻CFTR跨膜结构域突变体与蛋白稳态的相互作用来发挥作用。
T72062	BI-2865	Ras	GPCR/G Protein; MAPK
	BI-2865 是一种非共价的泛-KRAS 抑制剂。BI-2865 可与 KRAS WT、G12C、G12D、G12V 和 G13D 突变体结合，KD 值分别为 6.9、4.5、32、26、4.3 nM。BI-2865在对表达 KRAS G12C、G12D 或 G12V 突变体的 BaF3 细胞实验的过程中显示出抗增殖活性，平均 IC50值大约为 140 nM。
T11761	Tarlox-TKI Kinase inhibitor-1	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Tarlox-TKI (Kinase inhibitor-1) 是一种 pan-ErbB 抑制剂，是 Tarloxotinib 的活性成分，具有抗肿瘤活性。Tarlox-TKI 抑制 NRG1，抑制HER2 突变体。
T22592	ATPγS tetralithium salt ATP-gamma-S tetralithium salt	PERK	Apoptosis
	ATPγS tetralithium salt 是真核生物翻译起始因子 eIF4A 的核苷酸水解和RNA解链活性的底物，与 p97 突变体和朊病毒相关。
T6824	EAI045	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	EAI045是突变体EGFR 的变构抑制剂，在10 μM ATP 时抑制EGFR、EGFRL858R、EGFRT790M 和 EGFRL858R/T790M 的IC50值分别为1.9、0.019、0.19 和 0.002 μM。
T2104	AGI-5198 IDH-C35	Dehydrogenase; Isocitrate Dehydrogenase (IDH)	Metabolism
	AGI-5198 (IDH-C35) 是一种选择性的突变体 IDH1R132H 抑制剂，IC50=0.07 μM。
T2620	G-749 G749	Apoptosis; FLT; c-RET; TAM Receptor; Aurora Kinase	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
	G-749 是一种新型 FLT3 抑制剂，对 FLT3 野生型和突变体有持续的抑制作用，IC50值分别为 0.4 nM 和 0.6 nM。它可用于急性髓系白血病的耐药研究。
T6198	Dolutegravir S/GSK1349572,GSK1349572,度鲁特韦,多替拉韦	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Dolutegravir (GSK1349572) 是口服HIV 整合酶链转移高效抑制剂，抑制 HIV-1 病毒在外周血单个核细胞中的复制。它对耐拉替拉韦的特征突变体 Y143R、Q148K、N155H 和 G140S/Q148H 具有中等活性。
T34656	SKLB 1028 Ruserontinib	EGFR; FLT; Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	SKLB 1028 (Ruserontinib) 是口服活性的、新型的EGFR、FLT3和Abl 多激酶抑制剂。SKLB 1028 在FLT3驱动的AML 模型中显示出优异的活性，在含有Abl 突变体的CML 模型中显示了相当大的效力
T16516	PG01 Phenylglycine-01	CFTR	Membrane transporter/Ion channel
	PG01是一种有效的CFTR Cl-通道增效剂,PG01对 ΔF508（Ka 为 0.3 μM）有效。PG01 对 E193K，G970R 和 G551D (CFTR 突变体)也有效，Kd 值分别为 0.22 μM，0.45 μM 和 1.94 μM 。PG01在加入Forskolin 后可增加ΔF508-CFTR Cl-电流，纠正CFTR 突变体的门控缺陷。
T2147	Nilotinib monohydrochloride monohydrate Nilotinib (monohydrochloride monohydrate),尼洛替尼盐酸盐一水合物,AMN107 (monohydrochloride monohydrate),尼罗替尼中间体	Bcr-Abl; Autophagy	Angiogenesis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Nilotinib monohydrochloride monohydrate (Nilotinib (monohydrochloride monohydrate)) 是酪氨酸酶抑制剂，有效抑制 BCR-ABL 及其突变体。
TQ0277	Pralsetinib 普拉替尼,Blu667	c-RET	Apoptosis; Tyrosine Kinase/Adaptors
	Pralsetinib (Blu667) 是高效的、选择性的RET 抑制剂。它能够抑制 WT RET (IC50:0.4 nM)，RET 突变体 V804L (IC50:0.3 nM)，V804M (IC50:0.4 nM)，M918T (IC50:0.4 nM) 和 CCDC6-RET (IC50:0.4 nM) 的融合。
T7861	Flumatinib mesylate 甲磺酸氟马替尼/氟马替尼,HHGV678 mesylate,甲磺酸氟马替尼	Bcr-Abl; PDGFR; c-Kit	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Flumatinib mesylate (HHGV678 mesylate) 是一种具有口服活性的选择性Bcr-Abl 抑制剂，能够作用于 c-Abl (IC50:1.2 nM)，PDGFRβ (IC50:307.6 nM) 和 c-Kit (IC50:665.5 nM)。
T22324	Ensartinib hydrochloride Ensartinib dihydrochloride,X-396 dihydrochloride	Others; Trk receptor; c-Met/HGFR; ALK	Angiogenesis; Others; Tyrosine Kinase/Adaptors
	Ensartinib hydrochloride (X-396 dihydrochloride) 是双重的 ALK/MET 抑制剂，IC50分别 <0.4 nM 和 0.74 nM。
T2287	PIK-75 hydrochloride PIK-75 HCl,2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐,PIK-75	Apoptosis; DNA-PK; PI3K	Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	PIK-75 hydrochloride (PIK-75 HCl) 是一种可逆的 DNA-PK 和 p110α-选择性抑制剂，抑制 DNA-PK，p110α和 p110γ，可诱导凋亡。
T11438	GNE-1858	Others; MAPK	MAPK; Others
	GNE-1858 是高效的 ATP 竞争性造血祖细胞激酶-1抑制剂，能够抑制野生型(IC50:1.9 nM)、活性模拟突变株 HPK1-TSEE (IC50:1.9 nM)、 HPK1-SA (IC50:4.5 nM)的活性。
T2329	Dolutegravir sodium 度鲁特韦钠,GSK1349572,度鲁特韦钠盐,GSK-1349572A	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Dolutegravir sodium (GSK-1349572A) 是一种高效、口服的 HIV 整合酶链转移抑制剂，在 HIV-1 整合酶催化的链转移中的 IC50值为 2.7 nM，抑制 HIV-1 病毒在外周血单个核细胞中的复制，IC50为 0.51 nM。它对 Y143R，N155H 和 G140S/Q148H 突变体也保持高效。
T8758	Poziotinib hydrochloride HM 781-36B hydrochloride,NOV120101 hydrochloride,波齐替尼盐酸盐	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Poziotinib hydrochloride 不可逆地抑制 EGFR（HER1 或 ErbB1），包括 EGFR 突变体、HER2 和 HER4，从而抑制过度表达这些受体的肿瘤细胞的增殖。它是一种口服生物可利用的、基于喹唑啉的泛表皮生长因子受体（EGFR 或 HER）抑制剂，具有潜在的抗肿瘤活性。
T4428	CCT241736	FLT; Aurora Kinase	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors
	CCT241736 是一种口服生物可利用的双重 FLT3/Aurora 激酶抑制剂，还抑制临床相关的 FLT3 耐药突变体，包括 FLT3-ITD 和 FLT3。它是 CCT137690 的高级类似物，是治疗人类恶性肿瘤的临床前开发候选物。
T75129	Luxdegalutamide ARV-766	Androgen Receptor; PROTACs	Endocrinology/Hormones; PROTAC
	Luxdegalutamide (ARV-766) 是一种可口服且有效的蛋白水解靶向嵌合体 (PROTAC) 的蛋白质降解剂。Luxdegalutamide降解野生型雄激素受体 AR，也降解包括最普遍的致病性 AR L702H、H875Y 和 T878A 突变相关的 AR LBD 突变体。
T63321	20S Proteasome activator 1	Proteasome	Proteases/Proteasome; Ubiquitination
	20S Proteasome activator 1 是一种 20S 蛋白酶激活剂，对胰蛋白酶样位点、胰凝乳蛋白酶样位点和半胱天冬酶位点的 IC50 分别为 0.3 μM、0.7 μM 和 1.8 μM。20S Proteasome activator 1 通过在细胞系统中翻译来防止致病性 α-synuclein A53T 突变体积累从而减少疾病发生的概率。20S Proteasome activator 1 可用于研究神经退行性疾病。
T41068	P53R3	p53	Apoptosis
	P53R3是一种有效的 p53再激活剂。P53R3可恢复 p53热点突变体的序列特异性 DNA 结合，包括p53 R175H、p53 R248W 和p53 R273H。P53R3特异性诱导p53依赖性抗增殖作用，其特异性比PRIMA-1高得多的。P53R3增强野生型p53和p53 M237I 向靶基因启动子的募集。P53R3强烈增强死亡受体死亡受体5（DR5）的mRNA、总蛋白和细胞表面的水平。P53R3用于癌症研究。
T9533	BC-LI-0186 4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide	Others	Others
	BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) 是选择性抑制亮氨酸 tRNA 合成酶与 Ras 相关的 GTP 结合蛋白 D 相互作用(IC50=46.11 nM)。BC-LI-0186能有效抑制肿瘤相关 MTOR 突变体的特性和雷帕霉素耐药癌细胞的生长，能够用于肺癌的相关研究。
T1283	Clinafloxacin 克林沙星,PD 127391,CI-960,AM-1091	Antibacterial; Antibiotic	Microbiology/Virology
	Clinafloxacin (CI-960) 是一种高效广谱氟喹诺酮类抗生素，抑制革兰氏阳性、革兰氏阴性和厌氧病原体。它对金黄色葡萄球菌的 DNA 促旋酶和拓扑异构酶 IV 有抑制作用，IC50值分别为 0.92 µg/ml 和 1.62 µg/ml。
TQ0277L	Pralsetinib HCl (2097132-94-8 free base) Pralsetinib HCl,Pralsetinib hydrochloride,BLU-667,BLU667,BLU 667
	Pralsetinib is a selective and next-generation RET inhibitor (IC50: 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T, and CCDC6-RET fusion). BLU-667 is an effective and selective inhibitor of RET mutations, fusions, and predicted resistant mutants.
T26388	4-CPI 4 CPI
	4-CPI inhibits non-active site mutants of cytochrome P450 2B4.
T70565	Saussureamine C
	Saussureamine C is an inhibitor of H274Y and N294S mutants.
T28988	TNK-6123 TNK6123
	TNK-6123 is an emivirine analog. TNK-6123 has improved activity against drug-resistant HIV mutants.
T69045	ON012380
	ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I.
T15442	GSK864	Others	Others
	GSK864 is an inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant. GSK864 inhibits IDH1 mutants R132C, R132H, and R132G (IC50: 8.8, 15.2, and 16.6 nM).
T40150	Trk-IN-6
	Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants ( IC 50 = 0.2-0.7 nM).
T61179	EMI48
	EMI48, a derivative of EMI1, exhibits increased efficacy against mutant EGFR compared to EMI1. It specifically inhibits EGFR triple mutants [1].
T68368	HWY-5069 bromide
	HWY-5069 bromide is an isoquinolinium derivative that inhibits the proliferation of wild-type and all mutants of Schizosaccharomyces pombe.
T71006	BI-1388
	BI-1388 is a highly potent inhibitor of HCV NS3 protease activity, inhibiting viral replication for various HCV genotypes and for resistant mutants D168V and R155K.
T12175	Naquotinib mesylate ASP8273 (mesylate)	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Naquotinib mesylate (ASP8273 (mesylate)) 是一种口服的、突变体选择性和不可逆的 EGFR 抑制剂，对 EGFR 突变体和 EGFR 的 IC50值分别为8-33和230 nM。
T24944	VPC-14449 VPC14449,VPC 14449
	VPC-14449 is a specific inhibitor of AR-DBD that acts by inhibiting both Y594A and Q592A mutants.
T70844	CM-118
	CM-118 is a potent and selective dual inhibitor of c-Met and ALK which potently abrogates hepatocyte growth factor (HGF)-induced c-Met phosphorylation and cell migration, as well as phosphorylation of ALK, EML4-ALK, and ALK resistance mutants in transfected cells.
T28898	T145 T 145,T-145
	T145 inhibits growth of Enterococcus faecalis, Staphylococcus aureus and Mycobacterium tuberculosis (Mtb) with sub μg/ml potencies that are potentially therapeutically valuable. T145 minimizes selection of spontaneous resistant mutants, a trait that prolo
T70597	G-749 hydrochloride
	G-749 hydrochloride is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays.
T70668	GNE-431
	GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM. GNE-431 showed excellent potency against the C481R, T474I, and T474M mutants. GNE-431 may provide a treatment option to patients, especially those who have acquired resistance to ibrutinib by mutation of Cys481 or Thr474.
T35913	EMI56
	EMI56, a derivative of EMI1, exhibits enhanced potency against mutant EGFR compared to EMI1. Additionally, EMI56 effectively inhibits EGFR triple mutants[1].
T23975	Deacylcortivazol UNII-3JO09QT49F,DAC,NSC 325316
	Deacylcortivazol (DAC) is a potent glucocorticoid. When incubated with glucocorticoid-resistant mutants derived from the glucocorticoid-sensitive human leukemic cell line CEM-C7, DAC caused significant growth inhibition. The cytotoxicity of DAC at concent
T20163L	Acetyltrialanine acetate Acetyltrialanine acetate(19245-85-3 Free base)	Others	Others
	Acetyltrialanine acetate 是鼠伤寒沙门氏菌突变体的氮源。
T31218	DBHDA
	DBHDA is a reagent to convert a Cys into a Dha moiety by reacting with a C-terminal Cys residue and thus allowing the use of recombinant Ubl G76C mutants to prepare probes.
T27201	DPC-082 DPC 082
	DPC-082 is a reverse transcriptase inhibitor. DPC-082 exhibits low-nanomolar potency toward wild-type virus, L100I and K103N single-mutation variants, and multiplies amino acid-substituted HIV type 1 mutants.
T38943	L-Azidonorleucine hydrochloride
	L-Azidonorleucine hydrochloride, an unnatural amino acid, serves as a surrogate for Methionine. It is utilized for labeling mammalian cell proteins and identifying a broad range of methionyl-tRNA synthetase (MetRS) mutants.
TP2116	SAH-SOS1A
	KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Display

化合物

Cat.No: T9072

Synonym: BDTX-189

Target: EGFR, HER, BTK, RIP kinase

Cat.No: TQ0092

Synonym: ASP8273

Target: EGFR

Cat.No: T24943

Synonym: VPC 14228,VPC14228

Target: Androgen Receptor

Cat.No: T31014

Synonym: Corr 4a,Corrector C-4,Corr4a,Corrector C 4,Corr-4a

Target: Others

Cat.No: T72062

Target: Ras

Cat.No: T11761

Synonym: Kinase inhibitor-1

Target: EGFR

ATPγS tetralithium salt

Cat.No: T22592

Synonym: ATP-gamma-S tetralithium salt

Target: PERK

Cat.No: T6824

Target: EGFR

Cat.No: T2104

Synonym: IDH-C35

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T2620

Synonym: G749

Target: Apoptosis, FLT, c-RET, TAM Receptor, Aurora Kinase

Cat.No: T6198

Synonym: S/GSK1349572,GSK1349572,度鲁特韦,多替拉韦

Target: HIV Protease

Cat.No: T34656

Synonym: Ruserontinib

Target: EGFR, FLT, Bcr-Abl

Cat.No: T16516

Synonym: Phenylglycine-01

Target: CFTR

Nilotinib monohydrochloride monohydrate

Cat.No: T2147

Synonym: Nilotinib (monohydrochloride monohydrate),尼洛替尼盐酸盐一水合物,AMN107 (monohydrochloride monohydrate),尼罗替尼中间体

Target: Bcr-Abl, Autophagy

Cat.No: TQ0277

Synonym: 普拉替尼,Blu667

Target: c-RET

Flumatinib mesylate

Cat.No: T7861

Synonym: 甲磺酸氟马替尼/氟马替尼,HHGV678 mesylate,甲磺酸氟马替尼

Target: Bcr-Abl, PDGFR, c-Kit

Ensartinib hydrochloride

Cat.No: T22324

Synonym: Ensartinib dihydrochloride,X-396 dihydrochloride

Target: Others, Trk receptor, c-Met/HGFR, ALK

PIK-75 hydrochloride

Cat.No: T2287

Synonym: PIK-75 HCl,2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐,PIK-75

Target: Apoptosis, DNA-PK, PI3K

Cat.No: T11438

Target: Others, MAPK

Dolutegravir sodium

Cat.No: T2329

Synonym: 度鲁特韦钠,GSK1349572,度鲁特韦钠盐,GSK-1349572A

Target: HIV Protease

Poziotinib hydrochloride

Cat.No: T8758

Synonym: HM 781-36B hydrochloride,NOV120101 hydrochloride,波齐替尼盐酸盐

Target: EGFR

Cat.No: T4428

Target: FLT, Aurora Kinase

Luxdegalutamide

Cat.No: T75129

Synonym: ARV-766

Target: Androgen Receptor, PROTACs

20S Proteasome activator 1

Cat.No: T63321

Target: Proteasome

Cat.No: T41068

Target: p53

Cat.No: T9533

Synonym: 4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide

Target: Others

Cat.No: T1283

Synonym: 克林沙星,PD 127391,CI-960,AM-1091

Target: Antibacterial, Antibiotic

Pralsetinib HCl (2097132-94-8 free base)

Cat.No: TQ0277L

Synonym: Pralsetinib HCl,Pralsetinib hydrochloride,BLU-667,BLU667,BLU 667

Cat.No: T26388

Synonym: 4 CPI

Saussureamine C

Cat.No: T70565

Cat.No: T28988

Synonym: TNK6123

Cat.No: T69045

Cat.No: T15442

Target: Others

Cat.No: T40150

Cat.No: T61179

HWY-5069 bromide

Cat.No: T68368

Cat.No: T71006

Naquotinib mesylate

Cat.No: T12175

Synonym: ASP8273 (mesylate)

Target: EGFR

Cat.No: T24944

Synonym: VPC14449,VPC 14449

Cat.No: T70844

Cat.No: T28898

Synonym: T 145,T-145

G-749 hydrochloride

Cat.No: T70597

Cat.No: T70668

Cat.No: T35913

Deacylcortivazol

Cat.No: T23975

Synonym: UNII-3JO09QT49F,DAC,NSC 325316

Acetyltrialanine acetate

Cat.No: T20163L

Synonym: Acetyltrialanine acetate(19245-85-3 Free base)

Target: Others

Cat.No: T31218

Cat.No: T27201

Synonym: DPC 082

L-Azidonorleucine hydrochloride

Cat.No: T38943

Cat.No: TP2116

Cat. No.	Product Name	Target	Signaling Pathways
T5084	Xanthosine dihydrate 黄苷二水合物	Others; Endogenous Metabolite	Metabolism; Others
	Xanthosine dihydrate 是衍生自黄嘌呤和核糖的核苷，能够提高牛和山羊的乳腺干细胞数量和产奶量。
TN3719	Cristacarpin	p38 MAPK; ROS; CDK; Antifection; p53	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation; MAPK; Microbiology/Virology
	Cristacarpin exhibits moderate but selective activity towards DNA repair-deficient yeast mutants. It promotes endoplasmic reticulum (ER) stress, leading to sub-lethal reactive oxygen species (ROS) generation and which eventually terminates by triggering s

天然产物

Xanthosine dihydrate

Cat.No: T5084

Synonym: 黄苷二水合物

Target: Others, Endogenous Metabolite

Cat.No: TN3719

Target: p38 MAPK, ROS, CDK, Antifection, p53

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