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Search Results for " dual-specificity "

26

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2431	ID-8 ID8	DYRK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	ID-8 是 DYRK 抑制剂，长时间培养能够维持胚胎干细胞的自我更新。
T6257	AZ191	DYRK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	AZ191 是特异性 DYRK1B 抑制剂。它对 DYRK1B 的特异性分别是 DYRK1A 和 DYRK2 的 5 倍和 110 倍。
TQ0111	LDN-192960	DYRK; Haspin Kinase	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	LDN-192960 是 Haspin 和 DYRK2 的有效抑制剂（IC50：10 nM 和 48 nM）。
T15422	GSK-626616	DYRK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	GSK-626616 是一种口服具有活力的 DYRK3抑制剂 (IC50:0.7 nM)。它以相似的效力抑制 DYRK 家族的其他成员，可用于研究贫血。
T14980	CLK-IN-T3	DYRK; CDK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	CLK-IN-T3 是 CLK1、CLK2 和 CLK3 的抑制剂，IC50 为 0.67、15 和 110 nM。 CLK-IN-T3 具有抗癌活性。
T40187	GNF2133	DYRK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	GNF2133 是一种有效的特异性 DYRK1A 抑制剂，IC50 为 6.2 nM。 GNF2133 可用于关于 1 型糖尿病的研究。
T11447	GNF4877	GSK-3; DYRK	Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	GNF4877 是一种 DYRK1A (IC50:6 nM) 和 GSK3β (IC50:16 nM) 抑制剂。它导致激活 T 细胞核因子核输出的阻断和 β 细胞增殖细胞增加。
T7323	BCI-215	Phosphatase	Metabolism
	BCI-215 是高效肿瘤细胞选择性的双重特异性磷酸酶DUSP-MKP 抑制剂。它对肿瘤细胞有细胞毒性，但对正常细胞无毒性。
T14364	AZ-Dyrk1B-33 3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine	DYRK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) 是高选择性的Dyrk1B 激酶抑制剂，其IC50=7 nM。
T4636	Protein kinase inhibitors 1	Others; DYRK	Cell Cycle/Checkpoint; Others; Tyrosine Kinase/Adaptors
	Protein kinase inhibitors 1 是新型的 HIPK2 抑制剂，其 IC50=74 nM，Kd=9.5 nM。
T4308	F1063-0967	Phosphatase	Metabolism
	F1063-0967 是双特异性磷酸酶 26 抑制剂，其IC50=11.62 μM。
T16357	DA-3003-1 NSC 663284	Phosphatase	Metabolism
	DA-3003-1 (DA-3003-1) 是一种可渗透进细胞膜且具有有效性和选择性的 Cdc25 dual specificity phosphatase 抑制剂，具有抗肿瘤活性，对 Cdc25B2、Cdc25A、Cdc25B2 和 Cdc25C具有抑制作用。
T12263L	NSC305787 hydrochloride (Rac)-NSC305787 hydrochloride	Others	Others
	NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride) 是一种可透过细胞膜且具有选择性和有效性的小分子 Cdc25 dual specificity phosphatase 和 EZR 双重抑制剂，在胰腺癌细胞中显示出抗肿瘤活性，对Cdc25B2， Cdc25A，Cdc25B2 和 Cdc25C 具有抑制作用。NSC 663284 抑制 NSD2 (IC50 of 170 nM) 酶的活性。
T16350	NSC-87877	Apoptosis; Phosphatase	Apoptosis; Metabolism
	NSC-87877 是一种Shp2和Shp1蛋白质酪氨酸磷酸酶抑制剂，IC50值分别为0.318 μM 和0.355 μM。它还抑制双特异性磷酸酶26。
T10486	BCI (E)-BCI	Phosphatase	Metabolism
	BCI ((E)-BCI) 是双重特异性磷酸酶的变构抑制剂。它特异性抑制 DUSP6和 DUSP1的 EC50分别为 13.3 和 8.0 μM，但不能够抑制 DUSP5。
T7078	NSC 95397	Apoptosis; Phosphatase	Apoptosis; Metabolism
	NSC 95397 是一种选择性的Cdc25双特异性磷酸酶抑制剂。它抑制丝裂原活化蛋白激酶磷酸酶-1(MKP-1)，通过 MKP-1 和 ERK1/2 途径抑制结肠癌细胞的增殖并诱导细胞凋亡。
T2381	Abemaciclib CDK4/6 dual inhibitor,LY2835219	CDK	Cell Cycle/Checkpoint
	Abemaciclib (LY2835219) 是一种 CDK4/6 的双重抑制剂 (IC50=2/10 nM)，具有选择性和特异性。Abemaciclib 具有抗肿瘤活性，被用于治疗晚期或转移性乳腺癌。
T11139	(E/Z)-BCI NSC 150117	Apoptosis; Phosphatase	Apoptosis; Metabolism
	(E/Z)-BCI (NSC-150117) 是一种DUSP6抑制剂，可通过激活 Nrf2 信号和抑制 NF-κB 通路，减弱 LPS 诱导的巨噬细胞炎症和 ROS 生成，具有抗炎活性。
T11830	LDN-192960 hydrochloride	Others	Others
	LDN-192960 hydrochloride is an inhibitor of Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) and Haspin with IC50s of 48 nM and 10 nM, respectively.
T11132	DYRKs-IN-1	DYRK	Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors
	DYRKs-IN-1 has antitumor activity. DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively.
T10486L	BCI hydrochloride (E)-BCI hydrochloride	Others	Others
	BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5. BCI hydrochloride is an allosteric inhibitor of dual specificity phosphatase (DUSP).
T40968	MLS-0437605
	MLS-0437605 is a potent and selective inhibitor of dual-specificity phosphatase 3 (DUSP3), with an IC50 of 3.7 μM. It exhibits higher selectivity towards DUSP3 in comparison to DUSP22 and other protein tyrosine phosphatases (PTPs).
T72242	DYRKs-IN-1 hydrochloride
	DYRKs-IN-1 hydrochloride是一种有效的DYRKs(双特异性酪氨酸磷酸化调节激酶)抑制剂，对DYRK1A和DYRK1B的IC50分别为5 nM和8 nM，具有抗肿瘤活性。
T69826	U-0126
	U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. It was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase and mammalian target of rapamycin pathways.
T71163	Pimasertib HCl
	Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activati...
T60824	Dyrk1A-IN-3
	Dyrk1A-IN-3 (Compound 8b) 是双特异性酪氨酸调节激酶 1A (DYRK1A) 的高选择性抑制剂。Dyrk1A-IN-3与 DYRK1A 结合具有高结合亲和力，IC50值为76 nM。Dyrk1A-IN-3可用于研究神经退行性疾病，例如，阿尔茨海默病、亨廷顿病和帕金森病等。

化合物

Cat.No: T2431

Synonym: ID8

Target: DYRK

Cat.No: T6257

Target: DYRK

Cat.No: TQ0111

Target: DYRK, Haspin Kinase

Cat.No: T15422

Target: DYRK

Cat.No: T14980

Target: DYRK, CDK

Cat.No: T40187

Target: DYRK

Cat.No: T11447

Target: GSK-3, DYRK

Cat.No: T7323

Target: Phosphatase

Cat.No: T14364

Synonym: 3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine

Target: DYRK

Protein kinase inhibitors 1

Cat.No: T4636

Target: Others, DYRK

Cat.No: T4308

Target: Phosphatase

Cat.No: T16357

Synonym: NSC 663284

Target: Phosphatase

NSC305787 hydrochloride

Cat.No: T12263L

Synonym: (Rac)-NSC305787 hydrochloride

Target: Others

Cat.No: T16350

Target: Apoptosis, Phosphatase

Cat.No: T10486

Synonym: (E)-BCI

Target: Phosphatase

Cat.No: T7078

Target: Apoptosis, Phosphatase

Cat.No: T2381

Synonym: CDK4/6 dual inhibitor,LY2835219

Target: CDK

Cat.No: T11139

Synonym: NSC 150117

Target: Apoptosis, Phosphatase

LDN-192960 hydrochloride

Cat.No: T11830

Target: Others

Cat.No: T11132

Target: DYRK

BCI hydrochloride

Cat.No: T10486L

Synonym: (E)-BCI hydrochloride

Target: Others

Cat.No: T40968

DYRKs-IN-1 hydrochloride

Cat.No: T72242

Cat.No: T69826

Cat.No: T71163

Cat.No: T60824

Cat. No.	Product Name	Target	Signaling Pathways
T1711	Harmine Telepathine,去氢骆驼蓬碱	MAO; 5-HT Receptor; DYRK	Cell Cycle/Checkpoint; GPCR/G Protein; Metabolism; Neuroscience; Tyrosine Kinase/Adaptors
	Harmine (Telepathine) 是一种从山茱萸种子中分离出来的生物碱，具有抗癌和抗炎活性。它是双特异性酪氨酸磷酸化调节激酶抑制剂，对5-HT2A 血清素受体具有高亲和力，Ki 值为 397 nM。
T2811	Harmine hydrochloride telepathine hydrochloride,盐酸哈尔明碱	5-HT Receptor; DYRK; GluR	Cell Cycle/Checkpoint; GPCR/G Protein; Neuroscience; Tyrosine Kinase/Adaptors
	Harmine hydrochloride (telepathine hydrochloride) 是一种 DYRK 抑制剂，具有抗癌和抗炎活性。它对5-HT2A 血清素受体具有高亲和力，Ki 值为 397 nM。
T10238	Aclacinomycin A hydrochloride 盐酸阿柔比星,Aclarubicin hydrochloride	Proteasome	Proteases/Proteasome; Ubiquitination
	Aclacinomycin A (Aclarubicin) hydrochloride is a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II.

天然产物

Cat.No: T1711

Synonym: Telepathine,去氢骆驼蓬碱

Target: MAO, 5-HT Receptor, DYRK

Harmine hydrochloride

Cat.No: T2811

Synonym: telepathine hydrochloride,盐酸哈尔明碱

Target: 5-HT Receptor, DYRK, GluR

Aclacinomycin A hydrochloride

Cat.No: T10238

Synonym: 盐酸阿柔比星,Aclarubicin hydrochloride

Target: Proteasome

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