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18

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T16163	MV1	Apoptosis	Apoptosis
	MV1 是一种 IAP 拮抗剂。当与 HaloTag 配体结合时，它会导致 HaloTag 融合蛋白的蛋白质敲低。
T18613	MV-1-NH-Me PROTAC IAP binding moiety 2	Others	Others
	MV-1-NH-Me, an MV-1-derived IAP ligand, connects to an ABL inhibitor through a linker, resulting in the formation of SNIPER[1].
T18685	SNIPER(ABL)-015	Others	Others
	SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5 μM [1].
T18686	SNIPER(ABL)-019	Others	Others
	SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM[1].
T18694	SNIPER(ABL)-050	Others	Others
	SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker. This conjugation results in the reduction of BCR-ABL protein[1].
T15399	GNE-207	Epigenetic Reader Domain	Chromatin/Epigenetic
	GNE-207 is a selective and orally bioavailable inhibitor of the bromodomain of CBP (IC50: 1 nM). It has a selective index of >2500-fold against BRD4 (1). GNE-207 displays excellent CBP potency (EC50: 18 nM for MYC expression in MV-4-11 cells).
T18692	SNIPER(ABL)-047	Others	Others
	SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 2 μM[1].
T82567	Di-4-ANEPPS
	Di-4-ANEPPS为膜电位电压敏感染料，时间分辨率达1 ms优于，并能够呈现每100 mV荧光变化高至10%。常用于描绘心脏电活动图，对兔离体心脏模型的自发心率和心室冲动传导显示出显著直接不可逆影响。
T82393	FLT3/CHK1-IN-1
	FLT3/CHK-IN-1（Compound 18）为FLT3/CHK1双重抑制剂，其对c-KIT的选择性超1700倍，同时显著降低对hERG的亲和力，IC50为58.4 μM。在MV-4-11细胞接种小鼠异种移植模型中有效抑制肿瘤生长。
T74270	PROTAC BRD4 Degrader-17
	PROTACBRD4 Degrader-17 (compound 13i)，作为一种高效的 PROTACBRD4 降解剂，其 IC50 值分别为 29.54 nM（针对 BRD4(BD1)）和 3.82 nM（针对 BRD4(BD2)）。该化合物有效抑制 G2/M 相的细胞周期蛋白 B1 (Cyclin B1) 的表达，并在 MV-4-11 细胞中显著诱导细胞凋亡（apoptosis）。
T79391	FLT3-IN-21
	FLT3-IN-21（复合物LC-3）是一种高效的FLT3抑制剂，具有促进细胞凋亡的能力，其对FLT3酶的半抑制浓度（IC50）为8.4 nM。该化合物能够使细胞周期在G1期停滞，并对FLT3-ITD阳性的AML细胞系MV-4-11显示出显著的抑制作用（IC50：5.3 nM）。在小鼠体内，FLT3-IN-21以每日10 mg/kg的剂量可以有效抑制MV-4-11细胞异种移植瘤的生长，肿瘤生长抑制率（TGI）达到92.16%。
T61005	K783-0308
	K783-0308 是有效的、选择性的MNK2和FLT3的双重抑制剂，IC50值分别为 406 和 680nM。 K783-0308 促进急性髓性白血病 (AML)的细胞凋亡和细胞周期停滞在 G0/G1 期。K783-0308 抑制 MV-4-11 和 MOLM-13 细胞生长，IC50 值分别为 10.4 和 10.5 μM
T78647	PROTAC BRD4 Degrader-16	PROTACs	PROTAC
	PROTACBRD4Degrader-16是一种高效的PROTAC BRD4降解剂，具有对BRD4(BD1)和BRD4(BD2)分别为34.58 nM及40.23 nM的IC50值。该化合物有效抑制G2/M阶段细胞周期蛋白B1（Cyclin B1）的表达，并显著诱导MV-4-11细胞的细胞凋亡（apoptosis）。
T79456	FD1024	Pim	Chromatin/Epigenetic; JAK/STAT signaling
	FD1024是一种PIM抑制剂，对PIM1、PIM2和PIM3的IC50s分别为1.96、38.9及4.17 nM。用于急性髓系白血病研究的FD1024，对AML细胞系显示出显著的抗增殖效果，其对EOL-1、MV-4-11、KG-1和MOLM-16细胞的抑制浓度(IC50s)分别为0.16 μM、0.12 μM、1.05 μM和1.39 μM。此外，FD1024在小鼠模型中也表现出抗肿瘤活性。
T28269	ORY-1001 free base RG 6016,ORY-1001,ORY 1001,ORY1001,RG-6016,RG6016
	ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation a
T79322	Antiproliferative agent-30
	Antiproliferative agent-30 (Compound 8g) 抑制微管蛋白组装且可抑制FLT3及Abl1。该化合物展现出对血管的破坏活性，并对多种癌细胞系表现出强效的抗增殖能力，包括HCT-116、K562及MV-4-11细胞（IC50值分别为0.054 nM、0.008 nM、0.144 nM）。此外，Antiproliferative agent-30 亦对携带FLT3-ITD-TKD突变的AML显示出抗癌效果。
T36215	17R(18S)-EpETE
	17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases ...
T39937	M-808
	M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM.

化合物

Cat.No: T16163

Target: Apoptosis

Cat.No: T18613

Synonym: PROTAC IAP binding moiety 2

Target: Others

SNIPER(ABL)-015

Cat.No: T18685

Target: Others

SNIPER(ABL)-019

Cat.No: T18686

Target: Others

SNIPER(ABL)-050

Cat.No: T18694

Target: Others

Cat.No: T15399

Target: Epigenetic Reader Domain

SNIPER(ABL)-047

Cat.No: T18692

Target: Others

Cat.No: T82567

Cat.No: T82393

PROTAC BRD4 Degrader-17

Cat.No: T74270

Cat.No: T79391

Cat.No: T61005

PROTAC BRD4 Degrader-16

Cat.No: T78647

Target: PROTACs

Cat.No: T79456

Target: Pim

ORY-1001 free base

Cat.No: T28269

Synonym: RG 6016,ORY-1001,ORY 1001,ORY1001,RG-6016,RG6016

Antiproliferative agent-30

Cat.No: T79322

Cat.No: T36215

Cat.No: T39937

Cat. No.	Product Name	Target	Signaling Pathways
T75333	Quinine hemisulfate hydrate
	Quinine hemisulfate hydrate，一种从金鸡纳树皮提取的生物碱，具有抗疟疾效果。作为钾离子通道 (potassium channel) 抑制剂，它能够抑制由电压脉冲触发的MT mSlo3 (KCa5.1) 通道在+100 mV下的电流活动，其IC50值达169 μM。

天然产物

Quinine hemisulfate hydrate

Cat.No: T75333

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