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41

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16027	Mcl1-IN-1	Others	Others
	Mcl1-IN-1 is a myeloid cell factor 1 inhibitor (IC50=2.4 µM).
T16029	Mcl1-IN-3	Others	Others
	Mcl1-IN-3 is an Mcl1 inhibitor. It has an IC50 and Ki of 0.67 and 0.13 μM, respectively.
T11974	Mcl1-IN-12	BCL	Apoptosis
	Mcl1-IN-12 has anti-tumor activity.It is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively.
T11977	Mcl1-IN-9	BCL	Apoptosis
	Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
T11973	Mcl1-IN-11	BCL	Apoptosis
	Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively.
T11975	PROTAC Mcl1 degrader-1	BCL	Apoptosis
	PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.
T16028	IMB-XH1 Mcl1-IN-2,7-[(2-吡啶基氨基)-2-噻吩基甲基]-8-喹啉醇	BCL; Antibacterial	Apoptosis; Microbiology/Virology
	IMB-XH1 (Mcl1-IN-2) 是一种骨髓细胞因子 1 抑制剂。它也是非竞争性的 Delhi metallo-β-lactamase(NDM-1) 抑制剂。它对金属 β-内酰胺酶 NDM-1，IMP-4，ImiS 和 L1 的 IC50值分别为 0.4637 μM，3.980 μM，0.2287 μM 和 1.158 μM。
T11976	Mcl1-IN-4	Others	Others
	Mcl1-IN-4 is an inhibitor of Mcl1 ( IC50:0.2 μM).
T16030	Mcl1-IN-8	Others	Others
	Mcl1-IN-8 is an Mcl-1-PUMA interface inhibitor (Ki: 0.3 μM). In cancer cells, Mcl1-IN-8 shows dual activity on reducing PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis.
T24436	Mcl1-IN-26
	Mcl1-IN-26 is an effective and selective myeloid cell leukemia 1 inhibitor.
T19172	A-1210477-piperazinyl PROTAC Mcl1-binding moiety 1	Others	Others
	A-1210477-piperazinyl is a compound that specifically targets and binds to the protein myeloid cell leukemia 1 (MCL1). This compound is utilized in PROTAC technology, which harnesses the ability to selectively degrade target proteins.
T12041	MIM1 Inhibitor of Mcl-1	BCL	Apoptosis
	MIM1 (Inhibitor of Mcl-1) 是一种骨髓细胞因子 1 抑制剂。
T11972	Mcl-1 inhibitor 3	BCL	Apoptosis
	Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay).
T11967	Mcl-1 antagonist 1	Others	Others
	Mcl-1 antagonist 1 is a Mcl-1 protein antagonist.
T11969	MCL-1/BCL-2-IN-2	Others	Others
	MCL-1/BCL-2-IN-2 is a potent and selective Bcl-2 and Mcl-1 dual inhibitor.
T11971	MCL-1/BCL-2-IN-4	Others	Others
	MCL-1/BCL-2-IN-4 is a selective and potent Mcl-1 and Bcl-2 dual inhibitor.
T40230	Mcl-1 inhibitor 6
	Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d >10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.
T11968	MCL-1/BCL-2-IN-1	BCL	Apoptosis
	MCL-1/BCL-2-IN-2 (Compound Nap-1) 是一种有效的选择性 Mcl-1和 Bcl-2双重抑制剂，IC50分别为 4.45 和 3.18 μM。
T11970	MCL-1/BCL-2-IN-3	Others	Others
	MCL-1/BCL-2-IN-3 is a selective and potent Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectiely.
T13657	dMCL1-2	Others	Others
	dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, which binds to MCL1 with a KD of 30 nM. dmcl-2 activates the apoptosis mechanism by degrading MCL1.
T5346	S63845	BCL	Apoptosis
	S63845 是一种选择性骨髓细胞白血病 1 抑制剂，结合人 MCL1的 Kd 值为 0.19 nM。
T23601	ABC1183 ABC 1183,ABC-1183	GSK-3; CDK	Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
	ABC1183是一种抑制GSK3α， GSK3β和CDK9的新型二氨基噻唑。ABC1183通过诱导G2/M 阻滞和改变GSK3、糖原合成酶、β-catenin 磷酸化和MCL1表达降低细胞存活率来抑制多种癌细胞株的生长，并具有口服活性。
T9083	TC11 CLT-003,1H-Isoindole-1,3(2H)-dione, 5-amino-2-[2,6-bis(1-methylethyl)phenyl]-TC11	BCL; Caspase; CDK	Apoptosis; Cell Cycle/Checkpoint; Proteases/Proteasome
	TC11 (1H-Isoindole-1,3(2H)-dione, 5-amino-2-[2,6-bis(1-methylethyl)phenyl]-TC11) 是一种有效的肿瘤细胞增殖抑制剂，并通过激活 caspase-3、8 和 9 诱导细胞凋亡。在长时间有丝分裂阻滞期间，它诱导 MCL1降解导致凋亡。它作为苯酞酰亚胺衍生物在结构上与免疫调节药物相关。
T22257	Murizatoclax	Others	Others
	AMG 397 is an oral MCL1 inhibitor .
T2632	A-1210477	Apoptosis; BCL	Apoptosis
	A-1210477 是一种选择性的MCL-1有效抑制剂，Ki 值为 0.45 nM。它特异性结合 MCL-1，并以 MCL-1 依赖性方式促进癌细胞凋亡。
T11944	Maritoclax Marinopyrrole A	BCL	Apoptosis
	Maritoclax (Marinopyrrole A) 是一种新型特异性 Mcl-1 抑制剂，IC50值为 10.1 μM，对 BCL-xl 的 IC50值 > 80 μM。
T12629L	MIK665 S-64315	BCL	Apoptosis
	MIK665 (S-64315) (S-64315) 对髓系细胞白血病具有抑制作用。
T6034	UMI-77 UMI77,UMI 77	BCL	Apoptosis
	UMI-77是一种选择性的Mcl-1抑制剂，结合到Mcl-1的 BH3 结合沟，Ki 值为 490 nM，对 Bcl-2 家族的其他成员具有选择性。
T14834	BT2 3,6-二氯-2-苯并噻吩羧酸	BCL	Apoptosis
	BT2 是 BCKDC 激酶(BDK)抑制剂，IC50值为 3.19 μM。它也是一种选择性的Mcl-1抑制剂，Ki 值为 59 μM。BT2 与 BDK 结合触发 N 端结构域的螺旋运动，导致 BDK 从支链 α-酮酸脱氢酶复合物 (BCKDC) 中解离。
T71242	AZD-1897
	AZD-1897 is an ATP-competitive pan-PIM inhibitor. When combined with the Akt inhibitor AZD5363, AML cells from putative leukaemia stem cells incur a reduction in levels of the anti-apoptotic protein MCL1. The combination of PIM and Akt inhibition holds promise for the treatment of AML.
T6281	TW-37 TW 37	BCL	Apoptosis
	TW-37 是重组 Bcl-2、Bcl-xL 和 Mcl-1 的非肽抑制剂，Ki 值分别为 0.26、0.29和1.11μM
T6396	(R)-(-)-Gossypol acetic acid (-)-Gossypol acetic acid,AT-101 (acetic acid),(R)-Gossypol acetic acid,AT101醋酸,AT101,AT101 acetate	BCL; Autophagy	Apoptosis; Autophagy
	(R)-(-)-Gossypol acetic acid (AT101 acetate) 是天然产物 Gossypol 的左旋异构体，与 Bcl-2、Bcl-xL 和 Mcl-1 结合，Ki 为 0.32 μM、0.48 μM 和 0.18 μM。
T70953	AZ5576 racemate
	AZ5576 racemate is a racemic mixture of AZ5576 isomers. AZ5576 is a potent, highly selective, and orally bioavailable inhibitor of Cdk9 that inhibits Cdk9 enzyme activity with an IC50 <5nM and decreases phosphorlyation of Ser2-RNAPII in cells with an IC50 of 96nM. In the MLL-fusion containing acute myeloid leukemia (AML) line, MV411, short-term treatment with AZ5576 led to a rapid dose-dependent decrease in pSer2-RNAPII with concomitant loss of Mcl1 mRNA and protein, resulting in the cleavage a...
T6650	Sabutoclax BI-97C1	BCL	Apoptosis
	Sabutoclax (BI-97C1) 是一种泛 Bcl-2 抑制剂，包括 Bcl-xL、Bcl-2、Mcl-1 和 Bfl-1，IC50 分别为 0.31 μM、0.32 μM、0.20 μM 和 0.62 μM。
T6749	A-1331852	BCL	Apoptosis
	A1331852是一种具有口服活性的BCL-XL 选择性抑制剂，Ki 值小于10 pM。它可用于治疗癌症、免疫和自身免疫疾病。
T76073	BH3 hydrochloride
	BH3 hydrochloride是一种能够穿透血脑屏障的多肽，其机制是通过直接激活促凋亡蛋白Bax/Bak或中和抗凋亡Bcl-2家族蛋白(Bcl-2、Bcl-XL、Bcl-w、mcl1和A-1)，从而诱导细胞凋亡。这一作用是通过与BH3结构域的结合实现的。
T10434	AZD-5991	BCL	Apoptosis
	AZD-5991 is a potent and selective Mcl-1 inhibitor (IC50: 0.7 nM in FRET assay; Kd: 0.17 nM in SPR assay).
T14213	Tapotoclax AMG-176	BCL	Apoptosis
	AMG-176 is a MCL-1 inhibitor (Ki: 0.13 nM).
T79036	Mcl-1 inhibitor 13
	Mcl-1 inhibitor13 (Example 9)，一种MCL-1抑制剂（Ki: 8.2 nM），主要用于癌症相关研究。
T10485	PROTAC Bcl2 degrader-1	BCL	Apoptosis
	PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).
T13459	(+)-Apogossypol Apogossypol,NSC736630	Others	Others
	(+)-Apogossypol is an antagonist of pan-BCL-2. (+)-Apogossypol binds to Mcl-1(Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively).

化合物

Cat.No: T16027

Target: Others

Cat.No: T16029

Target: Others

Cat.No: T11974

Target: BCL

Cat.No: T11977

Target: BCL

Cat.No: T11973

Target: BCL

PROTAC Mcl1 degrader-1

Cat.No: T11975

Target: BCL

Cat.No: T16028

Synonym: Mcl1-IN-2,7-[(2-吡啶基氨基)-2-噻吩基甲基]-8-喹啉醇

Target: BCL, Antibacterial

Cat.No: T11976

Target: Others

Cat.No: T16030

Target: Others

Cat.No: T24436

A-1210477-piperazinyl

Cat.No: T19172

Synonym: PROTAC Mcl1-binding moiety 1

Target: Others

Cat.No: T12041

Synonym: Inhibitor of Mcl-1

Target: BCL

Mcl-1 inhibitor 3

Cat.No: T11972

Target: BCL

Mcl-1 antagonist 1

Cat.No: T11967

Target: Others

MCL-1/BCL-2-IN-2

Cat.No: T11969

Target: Others

MCL-1/BCL-2-IN-4

Cat.No: T11971

Target: Others

Mcl-1 inhibitor 6

Cat.No: T40230

MCL-1/BCL-2-IN-1

Cat.No: T11968

Target: BCL

MCL-1/BCL-2-IN-3

Cat.No: T11970

Target: Others

Cat.No: T13657

Target: Others

Cat.No: T5346

Target: BCL

Cat.No: T23601

Synonym: ABC 1183,ABC-1183

Target: GSK-3, CDK

Cat.No: T9083

Synonym: CLT-003,1H-Isoindole-1,3(2H)-dione, 5-amino-2-[2,6-bis(1-methylethyl)phenyl]-TC11

Target: BCL, Caspase, CDK

Cat.No: T22257

Target: Others

Cat.No: T2632

Target: Apoptosis, BCL

Cat.No: T11944

Synonym: Marinopyrrole A

Target: BCL

Cat.No: T12629L

Synonym: S-64315

Target: BCL

Cat.No: T6034

Synonym: UMI77,UMI 77

Target: BCL

Cat.No: T14834

Synonym: 3,6-二氯-2-苯并噻吩羧酸

Target: BCL

Cat.No: T71242

Cat.No: T6281

Synonym: TW 37

Target: BCL

(R)-(-)-Gossypol acetic acid

Cat.No: T6396

Synonym: (-)-Gossypol acetic acid,AT-101 (acetic acid),(R)-Gossypol acetic acid,AT101醋酸,AT101,AT101 acetate

Target: BCL, Autophagy

AZ5576 racemate

Cat.No: T70953

Cat.No: T6650

Synonym: BI-97C1

Target: BCL

Cat.No: T6749

Target: BCL

BH3 hydrochloride

Cat.No: T76073

Cat.No: T10434

Target: BCL

Cat.No: T14213

Synonym: AMG-176

Target: BCL

Mcl-1 inhibitor 13

Cat.No: T79036

PROTAC Bcl2 degrader-1

Cat.No: T10485

Target: BCL

(+)-Apogossypol

Cat.No: T13459

Synonym: Apogossypol,NSC736630

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T3417	Amentoflavone Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin	Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal	Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
	Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物，有抗炎、抗氧化和神经保护等作用。
T6185	Gambogic Acid 藤黄酸,Beta-Guttiferrin,藤黄酸 A,Guttatic Acid,Guttic Acid	BCL; Autophagy	Apoptosis; Autophagy
	Gambogic Acid (Guttic Acid) 是来自藤黄树的一种藤黄树脂，抑制 Bcl-XL、Bcl-2、Bcl-W、Bcl-B、Bfl-1和 Mcl-1，IC50分别为 1.47 μM、1.21 μM、2.02 μM、0.66 μM、1.06 μM 和 0.79 μM。

天然产物

Cat.No: T3417

Synonym: Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin

Target: Apoptosis, P450, Phospholipase, Reactive Oxygen Species, Opioid Receptor, COX, Antibacterial, RSV, Antifungal

Cat.No: T6185

Synonym: 藤黄酸,Beta-Guttiferrin,藤黄酸 A,Guttatic Acid,Guttic Acid

Target: BCL, Autophagy

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