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Cat. No. Product Name Target Signaling Pathways
T1979 AVN-944

VX-944

Dehydrogenase Metabolism
AVN-944 (VX-944) 是一种选择性的、非竞争性 IMPDH 抑制剂,对IMPDH1和IMPDH2的Ki=为6-10nM。
T19661 8-Chloroadenosine

NSC 354258,8-Cl-Ado,NSC354258,NSC-354258,8-氯腺嘌呤核苷

AMPK Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
8-Chloroadenosine (NSC-354258) 是一种 5' AMP 激活的蛋白激酶激动剂,可能用于治疗慢性淋巴细胞白血病。 它的活性与 mTOR 通路的抑制有关。它是一种核苷类似物。在体内代谢为 8-氯-ATP。在转录过程中掺入 RNA 并抑制 RNA 合成。在 MM.1S、RPMI-8226 和 U266 癌细胞系中表现出细胞毒性;在 A549 和 H1299 细胞中诱导 G2/M 细胞周期停滞和有丝分裂灾难。它已被证明可消耗 ATP 并抑制血液恶性肿瘤以及肺癌和乳腺癌细胞系中的肿瘤生长。
T72762 Proteasome-IN-4

Proteasome-IN-4 是一种良好的非共价 proteasome 抑制剂 (IC50= 8.39 nM)。Proteasome-IN-4 对 RPMI-8226、MM-1S 和 MV-4-11 细胞系具有较强的抗增殖活性。Proteasome-IN-4 可用于癌症研究。
T61754 TMX-4116

TMX-4116为酪蛋白激酶1α (CK1α) 降解剂,具有显著的选择性,尤其是在MOLT4、Jurkat 和 MM.1S 细胞系中,其对CK1α的降解活性强,DC50值低于200 nM。因此,TMX-4116被用于多发性骨髓瘤相关研究。
T39913 TMX-4100

TMX-4100 is a potent degrader of phosphodiesterase 6D (PDE6D), exhibiting high degradation selectivity towards PDE6D with DC50 values below 200 nM in MOLT4, Jurkat, and MM.1S cells. This compound holds significant potential for research pertaining to multiple myeloma.
T78947 CST626

PROTACs PROTAC
CST626 (Compound 9) 为一种pan-IAP PROTAC降解剂,其在MM.1S细胞中对XIAP、cIAP1以及cIAP2的DC50分别为0.7 nM、2.4 nM和6.2 nM。
T36340 Abz-Val-Ala-Asp-Nva-Arg-Asp-Arg-Gln-EDDnp (trifluoroacetate salt)

Abz-Val-Ala-Asp-Nva-Arg-Asp-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human proteinase 3 (kcat/Km = 1,570 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm; em = 420 nm).
T74847 PROTAC pan-IAP degrader-1

PROTACpan-IAP degrader-1 (Compound 9) 是一种 pan-IAPPROTAC 降解剂。PROTACpan-IAP degrader-1 在 MM.1S 细胞中降解 XIAP、cIAP1 和 cIAP2 的 DC50分别为 0.7、2.4 和 6.2 nM。
T60386 LCS-1

LCS-1, a superoxide dismutase 1 (SOD1) inhibitor, effectively inhibits the enzymatic activity of SOD1 with an IC50 value of 1.07 μM. Additionally, LCS-1 triggers both early and late-stage apoptosis in multiple myeloma (MM.1S) cells [1] [2] [3].
T83867 UNC8153 TFA

UNC8153 是一种 NSD2(组蛋白-赖氨酸 N-甲基转移酶)的降解剂,其通过诱导NSD2的降解,具有350 nM的50%降解常数(DC50)值,并且在20 µM浓度下对NSD2具有选择性,而不选择NSD1和NSD3。在MM.1S多发性骨髓瘤细胞中,UNC8153 (10 µM) 能够诱导NSD2降解并减少组蛋白H3赖氨酸36位二甲基化(H3K36me2),这一效应可以被泛素激活酶抑制剂MLN4924所抑制。它减少了表达带有在1099位上谷氨酸到赖氨酸激活突变的NSD2(NSD2E1099K)的MM.1S细胞的增殖,但在20 µM浓度下,对表达野生型NSD2的MDA-MB-231、U2OS或HEK293细胞无效。UNC8153 (20 µM) 降低了在迁移实验中MM.1S细胞的附着能力。
T79523 HDAC6-IN-18

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
HDAC6-IN-18(化合物4)是首个针对HDAC6亚型的不可逆选择性抑制剂,显示出有效的抗多发性骨髓瘤活性。该抑制剂在RPMI8266、U266以及MM.1S细胞系中表现出对HDAC6的抑制效力,其IC50值分别为0.17、0.7和0.42 μM[1]。
T36339 Abz-Ala-Pro-Glu-Glu-Ile-Met-Arg-Arg-Gln-EDDnp

Abz-Ala-Pro-Glu-Glu-Ile-Met-Arg-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human neutrophil elastase (kcat/Km = 531 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm; em = 420 nm).
T63623 XPO1-IN-1

XPO1-IN-1 是口服具有活力的 XPO1 抑制剂,能够作用于 MM.1S 细胞 (IC50: 24 nM)。XPO1-IN-1 可以有效诱导细胞周期阻滞,并使细胞凋亡。XPO1-IN-1 表现出良好的代谢稳定性和药代动力学性质。XPO1-IN-1 能够用于研究多发性骨髓瘤。
T75373 Bz-FVR-AMC

Bz-FVR-AMC 是一种组织蛋白酶荧光底物,kcat/Km 值为 1070 mM-1s-1。高浓度 BZ-FVR-AMC 对底物有抑制作用。储存方式:避光。
T71252 PC-046

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with di...

化合物

AVN-944
Cat.No: T1979
Synonym: VX-944
Target: Dehydrogenase
8-Chloroadenosine
Cat.No: T19661
Synonym: NSC 354258,8-Cl-Ado,NSC354258,NSC-354258,8-氯腺嘌呤核苷
Target: AMPK
Proteasome-IN-4
Cat.No: T72762
Synonym:
Target:
TMX-4116
Cat.No: T61754
Synonym:
Target:
TMX-4100
Cat.No: T39913
Synonym:
Target:
CST626
Cat.No: T78947
Synonym:
Target: PROTACs
Abz-Val-Ala-Asp-Nva-Arg-Asp-Arg-Gln-EDDnp (trifluoroacetate salt)
Cat.No: T36340
Synonym:
Target:
PROTAC pan-IAP degrader-1
Cat.No: T74847
Synonym:
Target:
LCS-1
Cat.No: T60386
Synonym:
Target:
UNC8153 TFA
Cat.No: T83867
Synonym:
Target:
HDAC6-IN-18
Cat.No: T79523
Synonym:
Target: HDAC
Abz-Ala-Pro-Glu-Glu-Ile-Met-Arg-Arg-Gln-EDDnp
Cat.No: T36339
Synonym:
Target:
XPO1-IN-1
Cat.No: T63623
Synonym:
Target:
Bz-FVR-AMC
Cat.No: T75373
Synonym:
Target:
PC-046
Cat.No: T71252
Synonym:
Target:
TargetMol Loading
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