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Cat. No.: HY-156084

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LL-K9-3

Name: LL-K9-3
Brand: MedChemExpress
SKU: HY-156084
Price: 332.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

LL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC₅₀ values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer.
(Pink: CDK9/cyclinT1 ligand (HY-10008); Blue: hydrophobic tag ligand (HY-W093149); Black: linker).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 98.90%
CAS No.: 2809353-52-2
화학식: C₃₁H₄₉N₅O₆S₃
분자량:683.95

보관:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

LL-K9-3 Chemical Structure

CAS No.: 2809353-52-2

사이즈

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재고

수량

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

LL-K9-3 is a selective CDK9-cyclin T1 HyT degrader, with DC₅₀ values of 0.662 μM and 0.589 μM for CDK9 and Cyclin T1, respectively. LL-K9-3 lacks an E3 ligand moiety and induces polyubiquitination and proteasome-mediated synchronous degradation of CDK9 and cyclin T1 via a hydrophobic tag-mediated mechanism. LL-K9-3 downregulates the protein levels of androgen receptor (AR) and c-Myc, and exhibits antiproliferative and pro-apoptotic (apoptosis) activity in prostate cancer cells. LL-K9-3 can be used in studies related to prostate cancer^[1]^[2]. (Pink: CDK9/cyclinT1 ligand (HY-10008); Blue: hydrophobic tag ligand (HY-W093149); Black: linker).

IC₅₀ & Target

^[1]

CDK9

662 nM (DC₅₀)

cyclin T1

589 nM (DC₅₀)

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	0.095 μM Compound: LL-K9-3	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 5 days by CellTiter-Glo assay	[PMID: 35925880]

In Vitro

LL-K9-3 (3 μM; 1-48 h) induces synchronous, time-dependent degradation of CDK9 and Cyclin T1 in 22RV1 cells, with a significant reduction starting at 5-7 h and near-complete depletion observed by 48 h^[1].
LL-K9-3 (5 days) potently inhibits the proliferation of 22RV1 cells, with IC₅₀ values of 95 nM (Ref. 1) and 224.85 nM (Ref. 2)^[1]^[2].
LL-K9-3 (100-400 nM; 14 days) potently inhibits colony formation of 22RV1 cells at nanomolar concentrations^[1].
LL-K9-3 (0.3-1 μM; 24 h) inhibits CDK9 and AR downstream signaling pathways in 22RV1 cells, including reducing the levels of cMyc, MCL-1, AR and AR target proteins^[1].
LL-K9-3 (2 μM; 24 h) inhibits MYC- and AR-mediated oncogenic transcriptional programs in 22RV1 cells^[1].
LL-K9-3 (0.3-1 μM; 24 h) induces G1-phase cell cycle arrest and significant apoptosis in 22RV1 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

22RV1
Concentration:

100, 200, 400 nM
Incubation Time:

14 days
Result:

Inhibited colony formation of 22RV1 cells.

Apoptosis Analysis^[1]

Cell Line:

22RV1
Concentration:

0.3 and 1 μM
Incubation Time:

24 h
Result:

Induced cell apoptosis.

Cell Cycle Analysis^[1]

Cell Line:

22RV1
Concentration:

0.3 and 1 μM
Incubation Time:

24 h
Result:

Induced G1-phase cell cycle arrest.

Western Blot Analysis^[1]

Cell Line:

22RV1
Concentration:

0.3 and 1 μM
Incubation Time:

24 h
Result:

Caused a pronounced decrease in phospho-Rpb1 CTD (Ser2) levels, indicating inhibition of CDK9 downstream signaling.
Reduced MCL-1, full-length AR, AR splice variant ARV7, NKX3-1, and KLK3 levels.

Chemical Information

CAS No. 2809353-52-2
Appearance Solid
분자량 683.95
화학식 C₃₁H₄₉N₅O₆S₃
Color White to off-white
SMILES

O=S(CCNC(CO[C@H]1[C@@H](CC[C@H](C1)C)C(C)C)=O)(N2CCC(CC2)C(NC3=NC=C(SCC4=NC=C(C(C)(C)C)O4)S3)=O)=O
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Li J, et al. Discovery of Small-Molecule Degraders of the CDK9-Cyclin T1 Complex for Targeting Transcriptional Addiction in Prostate Cancer. Journal of medicinal chemistry. 2022 Aug 25;65(16):11034-11057. [Content Brief]

[2]. Lin R, et al. Discovery of HyT-Based Degraders of CDK9-Cyclin T1 Complex. Chemistry & biodiversity. 2023 Aug;20(8):e202300769. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

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LL-K9-3

All CDK Isoforms